PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 28100326-7 2017 After treatment with the dopamine receptor agonist pramipexole dihydrochloride, the catechol-O-methyltransferase inhibitor entacapone, and vitamin B6, the boy showed mild improvements in hypotonia, blepharoptosis, and oculogyric crisis. entacapone 123-133 catechol-O-methyltransferase Homo sapiens 84-112 27522262-7 2016 (2) Inhibition of catechol-O-methyltransferase enzyme by entacapone decreased the antiproliferative effects of fisetin and quercetin. entacapone 57-67 catechol-O-methyltransferase Homo sapiens 18-46 27456338-8 2016 Since some amount of entacapone can cross the blood-brain barrier, this reagent may enhance L-DOPA transportation by inhibiting COMT and increase the astrocyte-mediated neuroprotective effects of L-DOPA on dopaminergic neurons. entacapone 21-31 catechol-O-methyltransferase Homo sapiens 128-132 27089846-6 2016 It is noteworthy that the inhibition constants (Ki) of tolcapone and entacapone against bilirubin-O-glucuronidation in human liver microsomes (HLM) are determined as 0.68muM and 30.82muM, respectively, which means that the inhibition potency of tolcapone on UGT1A1 mediated bilirubin-O-glucuronidation in HLM is much higher than that of entacapone. entacapone 69-79 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 258-264 27089846-7 2016 Furthermore, the potential risks of tolcapone or entacapone via inhibition of human UGT1A1 were quantitatively predicted by the ratio of the areas under the plasma drug concentration-time curve (AUC). entacapone 49-59 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 84-90 26582803-2 2016 Inhibitors of COMT, such as tolcapone and entacapone, are used clinically in the treatment of Parkinson"s disease. entacapone 42-52 catechol-O-methyltransferase Homo sapiens 14-18 27089846-1 2016 Tolcapone and entacapone are two potent catechol-O-methyltransferase (COMT) inhibitors with a similar skeleton and displaying similar pharmacological activities. entacapone 14-24 catechol-O-methyltransferase Homo sapiens 40-68 27089846-1 2016 Tolcapone and entacapone are two potent catechol-O-methyltransferase (COMT) inhibitors with a similar skeleton and displaying similar pharmacological activities. entacapone 14-24 catechol-O-methyltransferase Homo sapiens 70-74 27089846-4 2016 The results demonstrated that both tolcapone and entacapone exhibited inhibitory effects on UGT1A1, UGT1A7, UGT1A9 and UGT1A10. entacapone 49-59 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 92-98 27089846-4 2016 The results demonstrated that both tolcapone and entacapone exhibited inhibitory effects on UGT1A1, UGT1A7, UGT1A9 and UGT1A10. entacapone 49-59 UDP glucuronosyltransferase family 1 member A7 Homo sapiens 100-106 27089846-4 2016 The results demonstrated that both tolcapone and entacapone exhibited inhibitory effects on UGT1A1, UGT1A7, UGT1A9 and UGT1A10. entacapone 49-59 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 108-114 27089846-4 2016 The results demonstrated that both tolcapone and entacapone exhibited inhibitory effects on UGT1A1, UGT1A7, UGT1A9 and UGT1A10. entacapone 49-59 UDP glucuronosyltransferase family 1 member A10 Homo sapiens 119-126 25834315-1 2015 AIM: To study the effects of entacapone, a catechol-O-methyltransferase inhibitor, on colon motility and electrolyte transport in Parkinson"s disease (PD) rats. entacapone 29-39 catechol-O-methyltransferase Rattus norvegicus 43-71 27074629-3 2016 Tolcapone and entacapone are potent inhibitors of catechol-O-methyl transferase (COMT) for the treatment of Parkinson"s disease. entacapone 14-24 catechol-O-methyltransferase Homo sapiens 50-79 27074629-3 2016 Tolcapone and entacapone are potent inhibitors of catechol-O-methyl transferase (COMT) for the treatment of Parkinson"s disease. entacapone 14-24 catechol-O-methyltransferase Homo sapiens 81-85 26692288-3 2016 In randomized phase III trials, oral carbidopa/levodopa ER was significantly more effective than placebo with regard to improving motor symptoms and activities of daily living in patients with early PD after 30 weeks" treatment, and provided significantly greater reductions in daily "off-time" in patients with advanced PD than immediate-release (IR) carbidopa/levodopa or carbidopa/levodopa IR plus entacapone after a treatment period of 13 and 2 weeks, respectively, without increasing troublesome dyskinesia. entacapone 401-411 epiregulin Homo sapiens 56-58 26844013-1 2016 Tolcapone and entacapone are catechol-O-methyltransferase (COMT) inhibitors developed as adjunct therapies for treating Parkinson"s disease. entacapone 14-24 catechol-O-methyltransferase Homo sapiens 29-57 26844013-1 2016 Tolcapone and entacapone are catechol-O-methyltransferase (COMT) inhibitors developed as adjunct therapies for treating Parkinson"s disease. entacapone 14-24 catechol-O-methyltransferase Homo sapiens 59-63 26295926-1 2015 Entacapone is an inhibitor of catechol-O-methyltransferase (COMT) and is being used to extend the therapeutic effect of levodopa in patients with advanced and fluctuating Parkinson"s disease. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 30-58 26295926-1 2015 Entacapone is an inhibitor of catechol-O-methyltransferase (COMT) and is being used to extend the therapeutic effect of levodopa in patients with advanced and fluctuating Parkinson"s disease. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 60-64 25639262-2 2015 In the STRIDE-PD study, prostate cancer developed in 9 patients (3.7%) receiving levodopa/carbidopa with entacapone, a catechol-O-methyltransferase inhibitor, versus 2 cases (0.9%) without entacapone. entacapone 105-115 catechol-O-methyltransferase Homo sapiens 119-147 25834315-8 2015 The COMT inhibitor entacapone inhibited contraction of the PD rat longitudinal muscle in a dose-dependent manner. entacapone 19-29 catechol-O-methyltransferase Rattus norvegicus 4-8 25834315-16 2015 The beta2 adrenoceptor is involved in the entacapone-induced inhibition of colon motility. entacapone 42-52 adrenoceptor beta 2 Rattus norvegicus 4-22 25301937-5 2015 For example, similarly to the human UGT1A10, dUGT1A11 exhibited high glucuronidation activity toward the 3-OH of 17-beta-estradiol, 17-alpha-estradiol, and ethinylestradiol, and also conjugated the drug entacapone. entacapone 203-213 UDP glucuronosyltransferase family 1 member A10 Homo sapiens 36-43 25435314-5 2015 We found that systemic and local administration of the COMT inhibitor entacapone significantly improves learning performance. entacapone 70-80 catechol-O-methyltransferase Rattus norvegicus 55-59 24928742-7 2014 Methylated metabolites catalyzed by catechol-O-methyl transferase (COMT) were observed mainly in the in vitro incubation with rat liver cytosol, which was verified by using a COMT specific inhibitor entacapone and supported by molecular docking analysis. entacapone 199-209 catechol-O-methyltransferase Rattus norvegicus 36-65 24928742-7 2014 Methylated metabolites catalyzed by catechol-O-methyl transferase (COMT) were observed mainly in the in vitro incubation with rat liver cytosol, which was verified by using a COMT specific inhibitor entacapone and supported by molecular docking analysis. entacapone 199-209 catechol-O-methyltransferase Rattus norvegicus 67-71 24928742-7 2014 Methylated metabolites catalyzed by catechol-O-methyl transferase (COMT) were observed mainly in the in vitro incubation with rat liver cytosol, which was verified by using a COMT specific inhibitor entacapone and supported by molecular docking analysis. entacapone 199-209 catechol-O-methyltransferase Rattus norvegicus 175-179 24148818-2 2014 Entacapone and tolcapone, COMT inhibitors, are used to mitigate the symptoms of Parkinson"s disease. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 26-30 24830331-2 2014 Entacapone, a peripheral inhibitor of catechol-O-methyltransferase (COMT), reduces this motor complication by prolonging the effect of levodopa. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 38-66 24830331-2 2014 Entacapone, a peripheral inhibitor of catechol-O-methyltransferase (COMT), reduces this motor complication by prolonging the effect of levodopa. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 68-72 24148818-9 2014 In conclusion, the combination of EGCG and entacapone/tolcapone synergistically inhibited the growth of lung cancer cells in culture, and the mechanistic basis for this synergy is likely due in part to inhibition of COMT with resultant increase in the levels of unmetabolized EGCG. entacapone 43-53 catechol-O-methyltransferase Homo sapiens 216-220 24229565-4 2014 Hence, inhibition of COMT activity with entacapone should reverse PFC dopaminergic transmission. entacapone 40-50 catechol-O-methyltransferase Homo sapiens 21-25 23265352-9 2013 This result supports our hypothesis, at least in patients with levodopa-resistant FOG, and shows that the co-administration of L-DOPS and entacapone could be a new strategy for FOG treatment. entacapone 138-148 zinc finger protein, FOG family member 1 Homo sapiens 82-85 23673910-4 2013 Pharmacokinetic trials of oral LD/dopa decarboxylase inhibitor (DDCI) formulations with and without the catechol-O-methyltransferase inhibitor, entacapone, showed that repeated administration with entacapone causes an increase in both the maximum concentration (Cmax) and time to Cmax (Tmax) of LD. entacapone 144-154 catechol-O-methyltransferase Homo sapiens 104-132 23673910-4 2013 Pharmacokinetic trials of oral LD/dopa decarboxylase inhibitor (DDCI) formulations with and without the catechol-O-methyltransferase inhibitor, entacapone, showed that repeated administration with entacapone causes an increase in both the maximum concentration (Cmax) and time to Cmax (Tmax) of LD. entacapone 197-207 catechol-O-methyltransferase Homo sapiens 104-132 23281915-8 2013 LDh and LDl were administered in acute challenges in combination with vehicle and, for LDl, with the COMT inhibitor entacapone (5, 15 and 45 mg/kg). entacapone 116-126 catechol-O-methyltransferase Homo sapiens 101-105 23104937-2 2013 Pregnant Sprague-Dawley rats were given entacapone (a catechol-O-methyltransferase inhibitor) by gavage from the 10th to the 20th day of pregnancy. entacapone 40-50 catechol-O-methyltransferase Rattus norvegicus 54-82 23265352-6 2013 Of the 16 PD patients with FOG who completed this study, group 1 (n=6) received L-DOPS co-administered with entacapone, which is a COMT inhibitor used worldwide as an anti-parkinson drug, group 2 (n=5) received entacapone alone, and group 3 (n=5) received L-DOPS alone. entacapone 108-118 catechol-O-methyltransferase Homo sapiens 131-135 23265352-9 2013 This result supports our hypothesis, at least in patients with levodopa-resistant FOG, and shows that the co-administration of L-DOPS and entacapone could be a new strategy for FOG treatment. entacapone 138-148 zinc finger protein, FOG family member 1 Homo sapiens 177-180 23948989-3 2013 Entacapone, a catechol-O-methyltransferase inhibitor, can also be used to improve the bioavailability of levodopa, especially when used in conjunction with a DDCI. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 14-42 22999990-6 2012 The method was successfully validated and applied to the pharmacokinetic study when oral administration of FCE to rats with or without co-giving a COMT inhibitor, entacapone. entacapone 163-173 catechol-O-methyltransferase Rattus norvegicus 147-151 22999990-8 2012 Furthermore, AUC of luteolin was significantly increased by entacapone, while that of chrysoeriol was decreased by entacapone, which revealed COMT might play an important role in the disposition of luteolin in rats after dosing of FCE. entacapone 115-125 catechol-O-methyltransferase Rattus norvegicus 142-146 20641250-15 2004 In clinical studies, AAAD is commonly inhibited with carbidopa, whereas COMT is blocked by entacapone and nitecapone. entacapone 91-101 catechol-O-methyltransferase Homo sapiens 72-76 22860182-7 2012 Finally, novel non-nitrocatechol COMT inhibitors displayed less potent uncoupling of the mitochondrial membrane potential (MMP) compared to tolcapone as well as nonhepatotoxic entacapone, thus mitigating the risk of hepatotoxicity. entacapone 176-186 catechol-O-methyltransferase Homo sapiens 33-37 22123108-2 2012 At the present time, tolcapone and entacapone are the only two COMT inhibitors available in the market. entacapone 35-45 catechol-O-methyltransferase Homo sapiens 63-67 21280081-1 2011 OBJECTIVE: In Parkinson disease (PD), the selective C-O-methyltransferase (COMT) inhibitor entacapone prolongs the effect of levodopa on motor symptoms (ON time) by increasing its bioavailability. entacapone 91-101 catechol-O-methyltransferase Homo sapiens 75-79 21999147-9 2011 The COMT activity inhibiting drugs including tolcapone and entacapone, have shown promising potential as they selectively modulate dopaminergic transmission. entacapone 59-69 catechol-O-methyltransferase Homo sapiens 4-8 21856742-3 2011 Nonetheless, using the specific substrates entacapone and zidovudine (AZT) for UGT1A9 and UGT2B7, respectively, and using an improved ultrafiltration method for measuring drug binding to BSA and to biological membranes, we found that the presence of BSA during the glucuronidation reaction leads to a large increase in the V(max) value of UGT1A9, in addition to lowering its K(m) value. entacapone 43-53 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 79-85 21856742-3 2011 Nonetheless, using the specific substrates entacapone and zidovudine (AZT) for UGT1A9 and UGT2B7, respectively, and using an improved ultrafiltration method for measuring drug binding to BSA and to biological membranes, we found that the presence of BSA during the glucuronidation reaction leads to a large increase in the V(max) value of UGT1A9, in addition to lowering its K(m) value. entacapone 43-53 UDP glucuronosyltransferase family 2 member B7 Homo sapiens 90-96 21501335-1 2011 BACKGROUND: Entacapone is a promising drug used widely for the treatment of Parkinson"s disease (PD) as a catechol-O-methyl transferase (COMT) inhibitor. entacapone 12-22 catechol-O-methyltransferase Rattus norvegicus 106-135 21501335-1 2011 BACKGROUND: Entacapone is a promising drug used widely for the treatment of Parkinson"s disease (PD) as a catechol-O-methyl transferase (COMT) inhibitor. entacapone 12-22 catechol-O-methyltransferase Rattus norvegicus 137-141 21209248-4 2011 When luteolin was coadministered with a specific COMT inhibitor, entacapone, the formation of M1 and M2 was significantly reduced, whereas the plasma concentration of luteolin increased. entacapone 65-75 catechol-O-methyltransferase Rattus norvegicus 49-53 21280081-8 2011 Area under the concentration over time curve of levodopa increased more after entacapone in COMT(HH) than in COMT(LL) patients (+62 +- 6% vs +34 +- 8%, p = 0.01). entacapone 78-88 catechol-O-methyltransferase Homo sapiens 92-96 21280081-9 2011 COMT inhibition by entacapone was higher in COMT(HH) than in COMT(LL) patients (-0.54 +- 0.07 vs -0.31 +- 0.06 pmol/min/mg protein, p = 0.02). entacapone 19-29 catechol-O-methyltransferase Homo sapiens 0-4 21280081-9 2011 COMT inhibition by entacapone was higher in COMT(HH) than in COMT(LL) patients (-0.54 +- 0.07 vs -0.31 +- 0.06 pmol/min/mg protein, p = 0.02). entacapone 19-29 catechol-O-methyltransferase Homo sapiens 44-48 21280081-9 2011 COMT inhibition by entacapone was higher in COMT(HH) than in COMT(LL) patients (-0.54 +- 0.07 vs -0.31 +- 0.06 pmol/min/mg protein, p = 0.02). entacapone 19-29 catechol-O-methyltransferase Homo sapiens 44-48 21280081-10 2011 INTERPRETATION: The COMT(HH) genotype in PD patients enhances the effect of entacapone on the pharmacodynamics and pharmacokinetics of levodopa. entacapone 76-86 catechol-O-methyltransferase Homo sapiens 20-24 21164341-0 2011 Erythrocytes catechol-o-methyl transferase activity is up-regulated after a 3-month treatment by entacapone in parkinsonian patients. entacapone 97-107 catechol-O-methyltransferase Homo sapiens 13-42 21164341-1 2011 OBJECTIVES: Entacapone is a highly potent, reversible, peripherally acting catechol-O-methyl transferase (COMT) inhibitor that is used as an adjunct to L-dopa in the treatment of patients with Parkinson disease (PD). entacapone 12-22 catechol-O-methyltransferase Homo sapiens 75-104 21164341-1 2011 OBJECTIVES: Entacapone is a highly potent, reversible, peripherally acting catechol-O-methyl transferase (COMT) inhibitor that is used as an adjunct to L-dopa in the treatment of patients with Parkinson disease (PD). entacapone 12-22 catechol-O-methyltransferase Homo sapiens 106-110 21164341-2 2011 Nevertheless, the consequence of the long-lasting inhibition of COMT by entacapone has never been investigated. entacapone 72-82 catechol-O-methyltransferase Homo sapiens 64-68 21164341-3 2011 We assessed the variation of the soluble red blood cell (S-RBC)-COMT activity after 3 months of chronic treatment by entacapone. entacapone 117-127 catechol-O-methyltransferase Homo sapiens 64-68 21164341-9 2011 CONCLUSIONS: Our findings suggest that a long-lasting inhibition of the COMT may limit the efficacy of entacapone by development of a tolerance. entacapone 103-113 catechol-O-methyltransferase Homo sapiens 72-76 21524266-7 2011 Results from controlled human laboratory studies and small open-label clinical trials suggest that dronabinol, the COMT inhibitor entacapone, and lithium may warrant further study. entacapone 130-140 catechol-O-methyltransferase Homo sapiens 115-119 20464572-2 2010 The aim of this study was to assess plasma HCY levels in L-DOPA-treated Parkinson"s disease (PD) patients and its influence by adding the inhibitor COMT (entacapone). entacapone 154-164 catechol-O-methyltransferase Homo sapiens 148-152 21280081-0 2011 The COMT Val158Met polymorphism affects the response to entacapone in Parkinson"s disease: a randomized crossover clinical trial. entacapone 56-66 catechol-O-methyltransferase Homo sapiens 4-8 21280081-1 2011 OBJECTIVE: In Parkinson disease (PD), the selective C-O-methyltransferase (COMT) inhibitor entacapone prolongs the effect of levodopa on motor symptoms (ON time) by increasing its bioavailability. entacapone 91-101 catechol-O-methyltransferase Homo sapiens 52-73 20582993-2 2010 It has been hypothesized that providing more continuous delivery of L-dopa to the brain would reduce the risk of motor complications, and that this might be accomplished by combining L-dopa with entacapone, an inhibitor of catechol-O-methyltransferase, to extend its elimination half-life. entacapone 195-205 catechol-O-methyltransferase Homo sapiens 223-251 20856911-5 2010 In recent years, a new, safe, and efficacious armamentarium of treatment options has been provided by the marketing of the catechol-O-methyltransferase (COMT) inhibitor, entacapone, a peripheral blocker of dopa to 3-0-methyldopa metabolism, which increments levodopa brain availability. entacapone 170-180 catechol-O-methyltransferase Homo sapiens 123-151 20856911-5 2010 In recent years, a new, safe, and efficacious armamentarium of treatment options has been provided by the marketing of the catechol-O-methyltransferase (COMT) inhibitor, entacapone, a peripheral blocker of dopa to 3-0-methyldopa metabolism, which increments levodopa brain availability. entacapone 170-180 catechol-O-methyltransferase Homo sapiens 153-157 20572781-7 2010 The addition of the catechol-O-methyltransferase inhibitor entacapone (EN) to LD/carbidopa (CD) improves wearing off, as EN prolongs LD half-life and avoids troughs. entacapone 59-69 catechol-O-methyltransferase Homo sapiens 20-48 20572781-7 2010 The addition of the catechol-O-methyltransferase inhibitor entacapone (EN) to LD/carbidopa (CD) improves wearing off, as EN prolongs LD half-life and avoids troughs. entacapone 71-73 catechol-O-methyltransferase Homo sapiens 20-48 20694135-5 2010 Therefore, agents that prolong levodopa"s half-life were employed, such as carbidopa, an aromatic amino acid decarboxylase (AADC) inhibitor, and entacapone, a catechol-O-methyltransferase (COMT) inhibitor. entacapone 145-155 catechol-O-methyltransferase Homo sapiens 159-187 19629963-2 2010 Entacapone, a COMT inhibitor, prevented the formation of SAH only partially in the striatal homogenate whereas in the kidney homogenate the increase of SAH was prevented by entacapone. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 14-18 20150427-0 2010 Entacapone and tolcapone, two catechol O-methyltransferase inhibitors, block fibril formation of alpha-synuclein and beta-amyloid and protect against amyloid-induced toxicity. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 30-58 20150427-0 2010 Entacapone and tolcapone, two catechol O-methyltransferase inhibitors, block fibril formation of alpha-synuclein and beta-amyloid and protect against amyloid-induced toxicity. entacapone 0-10 synuclein alpha Homo sapiens 97-112 20150427-5 2010 Here, we show that entacapone and tolcapone are potent inhibitors of alpha-syn and beta-amyloid (Abeta) oligomerization and fibrillogenesis, and they also protect against extracellular toxicity induced by the aggregation of both proteins. entacapone 19-29 synuclein alpha Homo sapiens 69-78 20150427-5 2010 Here, we show that entacapone and tolcapone are potent inhibitors of alpha-syn and beta-amyloid (Abeta) oligomerization and fibrillogenesis, and they also protect against extracellular toxicity induced by the aggregation of both proteins. entacapone 19-29 amyloid beta precursor protein Homo sapiens 97-102 20150427-7 2010 Our findings present the first characterization of the anti-amyloidogenic properties of tolcapone and entacapone against both alpha-synuclein and Abeta42 and highlight the potential of this class of nitro-catechol compounds as anti-amyloidogenic agents. entacapone 102-112 synuclein alpha Homo sapiens 126-141 19629963-2 2010 Entacapone, a COMT inhibitor, prevented the formation of SAH only partially in the striatal homogenate whereas in the kidney homogenate the increase of SAH was prevented by entacapone. entacapone 173-183 catechol-O-methyltransferase Rattus norvegicus 14-18 20077469-2 2010 Adding the peripheral acting COMT inhibitor entacapone provides improvement for patients with PD suffering from motor fluctuations. entacapone 44-54 catechol-O-methyltransferase Homo sapiens 29-33 19909787-7 2010 Our results also support the conclusion that COMT inhibitors (entacapone or tolcapone), when administered in PD patients treated with l-Dopa, may potentiate the endogenous AdoHcy-dependent COMT inhibition mechanism already operative in a variable fashion. entacapone 62-72 catechol-O-methyltransferase Homo sapiens 45-49 19879254-0 2010 Entacapone, a catechol-O-methyltransferase inhibitor, improves the motor activity and dopamine content of basal ganglia in a rat model of Parkinson"s disease induced by Japanese encephalitis virus. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 14-42 19879254-5 2010 We analyzed the improvement in motor functions and catecholamine contents in various brain regions induced by a combination of the catechol-O-methyltransferase (COMT) inhibitor entacapone and a levodopa/dopadecarboxylase inhibitor (DDCI) in Japanese encephalitis virus (JEV) induced Parkinson"s disease model rats. entacapone 177-187 catechol-O-methyltransferase Rattus norvegicus 131-159 19909787-7 2010 Our results also support the conclusion that COMT inhibitors (entacapone or tolcapone), when administered in PD patients treated with l-Dopa, may potentiate the endogenous AdoHcy-dependent COMT inhibition mechanism already operative in a variable fashion. entacapone 62-72 catechol-O-methyltransferase Homo sapiens 189-193 19879254-5 2010 We analyzed the improvement in motor functions and catecholamine contents in various brain regions induced by a combination of the catechol-O-methyltransferase (COMT) inhibitor entacapone and a levodopa/dopadecarboxylase inhibitor (DDCI) in Japanese encephalitis virus (JEV) induced Parkinson"s disease model rats. entacapone 177-187 catechol-O-methyltransferase Homo sapiens 161-165 21095463-4 2010 One approach to the CDS is to prolong the half-life of L-dopa inhibiting its degradation by means of the administration of catechol-O-methyltransferase (COMT) inhibitors, as entacapone, a potent, selective, and reversible peripherally acting inhibitor. entacapone 174-184 catechol-O-methyltransferase Rattus norvegicus 123-151 21095464-1 2010 Entacapone and tolcapone are reversible COMT inhibitors which have been approved for clinical use in patients with Parkinson disease (PD). entacapone 0-10 catechol-O-methyltransferase Homo sapiens 40-44 19936145-4 2009 Recent LD trials indicate that a combination of LD with carbidopa (CD) and the catechol-O-methyltransferase (COMT) inhibitor entacapone (EN) may reduce the onset of these motor complications to a certain extent. entacapone 125-135 catechol-O-methyltransferase Homo sapiens 79-107 19783845-3 2010 Tolcapone and entacapone are potent inhibitors of catechol-O-methyltransferase (COMT) for the treatment of Parkinson"s disease. entacapone 14-24 catechol-O-methyltransferase Rattus norvegicus 50-78 19783845-3 2010 Tolcapone and entacapone are potent inhibitors of catechol-O-methyltransferase (COMT) for the treatment of Parkinson"s disease. entacapone 14-24 catechol-O-methyltransferase Rattus norvegicus 80-84 19936145-4 2009 Recent LD trials indicate that a combination of LD with carbidopa (CD) and the catechol-O-methyltransferase (COMT) inhibitor entacapone (EN) may reduce the onset of these motor complications to a certain extent. entacapone 125-135 catechol-O-methyltransferase Homo sapiens 109-113 19936145-4 2009 Recent LD trials indicate that a combination of LD with carbidopa (CD) and the catechol-O-methyltransferase (COMT) inhibitor entacapone (EN) may reduce the onset of these motor complications to a certain extent. entacapone 137-139 catechol-O-methyltransferase Homo sapiens 79-107 19936145-4 2009 Recent LD trials indicate that a combination of LD with carbidopa (CD) and the catechol-O-methyltransferase (COMT) inhibitor entacapone (EN) may reduce the onset of these motor complications to a certain extent. entacapone 137-139 catechol-O-methyltransferase Homo sapiens 109-113 19657587-2 2009 Aim was to investigate the impact of the peripheral COMT inhibitor entacapone (EN) on plasma concentrations of homocysteine, LD and 3-O-methyl-dopa (3-OMD). entacapone 67-77 catechol-O-methyltransferase Homo sapiens 52-56 19657587-2 2009 Aim was to investigate the impact of the peripheral COMT inhibitor entacapone (EN) on plasma concentrations of homocysteine, LD and 3-O-methyl-dopa (3-OMD). entacapone 79-81 catechol-O-methyltransferase Homo sapiens 52-56 19589043-8 2009 Stalevo is a combination tablet comprised of levodopa, carbidopa, and the COMT inhibitor entacapone. entacapone 89-99 catechol-O-methyltransferase Homo sapiens 74-78 19894644-3 2009 Furthermore, entacapone, a COMT inhibitor, is known to retain greater levodopa levels in plasma during coadministration. entacapone 13-23 catechol-O-methyltransferase Rattus norvegicus 27-31 19829918-5 2009 Levodopa/carbidopa/entacapone has been shown to improve the pharmacokinetic profile of levodopa and provide superior symptomatic control compared with conventional levodopa/dopa decarboxylase inhibitor therapy. entacapone 19-29 dopa decarboxylase Homo sapiens 173-191 19412946-1 2009 Controlled-release carbidopa and levodopa (CL-CR) and the combination of carbidopa, levodopa, and entacapone (CLE) are used for extending levodopa (L-dopa) effects. entacapone 98-108 RNA transcription, translation and transport factor Homo sapiens 110-113 18975095-2 2008 To some extent this is provided by Stalevo, which contains levodopa and two enzyme inhibitors: the DDC inhibitor carbidopa and the COMT inhibitor entacapone. entacapone 146-156 catechol-O-methyltransferase Homo sapiens 131-135 18691454-4 2009 Entacapone, a peripheral catechol-O-methyltransferase inhibitor has been shown to reduce OFF time and increase ON time in several therapeutic trials on PD patients treated with LD experiencing motor fluctuations. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 25-53 18520980-6 2008 The 3-OMD levels were significantly lower during catechol-O-methyltransferase (COMT) inhibition with entacapone. entacapone 101-111 catechol-O-methyltransferase Homo sapiens 49-77 19198095-3 2008 Good news were marketing of ropinirole, a new non-ergot agonist, in December 2006 and entacapone, the first catechol-O-methyl transferase (COMT) inhibitor in Japan in April 2007. entacapone 86-96 catechol-O-methyltransferase Homo sapiens 108-137 19198095-3 2008 Good news were marketing of ropinirole, a new non-ergot agonist, in December 2006 and entacapone, the first catechol-O-methyl transferase (COMT) inhibitor in Japan in April 2007. entacapone 86-96 catechol-O-methyltransferase Homo sapiens 139-143 18836344-1 2008 OBJECTIVE: The aim of the study was to explore the potential effect of the catechol-O-methyltransferase inhibitor entacapone coadministration on the rate of absorption and matched latency to motor response of an oral test dose of levodopa/benserazide in the treatment of Parkinson disease (PD). entacapone 114-124 catechol-O-methyltransferase Homo sapiens 75-103 18546331-1 2008 Entacapone (EN) improves the efficacy of levodopa/dopadecarboxylase inhibitor (LD/DDI) formulations by inhibition of the enzyme catechol-O-methyltransferase (COMT). entacapone 0-10 catechol-O-methyltransferase Homo sapiens 128-156 18546331-1 2008 Entacapone (EN) improves the efficacy of levodopa/dopadecarboxylase inhibitor (LD/DDI) formulations by inhibition of the enzyme catechol-O-methyltransferase (COMT). entacapone 0-10 catechol-O-methyltransferase Homo sapiens 158-162 18546331-1 2008 Entacapone (EN) improves the efficacy of levodopa/dopadecarboxylase inhibitor (LD/DDI) formulations by inhibition of the enzyme catechol-O-methyltransferase (COMT). entacapone 12-14 catechol-O-methyltransferase Homo sapiens 128-156 18546331-1 2008 Entacapone (EN) improves the efficacy of levodopa/dopadecarboxylase inhibitor (LD/DDI) formulations by inhibition of the enzyme catechol-O-methyltransferase (COMT). entacapone 12-14 catechol-O-methyltransferase Homo sapiens 158-162 18520980-6 2008 The 3-OMD levels were significantly lower during catechol-O-methyltransferase (COMT) inhibition with entacapone. entacapone 101-111 catechol-O-methyltransferase Homo sapiens 79-83 18290846-1 2008 Catechol-O-methyl transferase (COMT) inhibition by entacapone enhances levodopa absorption and reduces "off" time in Parkinson"s disease (PD). entacapone 51-61 catechol-O-methyltransferase Homo sapiens 0-29 18074122-7 2008 Furthermore, interfering in MDMA metabolism using the catechol-O-methyltransferase inhibitor entacapone potentiated the neurotoxicity of MDMA, indicating that metabolites that are substrates for this enzyme may contribute to neurotoxicity. entacapone 93-103 catechol-O-methyltransferase Rattus norvegicus 54-82 18290846-1 2008 Catechol-O-methyl transferase (COMT) inhibition by entacapone enhances levodopa absorption and reduces "off" time in Parkinson"s disease (PD). entacapone 51-61 catechol-O-methyltransferase Homo sapiens 31-35 18290846-6 2008 Bimodal entacapone increased COMT inhibition, improved the pharmacokinetics of levodopa and improved motor scores for 6 to 8 h. Bimodal use of entacapone may be useful in selected patients to improve motor control and implies that controlled release COMT inhibition would be beneficial in PD patients. entacapone 8-18 catechol-O-methyltransferase Homo sapiens 29-33 18290846-6 2008 Bimodal entacapone increased COMT inhibition, improved the pharmacokinetics of levodopa and improved motor scores for 6 to 8 h. Bimodal use of entacapone may be useful in selected patients to improve motor control and implies that controlled release COMT inhibition would be beneficial in PD patients. entacapone 8-18 catechol-O-methyltransferase Homo sapiens 250-254 18290846-6 2008 Bimodal entacapone increased COMT inhibition, improved the pharmacokinetics of levodopa and improved motor scores for 6 to 8 h. Bimodal use of entacapone may be useful in selected patients to improve motor control and implies that controlled release COMT inhibition would be beneficial in PD patients. entacapone 143-153 catechol-O-methyltransferase Homo sapiens 250-254 18052761-4 2007 Tolcapone and entacapone are selective and potent COMT inhibitors that slow the metabolism of levodopa, thus prolonging its effects. entacapone 14-24 catechol-O-methyltransferase Homo sapiens 50-54 18668620-2 2008 Recent studies have clearly demonstrated that the Off-related FOG is improved by levodopa (L-dopa) or entacapone treatment. entacapone 102-112 zinc finger protein, FOG family member 1 Homo sapiens 62-65 17935716-1 2007 More continuous delivery of l-3,4-dihydroxyphenylalanine (l-dopa) achieved by combination with the catechol-O-methyl transfer (COMT) inhibitor entacapone reduces the onset of dyskinesia in MPTP-treated common marmosets compared with pulsatile l-dopa regimens. entacapone 143-153 catechol O-methyltransferase Callithrix jacchus 99-125 17935716-1 2007 More continuous delivery of l-3,4-dihydroxyphenylalanine (l-dopa) achieved by combination with the catechol-O-methyl transfer (COMT) inhibitor entacapone reduces the onset of dyskinesia in MPTP-treated common marmosets compared with pulsatile l-dopa regimens. entacapone 143-153 catechol O-methyltransferase Callithrix jacchus 127-131 17935716-7 2007 In contrast, the addition of l-dopa BID or QID with entacapone also produced some further improvement in motor function with the combination of entacapone and l-dopa BID significantly improving motor disability compared to l-dopa alone, but no further increase in dyskinesia intensity was observed compared with ropinirole alone treatment. entacapone 52-62 BH3-interacting domain death agonist Callithrix jacchus 166-169 17935716-7 2007 In contrast, the addition of l-dopa BID or QID with entacapone also produced some further improvement in motor function with the combination of entacapone and l-dopa BID significantly improving motor disability compared to l-dopa alone, but no further increase in dyskinesia intensity was observed compared with ropinirole alone treatment. entacapone 144-154 BH3-interacting domain death agonist Callithrix jacchus 36-39 17705259-6 2007 Therefore, the capacity of three catechol-O-methyltransferase (COMT) inhibitors, entacapone, nitecapone, and tolcapone to protect ALP from oxidative damage was also investigated and found to be very similar to the most potent reference antioxidants. entacapone 81-91 alkaline phosphatase, placental Homo sapiens 130-133 17408604-9 2007 On the other hand entacapone, a catechol-O-methyl transferase (COMT) inhibitor, only increased the cytotoxicity of 3",4"-diCl-3,4-diOH-biphenyl, 3",4"-diCl-2,3-diOH-biphenyl and 4"-Cl-2,3-diOH-biphenyl. entacapone 18-28 catechol-O-methyltransferase Rattus norvegicus 32-61 17408604-9 2007 On the other hand entacapone, a catechol-O-methyl transferase (COMT) inhibitor, only increased the cytotoxicity of 3",4"-diCl-3,4-diOH-biphenyl, 3",4"-diCl-2,3-diOH-biphenyl and 4"-Cl-2,3-diOH-biphenyl. entacapone 18-28 catechol-O-methyltransferase Rattus norvegicus 63-67 17495756-6 2007 In addition, preclinical studies suggest that adjunctive use of the catechol-O-methyltransferase (COMT) inhibitor entacapone when levodopa is first introduced may be associated with fewer motor complications than treatment with levodopa alone. entacapone 114-124 catechol-O-methyltransferase Homo sapiens 68-96 17495756-6 2007 In addition, preclinical studies suggest that adjunctive use of the catechol-O-methyltransferase (COMT) inhibitor entacapone when levodopa is first introduced may be associated with fewer motor complications than treatment with levodopa alone. entacapone 114-124 catechol-O-methyltransferase Homo sapiens 98-102 16906435-4 2007 1-Naphthol (hUGT1A6), 1-hydroxypyrene (hUGT1A6/1A9), and entacapone (hUGT1A9) are markers of PAH-glucuronidating human uridine diphosphate-glucuronosyltransferases (UGT). entacapone 57-67 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 69-76 17630819-11 2007 Therefore, agents that block COMT, such as tolcapone and entacapone, increase the elimination half-life of levodopa. entacapone 57-67 catechol-O-methyltransferase Homo sapiens 29-33 16604302-1 2006 Addition of the catechol-O-methyltransferase (COMT) inhibitor entacapone (EN) prolongs plasma metabolism of levodopa (LD). entacapone 74-76 catechol-O-methyltransferase Homo sapiens 16-44 16604302-1 2006 Addition of the catechol-O-methyltransferase (COMT) inhibitor entacapone (EN) prolongs plasma metabolism of levodopa (LD). entacapone 74-76 catechol-O-methyltransferase Homo sapiens 46-50 16026927-7 2005 The ischemia-induced dialysate catecholamines levels were compared with and without the pretreatment with entacapone (COMT inhibitor, 10 mg/kg, i.p.). entacapone 106-116 catechol O-methyltransferase Oryctolagus cuniculus 118-122 16604302-1 2006 Addition of the catechol-O-methyltransferase (COMT) inhibitor entacapone (EN) prolongs plasma metabolism of levodopa (LD). entacapone 62-72 catechol-O-methyltransferase Homo sapiens 16-44 16604302-1 2006 Addition of the catechol-O-methyltransferase (COMT) inhibitor entacapone (EN) prolongs plasma metabolism of levodopa (LD). entacapone 62-72 catechol-O-methyltransferase Homo sapiens 46-50 17948613-7 2006 Catechol-O-methyltransferase (COMT)inhibitors, which increase dopamine levels by inhibiting the metabolism of levodopa and dopamine, recently have become available, including a tablet containing carbidopa, levodopa,and entacapone. entacapone 219-229 catechol-O-methyltransferase Homo sapiens 0-28 17948613-7 2006 Catechol-O-methyltransferase (COMT)inhibitors, which increase dopamine levels by inhibiting the metabolism of levodopa and dopamine, recently have become available, including a tablet containing carbidopa, levodopa,and entacapone. entacapone 219-229 catechol-O-methyltransferase Homo sapiens 30-34 16437585-4 2006 Inhibition of the enzyme catechol-O-methyl transferase (COMT) by entacapone extends the half-life of levodopa and minimizes variability in plasma levodopa levels. entacapone 65-75 catechol-O-methyltransferase Rattus norvegicus 25-54 16437585-4 2006 Inhibition of the enzyme catechol-O-methyl transferase (COMT) by entacapone extends the half-life of levodopa and minimizes variability in plasma levodopa levels. entacapone 65-75 catechol-O-methyltransferase Rattus norvegicus 56-60 16437585-5 2006 The aim of the present study was to characterize the effect of the early administration of the COMT inhibitor entacapone in the recently described model of LIDs in rats with a nigrostriatal lesion induced by 6-hydroxydopamine (6-OHDA). entacapone 110-120 catechol-O-methyltransferase Rattus norvegicus 95-99 16614536-1 2006 Adjunction of the catechol-O-methyltransferase (COMT) inhibitor entacapone (EN) to levodopa/carbidopa (LD/CD) improves motor symptoms in patients with Parkinson disease (PD) by a prolonged elimination of LD. entacapone 64-74 catechol-O-methyltransferase Homo sapiens 18-46 16614536-1 2006 Adjunction of the catechol-O-methyltransferase (COMT) inhibitor entacapone (EN) to levodopa/carbidopa (LD/CD) improves motor symptoms in patients with Parkinson disease (PD) by a prolonged elimination of LD. entacapone 64-74 catechol-O-methyltransferase Homo sapiens 48-52 16614536-1 2006 Adjunction of the catechol-O-methyltransferase (COMT) inhibitor entacapone (EN) to levodopa/carbidopa (LD/CD) improves motor symptoms in patients with Parkinson disease (PD) by a prolonged elimination of LD. entacapone 76-78 catechol-O-methyltransferase Homo sapiens 18-46 16614536-1 2006 Adjunction of the catechol-O-methyltransferase (COMT) inhibitor entacapone (EN) to levodopa/carbidopa (LD/CD) improves motor symptoms in patients with Parkinson disease (PD) by a prolonged elimination of LD. entacapone 76-78 catechol-O-methyltransferase Homo sapiens 48-52 16211593-2 2006 Administration of LD/CD with the catechol-O-methyltransferase inhibitor entacapone in one tablet (LCE) may extend plasma half-life of LD and thus its effect on motor symptoms in patients with Parkinson"s disease (PD). entacapone 72-82 catechol-O-methyltransferase Homo sapiens 33-61 16026927-10 2005 Inhibition of COMT activity by entacapone augmented the ischemia-induced NE levels (54,306+/-6618 pg/ml), EPI levels (2681+/-567 pg/ml), and DA (3551+/-710 pg/ml) levels at the last 15 min of coronary occlusion. entacapone 31-41 catechol O-methyltransferase Oryctolagus cuniculus 14-18 15802387-3 2005 The glucuronidation of entacapone by UGT1A9 was inhibited by 1-naphthol in a competitive fashion, with respect to entacapone, and an uncompetitive fashion, with respect to UDP-glucuronic acid (UDPGA). entacapone 23-33 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 37-43 15614425-0 2005 The COMT inhibitor, entacapone, reduces levodopa-induced elevations in plasma homocysteine in healthy adult rats. entacapone 20-30 catechol-O-methyltransferase Rattus norvegicus 4-8 15614425-3 2005 In this study, the effects of the COMT inhibitor, entacapone, on levodopa-induced hyperhomocysteinaemia were studied in rats. entacapone 50-60 catechol-O-methyltransferase Rattus norvegicus 34-38 15802387-3 2005 The glucuronidation of entacapone by UGT1A9 was inhibited by 1-naphthol in a competitive fashion, with respect to entacapone, and an uncompetitive fashion, with respect to UDP-glucuronic acid (UDPGA). entacapone 114-124 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 37-43 15802387-7 2005 Relative specificity constants were calculated for the eight UGT1A isoforms with 1-hydroxypyrene, 4-nitrophenol, scopoletin, 4-methylumbelliferone, and entacapone as aglycone substrates. entacapone 152-162 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 61-66 15779086-5 2005 tHcy export from astrocytes was also induced by the COMT substrates levodopa (L-DOPA), dopamine and quercetin, and it was blocked by the COMT inhibitors tropolone and entacapone. entacapone 167-177 catechol-O-methyltransferase Homo sapiens 137-141 15907741-4 2005 Randomised, controlled trials have shown that in patients with PD who have motor fluctuations, the addition of the COMT-inhibitor entacapone results in an improvement in motor fluctuations, particularly of the "wearing-off" type, with about 1.0-1.7 h more on-time and less off-time per day, reduced required levodopa dose, modest improvement in motor and disability scores (mean total unified PD rating scale [UPDRS] scores of about 4.5), and in some but not all studies improvement of health-related quality of life [HRQOL] scores. entacapone 130-140 catechol-O-methyltransferase Homo sapiens 115-119 15907741-5 2005 RECENT DEVELOPMENTS: Patients with stable PD, without motor fluctuations, also have improved HRQOL scores on treatment with entacapone in addition to levodopa with a dopa-decarboxylase inhibitor. entacapone 124-134 dopa decarboxylase Homo sapiens 166-184 15878587-4 2005 The objective of our study was to assess the impact of entacapone, a COMT inhibitor, on plasma levels of homocysteine, serum folate, and vitamin B12 in levodopa-treated PD patients. entacapone 55-65 catechol-O-methyltransferase Homo sapiens 69-73 15965309-1 2005 Entacapone is a catechol-O-methyltransferase (COMT) inhibitor used as an adjunct to levodopa/dopa decarboxylase inhibitors in the treatment of Parkinson"s disease. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 16-44 15965309-1 2005 Entacapone is a catechol-O-methyltransferase (COMT) inhibitor used as an adjunct to levodopa/dopa decarboxylase inhibitors in the treatment of Parkinson"s disease. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 46-50 15965309-1 2005 Entacapone is a catechol-O-methyltransferase (COMT) inhibitor used as an adjunct to levodopa/dopa decarboxylase inhibitors in the treatment of Parkinson"s disease. entacapone 0-10 dopa decarboxylase Homo sapiens 93-111 15965309-9 2005 Entacapone significantly reduced plasma 3-OMD concentration by about 50% (P = 0.0001), indicating marked COMT inhibiting activity. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 105-109 15613619-8 2005 In contrast, l-DOPA or the dopamine-metabolizing enzyme inhibitor entacapone suppressed low-salt-induced cortical COX-2 expression. entacapone 66-76 prostaglandin-endoperoxide synthase 2 Homo sapiens 114-119 15503197-4 2005 Catechol-O-methyltransferase (COMT) inhibitors such as entacapone extend the plasma half-life of levodopa and reduce "off" time. entacapone 55-65 catechol-O-methyltransferase Homo sapiens 0-28 15784340-1 2005 Aqueous solubility, apparent partition coefficient (logPapp) and catechol-O-methyltransferase (COMT, EC 2.1.1.6) inhibiting potency of entacapone and tolcapone were compared in vitro. entacapone 135-145 catechol-O-methyltransferase Rattus norvegicus 65-93 15784340-1 2005 Aqueous solubility, apparent partition coefficient (logPapp) and catechol-O-methyltransferase (COMT, EC 2.1.1.6) inhibiting potency of entacapone and tolcapone were compared in vitro. entacapone 135-145 catechol-O-methyltransferase Rattus norvegicus 95-99 15784340-6 2005 Entacapone and tolcapone inhibited equally rat striatal COMT in vitro with Ki values of 1.86 and 2.50 nM, respectively. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 56-60 15784340-10 2005 In conclusion, entacapone and tolcapone are equally potent COMT inhibitors against rat striatal COMT in vitro. entacapone 15-25 catechol-O-methyltransferase Rattus norvegicus 59-63 15784340-10 2005 In conclusion, entacapone and tolcapone are equally potent COMT inhibitors against rat striatal COMT in vitro. entacapone 15-25 catechol-O-methyltransferase Rattus norvegicus 96-100 15784340-11 2005 After local intrastriatal administration, entacapone appeared to inhibit COMT faster and more effectively than the more lipophilic tolcapone. entacapone 42-52 catechol-O-methyltransferase Rattus norvegicus 73-77 15698633-1 2005 The purpose of this study was to investigate the effect of the catechol-O-methyltransferase (COMT) inhibitor, entacapone, in the reversal and prevention of "wearing-off" phenomena in hemiparkinsonian rats. entacapone 110-120 catechol-O-methyltransferase Rattus norvegicus 63-91 15698633-1 2005 The purpose of this study was to investigate the effect of the catechol-O-methyltransferase (COMT) inhibitor, entacapone, in the reversal and prevention of "wearing-off" phenomena in hemiparkinsonian rats. entacapone 110-120 catechol-O-methyltransferase Rattus norvegicus 93-97 15503197-4 2005 Catechol-O-methyltransferase (COMT) inhibitors such as entacapone extend the plasma half-life of levodopa and reduce "off" time. entacapone 55-65 catechol-O-methyltransferase Homo sapiens 30-34 15548391-2 2004 Surprisingly, the corresponding mutation in UGT1A9 (Y483D) doubled the Vmax of scopoletin glucuronidation, whereas the entacapone glucuronidation rate was decreased by about 50%. entacapone 119-129 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 44-50 15548391-7 2004 The UGT1A4 was selected because it glucuronidates neither entacapone nor scopoletin at significant rates. entacapone 58-68 UDP glucuronosyltransferase family 1 member A4 Homo sapiens 4-10 15548391-8 2004 The active enzyme in these hetero-dimers was 1A9Sol, a truncation mutant of UGT1A9 that exhibited a very low ratio of entacapone to scopoletin glucuronidation rates. entacapone 118-128 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 76-82 15548391-9 2004 Interestingly, the ratio of entacapone to scopoletin glucuronidation rates in the co-infected cells was dependent on, and markedly increased with, the probability that 1A9Sol forms hetero-dimers with UGT1A4. entacapone 28-38 UDP glucuronosyltransferase family 1 member A4 Homo sapiens 200-206 15548391-10 2004 In addition, the apparent Km for entacapone in the hetero-dimers was much lower than in 1A9Sol, and resembled the corresponding value in full-length UGT1A9. entacapone 33-43 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 149-155 15379738-1 2004 BACKGROUND: Entacapone is a COMT inhibitor used in Parkinson"s disease (PD) patients, as an adjunctive therapy to L-dopa in order to prolong its bioavailability and thus its clinical effect. entacapone 12-22 catechol-O-methyltransferase Homo sapiens 28-32 15502970-2 2004 This study was aimed at investigating the effect of adding the catechol- O-methyltransferase (COMT) inhibitor entacapone to chronic treatment with l-DOPA/benserazide. entacapone 110-120 catechol-O-methyltransferase Rattus norvegicus 63-92 15502970-2 2004 This study was aimed at investigating the effect of adding the catechol- O-methyltransferase (COMT) inhibitor entacapone to chronic treatment with l-DOPA/benserazide. entacapone 110-120 catechol-O-methyltransferase Rattus norvegicus 94-98 15477510-1 2004 BACKGROUND: The catechol O-methyltransferase inhibitor entacapone acts by extending the elimination half-life of levodopa and is currently approved as an adjunct to levodopa for the treatment of patients with Parkinson disease (PD) with motor fluctuations. entacapone 55-65 catechol-O-methyltransferase Homo sapiens 16-44 15477510-11 2004 CONCLUSIONS: The catechol O-methyltransferase inhibitor entacapone, used as an adjunct to levodopa in PD patients who do not experience motor fluctuations, does not improve Unified Parkinson"s Disease Rating Scale motor scores but does improve a variety of quality-of-life measures. entacapone 56-66 catechol-O-methyltransferase Homo sapiens 17-45 15364620-7 2004 RESULTS: In control, entacapone increased interstitial dihydroxyphenylglycol (DHPG, intraneuronal NE metabolite by monoamine oxidase (MAO)) levels and decreased interstitial normetanephrine (NMN, extraneuronal NE metabolite by COMT) and 3-methoxy-4-hydroxyphenylglycol (MHPG, extraneuronal DHPG metabolite by COMT) levels, but did not change interstitial NE levels. entacapone 21-31 catechol O-methyltransferase Oryctolagus cuniculus 227-231 15364620-7 2004 RESULTS: In control, entacapone increased interstitial dihydroxyphenylglycol (DHPG, intraneuronal NE metabolite by monoamine oxidase (MAO)) levels and decreased interstitial normetanephrine (NMN, extraneuronal NE metabolite by COMT) and 3-methoxy-4-hydroxyphenylglycol (MHPG, extraneuronal DHPG metabolite by COMT) levels, but did not change interstitial NE levels. entacapone 21-31 catechol O-methyltransferase Oryctolagus cuniculus 309-313 15340869-0 2004 Clinical advantages of COMT inhibition with entacapone - a review. entacapone 44-54 catechol-O-methyltransferase Homo sapiens 23-27 15340869-1 2004 Two catechol- O-methyltransferase (COMT) inhibitors, entacapone and tolcapone, were developed during the 1990"s to be used as adjuncts to levodopa (LD) - dopa decarboxylase (DDC) inhibitors in the treatment of Parkinson"s disease (PD). entacapone 53-63 catechol-O-methyltransferase Homo sapiens 4-33 15340869-1 2004 Two catechol- O-methyltransferase (COMT) inhibitors, entacapone and tolcapone, were developed during the 1990"s to be used as adjuncts to levodopa (LD) - dopa decarboxylase (DDC) inhibitors in the treatment of Parkinson"s disease (PD). entacapone 53-63 catechol-O-methyltransferase Homo sapiens 35-39 14975680-1 2004 Tolcapone and entacapone are catechol-O-methyltransferase (COMT) inhibitors used as adjuncts to levodopa in the treatment of Parkinson"s disease (PD). entacapone 14-24 catechol-O-methyltransferase Homo sapiens 29-57 15372589-1 2004 We investigated whether administration of the catechol-O-methyl transferase (COMT) inhibitor entacapone, at doses of 200 mg and 400 mg, alters the pharmacokinetics of apomorphine in Parkinson"s disease patients experiencing severe motor fluctuations. entacapone 93-103 catechol-O-methyltransferase Homo sapiens 46-75 15372589-1 2004 We investigated whether administration of the catechol-O-methyl transferase (COMT) inhibitor entacapone, at doses of 200 mg and 400 mg, alters the pharmacokinetics of apomorphine in Parkinson"s disease patients experiencing severe motor fluctuations. entacapone 93-103 catechol-O-methyltransferase Homo sapiens 77-81 15221622-1 2004 Entacapone is a specific, peripherally acting catechol- O-methyltransferase (COMT) inhibitor that prevents peripheral degradation of L-dopa, thus improving its bioavailability. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 46-75 15221622-1 2004 Entacapone is a specific, peripherally acting catechol- O-methyltransferase (COMT) inhibitor that prevents peripheral degradation of L-dopa, thus improving its bioavailability. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 77-81 15182744-3 2004 Administration of COMT inhibitor (entacapone) decreased dialysate 3-methoxy 4-hydroxyphenylglycol (MHPG) levels. entacapone 34-44 catechol O-methyltransferase Oryctolagus cuniculus 18-22 15044611-7 2004 UGT1A9Sol exhibited a relatively high rate of scopoletin glucuronidation, whereas its activity toward 1-naphthol, entacapone, umbelliferone, and 4-nitrophenol was much lower. entacapone 114-124 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 0-6 14975680-1 2004 Tolcapone and entacapone are catechol-O-methyltransferase (COMT) inhibitors used as adjuncts to levodopa in the treatment of Parkinson"s disease (PD). entacapone 14-24 catechol-O-methyltransferase Homo sapiens 59-63 14767720-1 2004 The aim of this trial was to evaluate the effects of the COMT inhibitor entacapone on both the pharmacokinetic profile and clinical efficacy of controlled release levodopa in Parkinson"s disease (PD) patients. entacapone 72-82 catechol-O-methyltransferase Homo sapiens 57-61 14718678-1 2004 Several prospective double-blind, placebo-controlled trials have demonstrated that combining levodopa with the COMT inhibitor entacapone is efficacious in reducing motor fluctuations. entacapone 126-136 catechol-O-methyltransferase Homo sapiens 111-115 14718679-1 2004 Combining levodopa with the catechol-O-methyltransferase (COMT) inhibitor entacapone has been shown to be an effective strategy in the management of Parkinson"s disease (PD) patients experiencing motor fluctuations. entacapone 74-84 catechol-O-methyltransferase Homo sapiens 28-56 14718679-1 2004 Combining levodopa with the catechol-O-methyltransferase (COMT) inhibitor entacapone has been shown to be an effective strategy in the management of Parkinson"s disease (PD) patients experiencing motor fluctuations. entacapone 74-84 catechol-O-methyltransferase Homo sapiens 58-62 14718680-6 2004 In MPTP monkeys, administration of multiple small doses of levodopa in conjunction with the peripheral COMT inhibitor entacapone removes much of the pulsatility of motor function seen with standard levodopa treatment regimens and, at the same time, results in a lower incidence and intensity of dyskinesia. entacapone 118-128 catechol-O-methyltransferase Homo sapiens 103-107 14741081-1 2004 The catechol-O-methyl transferase inhibitor entacapone is given in combination with levodopa/dopa decarboxylase inhibitor for Parkinson"s disease (PD) patients experiencing end-of-dose wearing-off. entacapone 44-54 catechol-O-methyltransferase Homo sapiens 4-33 15124929-9 2003 Our models propose that increasing steric volume of e.g. the diethylamine tail of entacapone is favourable for COMT inhibitory activity. entacapone 82-92 catechol-O-methyltransferase Homo sapiens 111-115 14630372-4 2003 The MHPG concentrations were reduced by entacapone (catechol-O-methyltransferase inhibitor, COMT), augmented by local infusion of dihydroxyphenylglycol. entacapone 40-50 catechol O-methyltransferase Oryctolagus cuniculus 52-80 14654757-0 2003 Entacapone protects from angiotensin II-induced inflammation and renal injury. entacapone 0-10 angiotensinogen Rattus norvegicus 25-39 14654757-2 2003 We tested the hypothesis whether entacapone, a catechol-O-methyltransferase (COMT) inhibitor exerting antioxidative and anti-inflammatory properties, protects against the Ang II-induced inflammatory response and end-organ damage. entacapone 33-43 catechol-O-methyltransferase Rattus norvegicus 47-75 14654757-2 2003 We tested the hypothesis whether entacapone, a catechol-O-methyltransferase (COMT) inhibitor exerting antioxidative and anti-inflammatory properties, protects against the Ang II-induced inflammatory response and end-organ damage. entacapone 33-43 catechol-O-methyltransferase Rattus norvegicus 77-81 14654757-2 2003 We tested the hypothesis whether entacapone, a catechol-O-methyltransferase (COMT) inhibitor exerting antioxidative and anti-inflammatory properties, protects against the Ang II-induced inflammatory response and end-organ damage. entacapone 33-43 angiotensinogen Rattus norvegicus 171-177 14654757-6 2003 Entacapone ameliorated Ang II-induced vascular and glomerular damage, leucocyte infiltration, and intercellular adhesion molecule-1 (ICAM-1) overexpression in the kidneys. entacapone 0-10 angiotensinogen Rattus norvegicus 23-29 14654757-6 2003 Entacapone ameliorated Ang II-induced vascular and glomerular damage, leucocyte infiltration, and intercellular adhesion molecule-1 (ICAM-1) overexpression in the kidneys. entacapone 0-10 intercellular adhesion molecule 1 Rattus norvegicus 98-131 14654757-6 2003 Entacapone ameliorated Ang II-induced vascular and glomerular damage, leucocyte infiltration, and intercellular adhesion molecule-1 (ICAM-1) overexpression in the kidneys. entacapone 0-10 intercellular adhesion molecule 1 Rattus norvegicus 133-139 14654757-8 2003 Entacapone also decreased p22phox mRNA expression in the kidney. entacapone 0-10 cytochrome b-245 alpha chain Rattus norvegicus 26-33 14654757-11 2003 Even though entacapone decreased renal COMT activity by 40%, the renal dopaminergic tone remained unchanged in entacapone-treated dTGR. entacapone 12-22 catechol-O-methyltransferase Rattus norvegicus 39-43 14654757-12 2003 CONCLUSION: Our findings suggest that entacapone provides protection against Ang II-induced renal damage through antioxidative and anti-inflammatory mechanisms, rather than by COMT inhibition-induced changes in renal dopaminergic tone. entacapone 38-48 angiotensinogen Rattus norvegicus 77-83 12876237-1 2003 OBJECTIVE: To study the effect of entacapone, a specific peripherally acting catechol-O-methyltransferase (COMT) inhibitor used in combination with levodopa treatment, in cases of Parkinson"s disease with both fluctuating and non-fluctuating response to treatment. entacapone 34-44 catechol-O-methyltransferase Homo sapiens 77-105 12876237-10 2003 In this group of patients, ADL scores improved in the entacapone group (p < 0.01 v placebo), and there was also a 40 mg reduction in levodopa requirement (p < 0.01 v placebo). entacapone 54-64 sarcoglycan alpha Homo sapiens 27-30 12876237-13 2003 A novel finding was that patients without fluctuations also obtained benefit from the addition of entacapone to their levodopa treatment, as evidenced by improved ADL scores and a relatively reduced levodopa requirement. entacapone 98-108 sarcoglycan alpha Homo sapiens 163-166 12876237-1 2003 OBJECTIVE: To study the effect of entacapone, a specific peripherally acting catechol-O-methyltransferase (COMT) inhibitor used in combination with levodopa treatment, in cases of Parkinson"s disease with both fluctuating and non-fluctuating response to treatment. entacapone 34-44 catechol-O-methyltransferase Homo sapiens 107-111 12603288-1 2003 The long-term safety and efficacy of the catechol-O-methyltransferase (COMT) inhibitor entacapone was investigated in a 3-year open-label extension of the 6-month double-blind placebo-controlled Nordic (NOMECOMT) study. entacapone 87-97 catechol-O-methyltransferase Homo sapiens 41-69 12904105-1 2003 Entacapone and tolcapone are selective catechol-O-methyltransferase (COMT) inhibitors developed recently as adjuncts to levodopa for the treatment of Parkinson"s disease (PD). entacapone 0-10 catechol-O-methyltransferase Homo sapiens 39-67 12904105-1 2003 Entacapone and tolcapone are selective catechol-O-methyltransferase (COMT) inhibitors developed recently as adjuncts to levodopa for the treatment of Parkinson"s disease (PD). entacapone 0-10 catechol-O-methyltransferase Homo sapiens 69-73 12603288-1 2003 The long-term safety and efficacy of the catechol-O-methyltransferase (COMT) inhibitor entacapone was investigated in a 3-year open-label extension of the 6-month double-blind placebo-controlled Nordic (NOMECOMT) study. entacapone 87-97 catechol-O-methyltransferase Homo sapiens 71-75 12952501-1 2003 Entacapone (Comtess/Comtan) is Orion Pharma"s original proprietary catechol-O-methyl transferase (COMT) inhibitor. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 67-96 12588639-0 2003 Sleep attacks in Parkinson"s disease induced by Entacapone, a COMT-inhibitor. entacapone 48-58 catechol-O-methyltransferase Homo sapiens 62-66 12538800-1 2003 Two catechol-O-methyltransferase (COMT) inhibitors, entacapone and tolcapone, were compared in the rat to elucidate the actual differences between their pharmacokinetics and pharmacodynamics after single and repeated administration. entacapone 52-62 catechol-O-methyltransferase Rattus norvegicus 34-38 12538800-5 2003 After a single oral dose (10 mg/kg), both entacapone and tolcapone produced an equal maximal degree of COMT inhibition in peripheral tissues, but tolcapone inhibited striatal COMT more effectively than did entacapone. entacapone 42-52 catechol-O-methyltransferase Rattus norvegicus 103-107 12538800-5 2003 After a single oral dose (10 mg/kg), both entacapone and tolcapone produced an equal maximal degree of COMT inhibition in peripheral tissues, but tolcapone inhibited striatal COMT more effectively than did entacapone. entacapone 42-52 catechol-O-methyltransferase Rattus norvegicus 175-179 12538800-6 2003 After the 7-day treatment (10 mg/kg twice daily), COMT activity had recovered to a level of 67 to 101% of control within 8 h after the last dose of entacapone. entacapone 148-158 catechol-O-methyltransferase Rattus norvegicus 50-54 12538800-8 2003 The pharmacokinetic-pharmacodynamic modeling revealed that a plateau of COMT inhibition near the maximal attainable inhibition was reached already by plasma concentrations below 2000 ng/ml, both with entacapone and tolcapone. entacapone 200-210 catechol-O-methyltransferase Rattus norvegicus 72-76 12538800-9 2003 Entacapone and tolcapone inhibited equally rat liver COMT in vitro with K(i) values of 10.7 and 10.0 nM, respectively. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 53-57 12952501-1 2003 Entacapone (Comtess/Comtan) is Orion Pharma"s original proprietary catechol-O-methyl transferase (COMT) inhibitor. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 98-102 12573869-1 2003 Tolcapone is a mixed (peripheral and central) catechol-O-methyltransferase (COMT) inhibitor, whereas entacapone is a preferential peripheral COMT inhibitor. entacapone 101-111 catechol-O-methyltransferase Rattus norvegicus 141-145 12573869-5 2003 Tolcapone and entacapone, at the dose of 15 mg/kg p.o., were almost equally effective in inhibiting COMT activity in duodenum and liver. entacapone 14-24 catechol-O-methyltransferase Rattus norvegicus 100-104 12393055-1 2002 Catechol-O-methyl transferase (COMT) inhibitors, entacapone and tolcapone, are used as an adjunctive treatment to L-dopa in Parkinson"s disease. entacapone 49-59 catechol-O-methyltransferase Rattus norvegicus 31-35 12454735-1 2002 The toxicity profiles of entacapone and tolcapone, novel catechol- O-methyl-transferase (COMT) inhibitors, have been reported to differ from each other. entacapone 25-35 catechol-O-methyltransferase Rattus norvegicus 57-87 12454735-1 2002 The toxicity profiles of entacapone and tolcapone, novel catechol- O-methyl-transferase (COMT) inhibitors, have been reported to differ from each other. entacapone 25-35 catechol-O-methyltransferase Rattus norvegicus 89-93 12392583-1 2002 AIMS: Entacapone is a peripherally acting catechol-O-methyltransferase (COMT) inhibitor. entacapone 6-16 catechol-O-methyltransferase Homo sapiens 42-70 12392583-1 2002 AIMS: Entacapone is a peripherally acting catechol-O-methyltransferase (COMT) inhibitor. entacapone 6-16 catechol-O-methyltransferase Homo sapiens 72-76 12393055-6 2002 The COMT inhibitory activity of entacapone was reduced to half, while tolcapone had only about 1/10 of its activity left in the presence of serum. entacapone 32-42 catechol-O-methyltransferase Rattus norvegicus 4-8 12111468-0 2002 Different modes of action of catecholamine-O-methyltransferase inhibitors entacapone and tolcapone on adenylyl cyclase activity in vitro. entacapone 74-84 catechol-O-methyltransferase Rattus norvegicus 29-62 12135946-2 2002 METHODS AND RESULTS: We studied incremental doses of the COMT inhibitor entacapone, the sympathetic stimulant yohimbine, and placebo in 7 patients with multiple system atrophy (Shy Drager syndrome). entacapone 72-82 catechol-O-methyltransferase Homo sapiens 57-61 12083995-1 2002 Entacapone is one of a new class of drugs, the catechol-O-methyltransferase (COMT) inhibitors, which expand the therapeutic options for Parkinson"s disease by extending the action of levodopa. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 47-75 12083995-1 2002 Entacapone is one of a new class of drugs, the catechol-O-methyltransferase (COMT) inhibitors, which expand the therapeutic options for Parkinson"s disease by extending the action of levodopa. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 77-81 12180806-1 2002 Entacapone and tolcapone, novel catechol-O-methyl-transferase (COMT) inhibitors, have been developed for the treatment of Parkinson"s disease in combination with levodopa. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 32-61 12180806-1 2002 Entacapone and tolcapone, novel catechol-O-methyl-transferase (COMT) inhibitors, have been developed for the treatment of Parkinson"s disease in combination with levodopa. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 63-67 12403054-1 2002 The aim of this in vivo study was to assess the effect of improved oral bioavailability of entacapone on its actual pharmacodynamic response, COMT inhibition in erythrocytes. entacapone 91-101 catechol-O-methyltransferase Rattus norvegicus 142-146 12403054-4 2002 The administration of entacapone as a solution (plain solution pH 7.4; F=34.8% or entacapone/HP-beta-CD solution pH 3.0; F = 18.5%) resulted in significantly higher degree of COMT inhibition in erythrocytes than could be achieved by administering entacapone as a suspension (pH 3.0; F=8.9%). entacapone 22-32 catechol-O-methyltransferase Rattus norvegicus 175-179 12403054-4 2002 The administration of entacapone as a solution (plain solution pH 7.4; F=34.8% or entacapone/HP-beta-CD solution pH 3.0; F = 18.5%) resulted in significantly higher degree of COMT inhibition in erythrocytes than could be achieved by administering entacapone as a suspension (pH 3.0; F=8.9%). entacapone 82-92 catechol-O-methyltransferase Rattus norvegicus 175-179 12403054-4 2002 The administration of entacapone as a solution (plain solution pH 7.4; F=34.8% or entacapone/HP-beta-CD solution pH 3.0; F = 18.5%) resulted in significantly higher degree of COMT inhibition in erythrocytes than could be achieved by administering entacapone as a suspension (pH 3.0; F=8.9%). entacapone 82-92 catechol-O-methyltransferase Rattus norvegicus 175-179 12111468-1 2002 Catechol-O-methyltransferase (COMT) inhibitors such as entacapone and tolcapone are used as adjuncts to L-DOPA ( l-3,4-dihydroxyphenylalanine, levodopa) in the treatment of Parkinson"s disease. entacapone 55-65 catechol-O-methyltransferase Rattus norvegicus 0-28 12111468-1 2002 Catechol-O-methyltransferase (COMT) inhibitors such as entacapone and tolcapone are used as adjuncts to L-DOPA ( l-3,4-dihydroxyphenylalanine, levodopa) in the treatment of Parkinson"s disease. entacapone 55-65 catechol-O-methyltransferase Rattus norvegicus 30-34 12111468-5 2002 The aim of this study was to examine the effects of the COMT inhibitors entacapone and tolcapone on AC activity in membranes isolated from rat striatum, a brain structure enriched with dopaminergic G-protein-coupled receptors and AC activity. entacapone 72-82 catechol-O-methyltransferase Rattus norvegicus 56-60 11806720-3 2002 Of this series, compound 7b (1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone) was found to exhibit the most potent and selective inhibition of peripheral COMT, with an inhibition profile more similar to entacapone 2 than tolcapone 1 (an equipotent peripheral and central inhibitor) but with much improved duration of action (7b, 70% inhibition and 2, 25% inhibition at 9 h after administration). entacapone 205-215 catechol-O-methyltransferase Rattus norvegicus 156-160 11994054-0 2002 Effect of the catechol-O-methyltransferase inhibitor entacapone on the steady-state pharmacokinetics and pharmacodynamics of warfarin. entacapone 53-63 catechol-O-methyltransferase Homo sapiens 14-42 11994054-1 2002 AIMS: To investigate the influence of a multiple-dose regimen with the catechol-O-methyltransferase inhibitor entacapone on the pharmacokinetics and pharmacodynamics of warfarin. entacapone 110-120 catechol-O-methyltransferase Homo sapiens 71-99 11939936-1 2002 OBJECTIVES: To determine the efficacy and safety of the catechol-O-methyltransferase (COMT) inhibitor entacapone, used as an adjunct to levodopa, in Parkinson"s disease (PD) patients. entacapone 102-112 catechol-O-methyltransferase Homo sapiens 56-84 11939936-1 2002 OBJECTIVES: To determine the efficacy and safety of the catechol-O-methyltransferase (COMT) inhibitor entacapone, used as an adjunct to levodopa, in Parkinson"s disease (PD) patients. entacapone 102-112 catechol-O-methyltransferase Homo sapiens 86-90 11865133-0 2002 COMT genotype and effectiveness of entacapone in patients with fluctuating Parkinson"s disease. entacapone 35-45 catechol-O-methyltransferase Homo sapiens 0-4 11865133-1 2002 OBJECTIVE: To investigate the relationship between the catechol-O-methyltransferase (COMT) genotype and the therapeutic efficacy of entacapone. entacapone 132-142 catechol-O-methyltransferase Homo sapiens 55-83 11865133-1 2002 OBJECTIVE: To investigate the relationship between the catechol-O-methyltransferase (COMT) genotype and the therapeutic efficacy of entacapone. entacapone 132-142 catechol-O-methyltransferase Homo sapiens 85-89 11865133-5 2002 Two months of entacapone treatment resulted in a significant increase in "on" time, a reduction in "off" time, and a reduction in the total UPDRS score, but these results were independent of the COMT genotype of the patient. entacapone 14-24 catechol-O-methyltransferase Homo sapiens 195-199 11865133-7 2002 CONCLUSION: The COMT genotype seems to be a minor factor in judging the beneficial effects of entacapone administration. entacapone 94-104 catechol-O-methyltransferase Homo sapiens 16-20 11732751-1 2001 Entacapone is a new inhibitor of catechol-O-methyltransferase (COMT) that is used as an adjunct to L-dopa therapy in the treatment of Parkinson"s disease. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 33-61 11978145-16 2002 The COMT inhibitors entacapone and tolcapone dose-dependently inhibit the formation of the major metabolite of levodopa, 3-O-methyldopa, and improve the bioavailability and reduce the clearance of levodopa without significantly affecting its absorption. entacapone 20-30 catechol-O-methyltransferase Homo sapiens 4-8 11844927-8 2002 In later disease when patients have already developed motor complications on levodopa, the choice rests between adjuvant therapy with a dopamine agonist, a catechol-O-methyltransferase inhibitor (COMT; e.g. entacapone), and a monoamine oxidase B inhibitor (MAO B; e.g. selegiline). entacapone 207-217 catechol-O-methyltransferase Homo sapiens 196-200 11793162-0 2002 Chronic high dose L-DOPA alone or in combination with the COMT inhibitor entacapone does not increase oxidative damage or impair the function of the nigro-striatal pathway in normal cynomologus monkeys. entacapone 73-83 catechol-O-methyltransferase Homo sapiens 58-62 11732751-1 2001 Entacapone is a new inhibitor of catechol-O-methyltransferase (COMT) that is used as an adjunct to L-dopa therapy in the treatment of Parkinson"s disease. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 63-67 11586115-2 2001 Tolcapone and entacapone are two currently available catechol- O -methyltransferase inhibitors that have demonstrated efficacy in the treatment of advanced PD. entacapone 14-24 catechol-O-methyltransferase Homo sapiens 53-83 11290882-8 2001 Peripheral COMT inhibition with entacapone does not significantly alter cardiovascular autonomic responses in L-Dopa-treated patients with PD. entacapone 32-42 catechol-O-methyltransferase Homo sapiens 11-15 11498717-2 2001 OBJECTIVES: This study assessed the behavioural and pharmacokinetic effects of chronic oral administration of L-dopa plus carbidopa alone, or with co-administration of the peripheral COMT inhibitor entacapone, to normal macaque monkeys. entacapone 198-208 catechol-O-methyltransferase Homo sapiens 183-187 11498717-3 2001 Repeated high dose L-dopa administration was shown to induce marked dyskinesias in monkeys with an intact nigrostriatal system, and the threshold for dyskinesia expression was increased by peripheral catechol-O-methyltransferase inhibition with entacapone. entacapone 245-255 catechol-O-methyltransferase Homo sapiens 200-228 11510881-2 2001 We have previously shown that inhibition of COMT by entacapone results in a potent D1-like receptor-mediated natriuretic response. entacapone 52-62 catechol-O-methyltransferase Rattus norvegicus 44-48 11440283-0 2001 Entacapone: a catechol-O-methyltransferase inhibitor for the adjunctive treatment of Parkinson"s disease. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 14-42 11440283-4 2001 Entacapone is a selective inhibitor of COMT whose activity is primarily in the peripheral nervous system, with little effect in the central nervous system. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 39-43 11391126-5 2001 Entacapone decreased the COMT activity from predose level: 100 mg by 25%, 200 mg by 33%, and 400 mg by 32% (p < 0.001 vs. placebo for each dose). entacapone 0-10 catechol-O-methyltransferase Homo sapiens 25-29 11391126-12 2001 The study showed that repeated dosing of entacapone inhibits the COMT activity in a dose-dependent manner and thereby reduces the loss of L-Dopa to 3-OMD. entacapone 41-51 catechol-O-methyltransferase Homo sapiens 65-69 11318939-1 2001 BACKGROUND: In recent years, several nitrocatechol derivatives (tolcapone, entacapone, and nitecapone) have been developed and found to be highly selective and potent inhibitors of catechol-O-methyltransferase (COMT). entacapone 75-85 catechol-O-methyltransferase Rattus norvegicus 181-209 11318939-1 2001 BACKGROUND: In recent years, several nitrocatechol derivatives (tolcapone, entacapone, and nitecapone) have been developed and found to be highly selective and potent inhibitors of catechol-O-methyltransferase (COMT). entacapone 75-85 catechol-O-methyltransferase Rattus norvegicus 211-215 11160877-8 2001 Among the catechol drugs used in the L-DOPA treatment of Parkinson"s disease, the COMT inhibitors entacapone and tolcapone were not methylated, whereas the DOPA decarboxylase inhibitor benserazide was 15 times more specific substrate than L-DOPA, the target of COMT inhibition. entacapone 98-108 catechol-O-methyltransferase Homo sapiens 82-86 11294372-0 2001 Pharmacokinetics of entacapone, a peripherally acting catechol-O-methyltransferase inhibitor, in man. entacapone 20-30 catechol-O-methyltransferase Homo sapiens 54-82 11294372-2 2001 OBJECTIVE: This study investigated the pharmacokinetics of the catechol-O-methyltransferase (COMT) inhibitor entacapone by giving simultaneously stable non-radioactive isotope 13C-entacapone intravenously (i.v.) entacapone 109-119 catechol-O-methyltransferase Homo sapiens 63-91 11294372-2 2001 OBJECTIVE: This study investigated the pharmacokinetics of the catechol-O-methyltransferase (COMT) inhibitor entacapone by giving simultaneously stable non-radioactive isotope 13C-entacapone intravenously (i.v.) entacapone 109-119 catechol-O-methyltransferase Homo sapiens 93-97 11261749-1 2001 Entacapone and tolcapone are novel COMT (catechol-O-methyltransferase) inhibitors indicated for the adjunctive treatment of Parkinson"s disease (PD) in combination with levodopa. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 35-39 11261749-1 2001 Entacapone and tolcapone are novel COMT (catechol-O-methyltransferase) inhibitors indicated for the adjunctive treatment of Parkinson"s disease (PD) in combination with levodopa. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 41-69 11261749-9 2001 We conclude that the toxicological profile of the two COMT inhibitors, entacapone and tolcapone, differ from each other, tolcapone--unlike entacapone--showed hepatotoxicity. entacapone 71-81 catechol-O-methyltransferase Rattus norvegicus 54-58 11314772-2 2001 To investigate this hypothesis, the acute effects of two doses of the systemically administered COMT inhibitors entacapone (peripheral) and tolcapone (peripheral and central) on the extracellular formation of hydroxyl radicals in vivo following treatment with L-DOPA and the AADC inhibitor carbidopa were examined. entacapone 112-122 catechol-O-methyltransferase Rattus norvegicus 96-100 10703007-4 2000 We review data, especially on the remaining COMT inhibitor, entacapone, with regard to pre-clinical and clinical efficacy and safety. entacapone 60-70 catechol-O-methyltransferase Homo sapiens 44-48 11244274-1 2001 Entacapone is a potent, reversible and orally active inhibitor of catechol-O-methyltransferase. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 66-94 11038168-1 2000 The COMT inhibitors entacapone and tolcapone are rapidly metabolized in vivo, mainly by glucuronidation. entacapone 20-30 catechol-O-methyltransferase Homo sapiens 4-8 11038168-3 2000 Entacapone in particular was seen to be an exceptionally good substrate for UGT1A9 with an even higher reaction velocity value at 500 microM substrate concentration compared with that of the commonly used substrate, propofol (1.3 and 0.78 nmol min(-1) mg(-1), respectively). entacapone 0-10 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 76-82 11038168-6 2000 However, UGT1A1 was the only UGT capable of catalyzing the formation of two glucuronides of the catecholic entacapone. entacapone 107-117 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 9-15 11038168-6 2000 However, UGT1A1 was the only UGT capable of catalyzing the formation of two glucuronides of the catecholic entacapone. entacapone 107-117 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 9-12 11038168-9 2000 The kinetic data illustrates that UGT1A9 exhibited a much greater rate of glucuronidation and a far lower K(m) value for both entacapone and tolcapone than UGT2B15 and UGT2B7 whose contribution is minor by comparison. entacapone 126-136 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 34-40 11038168-10 2000 Entacapone showed a 3 to 4 times higher V(max) value and a 4 to 6 times lower K(m) value compared with those of tolcapone both in UGT1A9 cell lysates and in human liver microsomes. entacapone 0-10 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 130-136 11065170-6 2000 The measurement of enzyme activities and kinetic parameters using p-nitrophenol and nitrocatechol (entacapone) as substrates for UGT1A6 and UGT1A9, respectively, showed that the overall kinetic properties of the enzymes produced by the two systems were similar. entacapone 99-109 UDP glucuronosyltransferase family 1 member A6 Homo sapiens 129-135 11065170-6 2000 The measurement of enzyme activities and kinetic parameters using p-nitrophenol and nitrocatechol (entacapone) as substrates for UGT1A6 and UGT1A9, respectively, showed that the overall kinetic properties of the enzymes produced by the two systems were similar. entacapone 99-109 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 140-146 10900396-1 2000 Both the catechol-O-methyltransferase (COMT) inhibitor entacapone and the monoamine oxidase B (MAO-B) inhibitor selegiline are L-dopa extenders. entacapone 55-65 catechol-O-methyltransferase Homo sapiens 9-37 10900396-1 2000 Both the catechol-O-methyltransferase (COMT) inhibitor entacapone and the monoamine oxidase B (MAO-B) inhibitor selegiline are L-dopa extenders. entacapone 55-65 catechol-O-methyltransferase Homo sapiens 39-43 10900396-6 2000 or both entacapone and selegiline with the L-dopa/DDC inhibitor medication. entacapone 8-18 dopa decarboxylase Homo sapiens 50-53 10900396-15 2000 Our results suggest that co-administration of entacapone with L-dopa/DDC inhibitor, with or without selegiline, improves clinical disability, is safe, but may also enhance dopamine-related adverse events to some extent in PD patients with end-of-dose type motor fluctuations. entacapone 46-56 dopa decarboxylase Homo sapiens 69-72 10981253-1 2000 OBJECTIVE: To introduce entacapone, a new catechol-O-methyltransferase inhibitor, and discuss its pharmacology, pharmacodynamics, pharmacokinetics, clinical efficacy, drug interactions, adverse events, dosage guidelines, and therapeutic and formulary considerations. entacapone 24-34 catechol-O-methyltransferase Homo sapiens 42-70 10981253-6 2000 DATA SYNTHESIS: Entacapone is the second medication of a new class of drugs, the catechol-O-methyltransferase inhibitors, indicated for clinical use as an adjunct to levodopa/carbidopa to treat patients with idiopathic Parkinson"s disease who experience the signs and symptoms of end-of-dose wearing-off. entacapone 16-26 catechol-O-methyltransferase Homo sapiens 81-109 10882160-2 2000 Entacapone and tolcapone are new potent, selective and reversible nitrocatechol-type COMT inhibitors. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 85-89 10882160-4 2000 In human volunteers, both entacapone and tolcapone dose-dependently inhibit the COMT activity in erythrocytes, improve the bioavailability and decrease the elimination of levodopa, and inhibit the formation of 3-O-methyldopa (3-OMD). entacapone 26-36 catechol-O-methyltransferase Homo sapiens 80-84 10766888-0 2000 The catechol-O-methyltransferase (COMT) inhibitor entacapone enhances the pharmacokinetic and clinical response to Sinemet CR in Parkinson"s disease. entacapone 50-60 catechol-O-methyltransferase Homo sapiens 4-32 10766888-0 2000 The catechol-O-methyltransferase (COMT) inhibitor entacapone enhances the pharmacokinetic and clinical response to Sinemet CR in Parkinson"s disease. entacapone 50-60 catechol-O-methyltransferase Homo sapiens 34-38 10766888-1 2000 OBJECTIVES: Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor. entacapone 12-22 catechol-O-methyltransferase Homo sapiens 66-94 10766888-1 2000 OBJECTIVES: Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor. entacapone 12-22 catechol-O-methyltransferase Homo sapiens 96-100 10858804-2 2000 This consensus statement provides guidelines for the optimal use of the only currently available COMT inhibitor, entacapone (Comtess, Orion Pharma (UK) Ltd, Newbury, Berkshire). entacapone 113-123 catechol-O-methyltransferase Homo sapiens 97-101 11147507-4 2000 Two COMT inhibitors, tolcapone and entacapone, have recently been introduced as adjuncts to levodopa to further inhibit peripheral levodopa metabolism and thereby enhance brain levodopa availability. entacapone 35-45 catechol-O-methyltransferase Homo sapiens 4-8 10733264-15 2000 Entacapone, a purely peripheral COMT inhibitor with a lower potency than tolcapone, has also proved to be effective and has not been associated with liver damage, obviating the need for testing. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 32-36 11147510-1 2000 This paper reviews the issue of hepatotoxicity with the use of the catechol-O-methly transferase (COMT) inhibitors tolcapone and entacapone. entacapone 129-139 catechol-O-methyltransferase Homo sapiens 98-102 11147511-1 2000 Two inhibitors of catechol-O-methyl transferase (COMT), tolcapone and entacapone, have recently been introduced as adjuncts to levodopa in the treatment of Parkinson"s disease patients. entacapone 70-80 catechol-O-methyltransferase Homo sapiens 18-47 11147511-1 2000 Two inhibitors of catechol-O-methyl transferase (COMT), tolcapone and entacapone, have recently been introduced as adjuncts to levodopa in the treatment of Parkinson"s disease patients. entacapone 70-80 catechol-O-methyltransferase Homo sapiens 49-53 11147512-2 2000 Two COMT inhibitors, tolcapone and entacapone, have recently been made available as adjunctive agents to levodopa. entacapone 35-45 catechol-O-methyltransferase Homo sapiens 4-8 11503812-2 1999 (1) Entacapone, a catechol-O-methyltransferase inhibitor, is indicated, in combination with levodopa + a dopadecarboxylase inhibitor, for the treatment of parkinsonian patients who have motor fluctuations on levodopa therapy. entacapone 4-14 catechol-O-methyltransferase Homo sapiens 18-46 11147508-2 2000 This paper examines the pharmacology of COMT inhibitors such as tolcapone and entacapone, and considers the effects of these drugs on the pharmacolinetics of levodopa. entacapone 78-88 catechol-O-methyltransferase Homo sapiens 40-44 11147509-1 2000 Recent prospective, double-blind, placebo-controlled trials have examined the long-term effects of the catechol-O-methyl transferase (COMT) inhibitors entacapone and tolcapone as adjuncts to levodopa in PD patients with wearing-off motor fluctuations. entacapone 151-161 catechol-O-methyltransferase Homo sapiens 103-132 11147509-1 2000 Recent prospective, double-blind, placebo-controlled trials have examined the long-term effects of the catechol-O-methyl transferase (COMT) inhibitors entacapone and tolcapone as adjuncts to levodopa in PD patients with wearing-off motor fluctuations. entacapone 151-161 catechol-O-methyltransferase Homo sapiens 134-138 10555945-4 1999 Entacapone and tolcapone are two potent, selective, and reversible COMT inhibitors that effectively augment levodopa"s pharmacokinetics by increasing area under the plasma concentration versus time curve and plasma elimination half-life without significantly affecting peak levodopa concentrations. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 67-71 10570622-2 1999 Entacapone (Comtan) is a potent, peripherally acting, reversible and selective inhibitor of catechol-O-methyltransferase (COMT). entacapone 0-10 catechol-O-methyltransferase Homo sapiens 92-120 12973467-2 1999 Entacapone is a potent, selective peripheral catechol O-methyltransferase inhibitor which effectively inhibits the O-methylation of levodopa, thus increasing its central bioavailability and potentiating its behavioral effects. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 45-73 10451758-1 1999 The COMT inhibitors, tolcapone and entacapone, are a new class of Parkinson"s medications. entacapone 35-45 catechol-O-methyltransferase Homo sapiens 4-8 10492060-1 1999 OBJECTIVE: Entacapone is a peripherally acting catechol O-methyltransferase (COMT) inhibitor used as an adjunct to each daily levodopa/dopa decarboxylase (DDC) inhibitor dose in the treatment of Parkinson"s disease. entacapone 11-21 catechol-O-methyltransferase Homo sapiens 47-75 10492060-1 1999 OBJECTIVE: Entacapone is a peripherally acting catechol O-methyltransferase (COMT) inhibitor used as an adjunct to each daily levodopa/dopa decarboxylase (DDC) inhibitor dose in the treatment of Parkinson"s disease. entacapone 11-21 catechol-O-methyltransferase Homo sapiens 77-81 10492060-1 1999 OBJECTIVE: Entacapone is a peripherally acting catechol O-methyltransferase (COMT) inhibitor used as an adjunct to each daily levodopa/dopa decarboxylase (DDC) inhibitor dose in the treatment of Parkinson"s disease. entacapone 11-21 dopa decarboxylase Homo sapiens 135-153 10492060-13 1999 Entacapone reduced erythrocyte COMT activity after the first dose, and this effect was quite stable during frequent dosing. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 31-35 10570622-2 1999 Entacapone (Comtan) is a potent, peripherally acting, reversible and selective inhibitor of catechol-O-methyltransferase (COMT). entacapone 0-10 catechol-O-methyltransferase Homo sapiens 122-126 10570622-2 1999 Entacapone (Comtan) is a potent, peripherally acting, reversible and selective inhibitor of catechol-O-methyltransferase (COMT). entacapone 12-18 catechol-O-methyltransferase Homo sapiens 92-120 10570622-2 1999 Entacapone (Comtan) is a potent, peripherally acting, reversible and selective inhibitor of catechol-O-methyltransferase (COMT). entacapone 12-18 catechol-O-methyltransferase Homo sapiens 122-126 10439935-2 1999 UNLABELLED: Entacapone is a potent and specific peripheral catechol-O-methyltransferase (COMT) inhibitor. entacapone 12-22 catechol-O-methyltransferase Homo sapiens 59-87 10439935-2 1999 UNLABELLED: Entacapone is a potent and specific peripheral catechol-O-methyltransferase (COMT) inhibitor. entacapone 12-22 catechol-O-methyltransferase Homo sapiens 89-93 10439935-5 1999 In 2 well conducted trials of 6 months" duration and smaller short term studies, treatment with entacapone (200 mg with each dose of levodopa/AADC inhibitor) was associated with significant increases in daily "on" time and decreases in "off" time. entacapone 96-106 dopa decarboxylase Homo sapiens 142-146 10439935-7 1999 Entacapone also provided benefits when given with controlled release levodopa/ AADC inhibitor or with standard levodopa/AADC inhibitor and selegiline in small trials. entacapone 0-10 dopa decarboxylase Homo sapiens 79-83 10439935-7 1999 Entacapone also provided benefits when given with controlled release levodopa/ AADC inhibitor or with standard levodopa/AADC inhibitor and selegiline in small trials. entacapone 0-10 dopa decarboxylase Homo sapiens 120-124 10439935-11 1999 CONCLUSIONS: The efficacy and tolerability of entacapone administered with levodopa/AADC inhibitor have not yet been compared with those of other strategies for the treatment of Parkinson"s disease. entacapone 46-56 dopa decarboxylase Homo sapiens 84-88 10363328-1 1999 Entacapone (Comtan) is a potent, selective inhibitor of peripheral catechol-O-methyltransferase (COMT) with therapeutic potential as an adjuvant to levodopa therapy in patients with Parkinson"s disease. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 67-95 10363328-1 1999 Entacapone (Comtan) is a potent, selective inhibitor of peripheral catechol-O-methyltransferase (COMT) with therapeutic potential as an adjuvant to levodopa therapy in patients with Parkinson"s disease. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 97-101 10363328-1 1999 Entacapone (Comtan) is a potent, selective inhibitor of peripheral catechol-O-methyltransferase (COMT) with therapeutic potential as an adjuvant to levodopa therapy in patients with Parkinson"s disease. entacapone 12-18 catechol-O-methyltransferase Homo sapiens 67-95 10363328-1 1999 Entacapone (Comtan) is a potent, selective inhibitor of peripheral catechol-O-methyltransferase (COMT) with therapeutic potential as an adjuvant to levodopa therapy in patients with Parkinson"s disease. entacapone 12-18 catechol-O-methyltransferase Homo sapiens 97-101 9808337-1 1998 A new approach in the treatment of Parkinson"s disease is the inhibition of catechol-O-methyltransferase (COMT) with new generation COMT inhibitors, entacapone and tolcapone. entacapone 149-159 catechol-O-methyltransferase Homo sapiens 76-104 15992091-0 1999 Entacapone, a catechol-O-methyltransferase inhibitor for treating Parkinson"s disease: review and current status. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 14-42 15992091-3 1999 Entacapone (Comtan) is a selective, reversible catechol-O-methyltransferase inhibitor that dose-dependently increases the peripheral bioavailability of levodopa and prolongs its duration of action. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 47-75 15992091-3 1999 Entacapone (Comtan) is a selective, reversible catechol-O-methyltransferase inhibitor that dose-dependently increases the peripheral bioavailability of levodopa and prolongs its duration of action. entacapone 12-18 catechol-O-methyltransferase Homo sapiens 47-75 10220913-2 1999 Entacapone is a novel drug which, as a potent inhibitor of catechol-O-methyltransferase (COMT), is used as an adjunct in the standard therapy of Parkinson"s disease. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 59-87 10220913-2 1999 Entacapone is a novel drug which, as a potent inhibitor of catechol-O-methyltransferase (COMT), is used as an adjunct in the standard therapy of Parkinson"s disease. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 89-93 10229966-0 1999 [Entacapone++ : a new catechol-O-methyltransferase inhibitor which improves the response to levodopa in patients with Parkinson disease and fluctuating motor function]. entacapone 1-11 catechol-O-methyltransferase Homo sapiens 22-50 10027643-2 1999 Entacapone is a novel, potent inhibitor of catechol-O-methyltransferase (COMT) intended for use as an adjunct in the treatment of Parkinson"s disease. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 43-71 10027643-2 1999 Entacapone is a novel, potent inhibitor of catechol-O-methyltransferase (COMT) intended for use as an adjunct in the treatment of Parkinson"s disease. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 73-77 10410761-0 1999 COMT inhibition with entacapone in the treatment of Parkinson"s disease. entacapone 21-31 catechol-O-methyltransferase Homo sapiens 0-4 9808337-1 1998 A new approach in the treatment of Parkinson"s disease is the inhibition of catechol-O-methyltransferase (COMT) with new generation COMT inhibitors, entacapone and tolcapone. entacapone 149-159 catechol-O-methyltransferase Homo sapiens 106-110 9808337-9 1998 Based on the duration of COMT inhibition entacapone is administered with each levodopa/DDC inhibitor dose whereas tolcapone is given three times daily. entacapone 41-51 catechol-O-methyltransferase Homo sapiens 25-29 9818851-3 1998 BACKGROUND: Entacapone is a catechol-O-methyltransferase (COMT) inhibitor that has been shown to increase the area under the concentration-time curve of plasma levodopa by decreasing its systemic elimination, thereby promoting and improving therapeutic response to it. entacapone 12-22 catechol-O-methyltransferase Homo sapiens 28-56 9818851-3 1998 BACKGROUND: Entacapone is a catechol-O-methyltransferase (COMT) inhibitor that has been shown to increase the area under the concentration-time curve of plasma levodopa by decreasing its systemic elimination, thereby promoting and improving therapeutic response to it. entacapone 12-22 catechol-O-methyltransferase Homo sapiens 58-62 9633684-4 1998 The new nitrocatechol-type COMT inhibitors entacapone, nitecapone, and tolcapone inhibit COMT in the periphery; tolcapone also inhibits COMT activity centrally. entacapone 43-53 catechol-O-methyltransferase Homo sapiens 27-31 9633684-4 1998 The new nitrocatechol-type COMT inhibitors entacapone, nitecapone, and tolcapone inhibit COMT in the periphery; tolcapone also inhibits COMT activity centrally. entacapone 43-53 catechol-O-methyltransferase Homo sapiens 89-93 9633684-4 1998 The new nitrocatechol-type COMT inhibitors entacapone, nitecapone, and tolcapone inhibit COMT in the periphery; tolcapone also inhibits COMT activity centrally. entacapone 43-53 catechol-O-methyltransferase Homo sapiens 89-93 9358559-8 1997 The kinetic parameters for COMT inhibitors were in the following order: K(m) nitecapone > > entacapone > tolcapone; Vmax nitecapone > entacapone > tolcapone; Vmax/K(m) tolcapone > nitecapone > entacapone. entacapone 98-108 catechol-O-methyltransferase Rattus norvegicus 27-31 9681662-0 1998 Catechol-O-methyltransferase: variation in enzyme activity and inhibition by entacapone and tolcapone. entacapone 77-87 catechol-O-methyltransferase Homo sapiens 0-28 9681662-1 1998 OBJECTIVE: The aim of this investigation was to study the variation of catechol-O-methyltransferase (COMT) activity in the human liver, duodenal mucosa and renal cortex, and to investigate the inhibition of COMT by entacapone and tolcapone. entacapone 215-225 catechol-O-methyltransferase Homo sapiens 101-105 9681662-1 1998 OBJECTIVE: The aim of this investigation was to study the variation of catechol-O-methyltransferase (COMT) activity in the human liver, duodenal mucosa and renal cortex, and to investigate the inhibition of COMT by entacapone and tolcapone. entacapone 215-225 catechol-O-methyltransferase Homo sapiens 207-211 9681662-7 1998 CONCLUSION: Entacapone and tolcapone were powerful inhibitors of COMT and their IC50 estimates were 151 and 773 nM (P = 0.008), respectively, in the liver; consistent results were obtained with the other tissues. entacapone 12-22 catechol-O-methyltransferase Homo sapiens 65-69 9591516-4 1998 This review focuses on the role of the new catechol O-methyltransferase (COMT) inhibitors tolcapone and entacapone as adjuncts to levodopa therapy. entacapone 104-114 catechol-O-methyltransferase Homo sapiens 43-71 9591516-4 1998 This review focuses on the role of the new catechol O-methyltransferase (COMT) inhibitors tolcapone and entacapone as adjuncts to levodopa therapy. entacapone 104-114 catechol-O-methyltransferase Homo sapiens 73-77 9591519-3 1998 Two basic classes of COMT inhibitors are being studied in patients with PD: those that act exclusively extracerebrally or peripherally (e.g., entacapone) and those that cross the blood-brain barrier (e.g., tolcapone). entacapone 142-152 catechol-O-methyltransferase Homo sapiens 21-25 9610919-0 1998 Conditioned place preference induced by a combination of L-dopa and a COMT inhibitor, entacapone, in rats. entacapone 86-96 catechol-O-methyltransferase Rattus norvegicus 70-74 9610919-1 1998 The interaction of dopamine (DA) precursor L-dopa and catechol-O-methyltransferase (COMT) inhibitor, entacapone, was examined in rats using conditioned place preference (CPP) paradigm to assess reinforcement, and by measuring DA metabolism in the striatum and the limbic forebrain. entacapone 101-111 catechol-O-methyltransferase Rattus norvegicus 54-82 9610919-1 1998 The interaction of dopamine (DA) precursor L-dopa and catechol-O-methyltransferase (COMT) inhibitor, entacapone, was examined in rats using conditioned place preference (CPP) paradigm to assess reinforcement, and by measuring DA metabolism in the striatum and the limbic forebrain. entacapone 101-111 catechol-O-methyltransferase Rattus norvegicus 84-88 9610919-5 1998 Entacapone alone had no effect on limbic or striatal DA concentrations, while it reduced the concentrations of the COMT products 3-methoxytyramine (3-MT), a metabolite reflecting DA release, and homovanillic acid (HVA) in both brain areas. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 115-119 9597116-6 1998 Pretreatment with the selective dopamine DA1-receptor antagonist SCH23390 reduced the entacapone-induced natriuretic response by 69%. entacapone 86-96 RT1 class II, locus Da Rattus norvegicus 41-44 9597116-10 1998 In conclusion, COMT inhibition using entacapone results in a mainly DA1 receptor mediated natriuresis involving inhibition of tubular transport processes, supporting a role for dopamine metabolism in sodium homeostasis. entacapone 37-47 catechol-O-methyltransferase Rattus norvegicus 15-19 9597116-10 1998 In conclusion, COMT inhibition using entacapone results in a mainly DA1 receptor mediated natriuresis involving inhibition of tubular transport processes, supporting a role for dopamine metabolism in sodium homeostasis. entacapone 37-47 RT1 class II, locus Da Rattus norvegicus 68-71 9537825-0 1997 Entacapone, a novel catechol-O-methyltransferase inhibitor for Parkinson"s disease, does not impair mitochondrial energy production. entacapone 0-10 catechol-O-methyltransferase Mus musculus 20-48 9537825-1 1997 Entacapone, a novel mainly peripherally acting catechol-O-methyltransferase inhibitor used in the treatment of Parkinson"s disease, was evaluated for its possible uncoupling activity in cell culture, in rat liver mitochondria, and in isolated guinea-pig heart. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 47-75 9537825-8 1997 These results show that peripherally acting entacapone, unlike the brain-penetrating tolcapone, is a safe catechol-O-methyltransferase inhibitor for the treatment of Parkinson"s disease, since it does not interfere with mitochondrial energy metabolism at pharmacologically effective concentrations. entacapone 44-54 catechol-O-methyltransferase Mus musculus 106-134 9372556-1 1997 The aim was to investigate the effects of inhibition of monoamine oxidase type B (MAO-B) with selegiline alone and the combined inhibition of peripheral catechol-O-methyltransferase (COMT) with entacapone and MAO-B with selegiline on striatal 6-[18F]fluorodopa (FDOPA) accumulation, and whether the effect of entacapone + selegiline on FDOPA uptake differed depending on the severity of the presynaptic dopaminergic dysfunction. entacapone 194-204 catechol-O-methyltransferase Homo sapiens 183-187 9392574-3 1997 Entacapone, a peripherally acting, reversible inhibitor of catechol-O-methyltransferase, slows the elimination of levodopa in humans by reducing the formation of 3-O-methyldopa. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 59-87 9399218-3 1997 Pretreatment with the peripheral COMT inhibitor entacapone (12.5 mg/kg p.o.) entacapone 48-58 catechol O-methyltransferase Callithrix jacchus 33-37 9337447-13 1997 The COMT inhibitors, tolcapone and entacapone, improve the pharmacokinetics of levodopa by preventing its peripheral catabolism and increasing the concentration of brain dopamine; thus, these agents may reduce the incidence of "wearing-off" effects associated with the short half-life of levodopa and the progression of Parkinson"s disease. entacapone 35-45 catechol-O-methyltransferase Homo sapiens 4-8 9337447-17 1997 The COMT inhibitors, entacapone and tolcapone, have also demonstrated efficacy in improving on-time in patients with stable disease. entacapone 21-31 catechol-O-methyltransferase Homo sapiens 4-8 9358559-8 1997 The kinetic parameters for COMT inhibitors were in the following order: K(m) nitecapone > > entacapone > tolcapone; Vmax nitecapone > entacapone > tolcapone; Vmax/K(m) tolcapone > nitecapone > entacapone. entacapone 146-156 catechol-O-methyltransferase Rattus norvegicus 27-31 9358559-8 1997 The kinetic parameters for COMT inhibitors were in the following order: K(m) nitecapone > > entacapone > tolcapone; Vmax nitecapone > entacapone > tolcapone; Vmax/K(m) tolcapone > nitecapone > entacapone. entacapone 146-156 catechol-O-methyltransferase Rattus norvegicus 27-31 8784230-3 1996 Pretreatment with entacapone (OR-611), a peripheral catechol O-methyl-transferase (COMT) inhibitor, greatly reduces the plasma 3OMFD fraction and provides an ideal situation to evaluate the contribution of the plasma 3OMFD fraction in several kinetic models of FDOPA uptake. entacapone 18-28 catechol-O-methyltransferase Homo sapiens 83-87 9232524-0 1997 Iron(III)-chelating properties of the novel catechol O-methyltransferase inhibitor entacapone in aqueous solution. entacapone 83-93 catechol-O-methyltransferase Homo sapiens 44-72 9232524-1 1997 The iron(III) complex formation of entacapone, a novel catechol O-methyltransferase (COMT) inhibitor, has been studied at 25 degrees C in aqueous 0.1 mol/L NaCl solution by using the electromotive force titration method. entacapone 35-45 catechol-O-methyltransferase Homo sapiens 55-83 9232524-1 1997 The iron(III) complex formation of entacapone, a novel catechol O-methyltransferase (COMT) inhibitor, has been studied at 25 degrees C in aqueous 0.1 mol/L NaCl solution by using the electromotive force titration method. entacapone 35-45 catechol-O-methyltransferase Homo sapiens 85-89 9251066-13 1997 Entacapone decreased erythrocyte COMT activity by > 35% (p < 0.001), and platelet MAO-B activity was almost completely inhibited by selegiline (p < 0.001). entacapone 0-10 catechol-O-methyltransferase Homo sapiens 33-37 9105581-1 1997 The effects of new selective catechol-O-methyltransferase (COMT) inhibitors entacapone (mainly peripheral effect) and tolcapone (acting also in the brain) on normal and impaired cognitive functions were studied in aversively motivated inhibitory avoidance using a single-trial passive avoidance paradigm in young adult rats. entacapone 76-86 catechol-O-methyltransferase Rattus norvegicus 59-63 8784230-3 1996 Pretreatment with entacapone (OR-611), a peripheral catechol O-methyl-transferase (COMT) inhibitor, greatly reduces the plasma 3OMFD fraction and provides an ideal situation to evaluate the contribution of the plasma 3OMFD fraction in several kinetic models of FDOPA uptake. entacapone 30-36 catechol-O-methyltransferase Homo sapiens 83-87 8726541-8 1996 Peripheral COMT inhibition with entacapone increased significantly the bioavailability of levodopa and prolonged its antiparkinsonian effect after a single dose and after repeated dosing for 4 weeks. entacapone 32-42 catechol-O-methyltransferase Homo sapiens 11-15 24283686-1 1995 We investigated clinical response and pharmacokinetics of levodopa when entacapone, a catechol O-methyltransferase (COMT) inhibitor, was administered concomitantly with either a standard (Std) or a controlled-release (CR) levodopa/carbidopa preparation to 12 patients with Parkinson"s disease. entacapone 72-82 catechol-O-methyltransferase Homo sapiens 116-120 8612391-2 1996 BACKGROUND: Entacapone, a COMT inhibitor, is studied as an adjunct to levodopa treatment in patients with Parkinson"s disease. entacapone 12-22 catechol-O-methyltransferase Homo sapiens 26-30 8612391-5 1996 It was therefore considered to be important to investigate the tolerability of combined COMT and MAO-A inhibition with entacapone and moclobemide. entacapone 119-129 catechol-O-methyltransferase Homo sapiens 88-92 8738181-9 1996 For both normal volunteers and patients having Parkinson"s disease, a single 400 mg dose of entacapone, a peripherally acting COMT inhibitor, decreased the erythrocyte COMT activity. entacapone 92-102 catechol-O-methyltransferase Homo sapiens 126-130 8738181-9 1996 For both normal volunteers and patients having Parkinson"s disease, a single 400 mg dose of entacapone, a peripherally acting COMT inhibitor, decreased the erythrocyte COMT activity. entacapone 92-102 catechol-O-methyltransferase Homo sapiens 168-172 9010698-1 1996 OBJECTIVE: We have evaluated the effects of simultaneous inhibition of catechol-O-methyltransferase (COMT) by entacapone and of neuronal monoamine reuptake by imipramine on haemodynamics and catecholamine metabolism, and the safety and tolerability of the drug combination in healthy women. entacapone 110-120 catechol-O-methyltransferase Homo sapiens 71-99 9010698-1 1996 OBJECTIVE: We have evaluated the effects of simultaneous inhibition of catechol-O-methyltransferase (COMT) by entacapone and of neuronal monoamine reuptake by imipramine on haemodynamics and catecholamine metabolism, and the safety and tolerability of the drug combination in healthy women. entacapone 110-120 catechol-O-methyltransferase Homo sapiens 101-105 8836934-0 1996 COMT inhibition by entacapone does not affect growth hormone or prolactin secretion in healthy volunteers. entacapone 19-29 catechol-O-methyltransferase Homo sapiens 0-4 8836934-1 1996 We studied the effects of entacapone, a novel inhibitor of the enzyme catechol-O-methyltransferase (COMT), on spontaneous and levodopa (LD) modulated secretion of growth hormone (GH) and prolactin (PRL) in 12 healthy male volunteers. entacapone 26-36 catechol-O-methyltransferase Homo sapiens 100-104 8836934-5 1996 Entacapone had no effect on resting levels of GH, but PRL concentrations in plasma were slightly lower after entacapone than after placebo. entacapone 109-119 prolactin Homo sapiens 54-57 8836934-8 1996 Compared with the administration of LD/carbidopa together with placebo, concomitant administration of entacapone increased the AUC of LD by 29% and reduced the AUC of 3-O-methyldopa (a metabolite of LD produced by COMT) by 69%. entacapone 102-112 catechol-O-methyltransferase Homo sapiens 214-218 8558148-1 1996 OBJECTIVES: To establish, in a double blind manner, the antiparkinsonian effects of repeated dosing with entacapone, a peripheral COMT inhibitor. entacapone 105-115 catechol-O-methyltransferase Homo sapiens 130-134 24283686-1 1995 We investigated clinical response and pharmacokinetics of levodopa when entacapone, a catechol O-methyltransferase (COMT) inhibitor, was administered concomitantly with either a standard (Std) or a controlled-release (CR) levodopa/carbidopa preparation to 12 patients with Parkinson"s disease. entacapone 72-82 catechol-O-methyltransferase Homo sapiens 86-114 24283686-21 1995 The study shows that entacapone is an effective COMT inhibitor when combined with either Std levodopa or CR levodopa. entacapone 21-31 catechol-O-methyltransferase Homo sapiens 48-52 7874370-0 1994 COMT inhibition by high-dose entacapone does not affect hemodynamics but changes catecholamine metabolism in healthy volunteers at rest and during exercise. entacapone 29-39 catechol-O-methyltransferase Homo sapiens 0-4 7648772-1 1995 BACKGROUND: Entacapone is a potent, selective catechol-O-methyltransferase (COMT) inhibitor. entacapone 12-22 catechol-O-methyltransferase Homo sapiens 46-74 7648772-1 1995 BACKGROUND: Entacapone is a potent, selective catechol-O-methyltransferase (COMT) inhibitor. entacapone 12-22 catechol-O-methyltransferase Homo sapiens 76-80 7648772-2 1995 Entacapone could potentiate the hemodynamic effects of exogenously administered catecholamines, which are substrates of the COMT enzyme. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 124-128 8665534-0 1995 Effect of entacapone, a COMT inhibitor, on the pharmacokinetics and metabolism of levodopa after administration of controlled-release levodopa-carbidopa in volunteers. entacapone 10-20 catechol-O-methyltransferase Homo sapiens 24-28 8665534-1 1995 We studied the effect of entacapone, a catechol-O-methyltransferase (COMT) inhibitor, on the pharmacokinetics and metabolism of levodopa after administration of a controlled-release (CR) levodopa-carbidopa preparation (Sinemet CR) in an open, randomized trial in 12 healthy male volunteers. entacapone 25-35 catechol-O-methyltransferase Homo sapiens 69-73 8665534-5 1995 Entacapone decreased dose-dependently the activity of S-COMT in RBCs with a maximal inhibition of 66% after the highest dose (800 mg). entacapone 0-10 catechol-O-methyltransferase Homo sapiens 56-60 8665534-12 1995 Entacapone is an effective COMT inhibitor. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 27-31 9620057-0 1995 Striatal [18F]fluorodopa utilization after COMT inhibition with entacapone studied with PET in advanced Parkinson"s disease. entacapone 64-74 catechol-O-methyltransferase Homo sapiens 43-47 7874370-11 1994 COMT inhibition by entacapone seems not to affect hemodynamics or plasma concentrations of unconjugated adrenaline and noradrenaline in healthy volunteers either at rest or during exercise. entacapone 19-29 catechol-O-methyltransferase Homo sapiens 0-4 8001593-0 1994 Metabolite profiles of two [14C]-labelled catechol O-methyltransferase inhibitors, nitecapone and entacapone, in rat and mouse urine and rat bile. entacapone 98-108 catechol-O-methyltransferase Rattus norvegicus 42-70 7835624-4 1994 Entacapone, nitecapone and tolcapone are nitrocatechol-type potent COMT inhibitors in vitro (Ki in nanomolar range). entacapone 0-10 catechol-O-methyltransferase Homo sapiens 67-71 7835624-12 1994 In man, entacapone, nitecapone and tolcapone all inhibit dose dependently the COMT activity in erythrocytes. entacapone 8-18 catechol-O-methyltransferase Homo sapiens 78-82 8035933-1 1994 We used PET and [18F]-6-L-fluorodopa ([18F]dopa) to measure the effect of a peripheral COMT inhibitor, entacapone, on the extracerebral metabolism and subsequent striatal uptake of [18F]dopa. entacapone 103-113 catechol-O-methyltransferase Homo sapiens 87-91 8082707-2 1994 We studied the effects of entacapone, a peripheral catechol-O-methyl transferase inhibitor, on striatal [18F]fluoro-DOPA uptake in rats. entacapone 26-36 catechol-O-methyltransferase Rattus norvegicus 51-80 7518301-7 1994 In the presence of L-dopa/carbidopa, a peripherally active inhibitor of catechol O-methyltransferase (COMT) entacapone had a short-lasting increasing effect on L-dopa efflux. entacapone 108-118 catechol-O-methyltransferase Rattus norvegicus 72-100 7518301-7 1994 In the presence of L-dopa/carbidopa, a peripherally active inhibitor of catechol O-methyltransferase (COMT) entacapone had a short-lasting increasing effect on L-dopa efflux. entacapone 108-118 catechol-O-methyltransferase Rattus norvegicus 102-106 7518301-17 1994 Our results demonstrate that entacapone is a peripheral COMT inhibitor and support the view that CGP 18014 is mainly a centrally acting inhibitor of O-methylation. entacapone 29-39 catechol-O-methyltransferase Rattus norvegicus 56-60 8190296-9 1994 We conclude that inhibition of COMT by entacapone increases the plasma half-life of levodopa and augments the antiparkinsonian effects of single and repeated doses of levodopa. entacapone 39-49 catechol-O-methyltransferase Homo sapiens 31-35 27520516-2 1994 Entacapone, nitecapone and to1capone are nitrocatechol- type agents that are potent COMT inhibitors in vitro and are active in vivo after oral administration. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 84-88 27520516-5 1994 In human volunteers, entacapone, nitecapone and tolcapone inhibit dose-dependently COMT activity of erythrocytes. entacapone 21-31 catechol-O-methyltransferase Homo sapiens 83-87 27520516-6 1994 COMT inhibitors also decrease the levels of COMT-dependent metabolites of adrenaline (epinephrine) and noradrenaline (norepinephrine) in plasma.Entacapone, to1capone and CGP 28014 improve the bioavailability of levodopa and inhibit the formation of 3-0-methyldopa in human volunteers. entacapone 144-154 catechol-O-methyltransferase Homo sapiens 0-4 27520516-6 1994 COMT inhibitors also decrease the levels of COMT-dependent metabolites of adrenaline (epinephrine) and noradrenaline (norepinephrine) in plasma.Entacapone, to1capone and CGP 28014 improve the bioavailability of levodopa and inhibit the formation of 3-0-methyldopa in human volunteers. entacapone 144-154 catechol-O-methyltransferase Homo sapiens 44-48 8020535-0 1993 Identification of major urinary metabolites of the catechol-O-methyltransferase inhibitor entacapone in the dog. entacapone 90-100 catechol-O-methyltransferase Canis lupus familiaris 51-79 8126502-0 1994 Effect of entacapone, a peripherally acting catechol-O-methyltransferase inhibitor, on the motor response to acute treatment with levodopa in patients with Parkinson"s disease. entacapone 10-20 catechol-O-methyltransferase Homo sapiens 44-72 8039535-0 1994 Inhibition of soluble catechol-O-methyltransferase and single-dose pharmacokinetics after oral and intravenous administration of entacapone. entacapone 129-139 catechol-O-methyltransferase Homo sapiens 22-50 8039535-1 1994 The inhibition of soluble catechol-O-methyl-transferase (S-COMT) in red blood cells (RBCs) by entacapone, and the pharmacokinetics of entacapone after single oral (5-800 mg) and i.v. entacapone 94-104 catechol-O-methyltransferase Homo sapiens 59-63 8039535-3 1994 Oral entacapone dose-dependently decreased the activity of S-COMT in RBCs with a maximum inhibition of 82% after the highest dose (800 mg). entacapone 5-15 catechol-O-methyltransferase Homo sapiens 61-65 8039535-4 1994 The inhibition of S-COMT in RBCs was reversible and the activity recovered within 4-8 h. Entacapone showed linear pharmacokinetics over the dose range studied: Cmax and AUC were correlated with the dose of the drug. entacapone 89-99 catechol-O-methyltransferase Homo sapiens 20-24 8039535-10 1994 The results show that entacapone is an orally effective and reversible COMT inhibitor in man and has simple, linear pharmacokinetics. entacapone 22-32 catechol-O-methyltransferase Homo sapiens 71-75 8290096-0 1994 Effect of entacapone, a COMT inhibitor, on clinical disability and levodopa metabolism in parkinsonian patients. entacapone 10-20 catechol-O-methyltransferase Homo sapiens 24-28 12959293-0 1993 The effects of the COMT inhibitor entacapone on haemodynamics and peripheral catecholamine metabolism during exercise. entacapone 34-44 catechol-O-methyltransferase Homo sapiens 19-23 12959293-4 1993 The purpose of the present study was to establish whether the novel COMT inhibitor, entacapone, changes haemodynamic responses and catecholamine metabolism during exercise. entacapone 84-94 catechol-O-methyltransferase Homo sapiens 68-72 8020535-1 1993 Metabolites of entacapone, (E)-2-cyano-N,N-diethyl-3-(3,4-dihydroxy-5-nitrophenyl) propenamide, a potent inhibitor of catechol-O-methyltransferase, were isolated from dog urine. entacapone 15-25 catechol-O-methyltransferase Canis lupus familiaris 118-146 8477410-0 1993 The effect of catechol-O-methyl transferase inhibition by entacapone on the pharmacokinetics and metabolism of levodopa in healthy volunteers. entacapone 58-68 catechol-O-methyltransferase Homo sapiens 14-43 8341294-0 1993 Administration of the new COMT inhibitor OR-611 increases striatal uptake of fluorodopa. entacapone 41-47 catechol-O-methyltransferase Homo sapiens 26-30 8341294-3 1993 We studied the effect of OR-611, a new COMT inhibitor, on plasma and brain 6-[18F]-fluoro-L-dopa (6FD) metabolism in cynomolgus monkeys with positron emission tomography (PET). entacapone 25-31 catechol O-methyltransferase Macaca fascicularis 39-43 8477410-1 1993 We studied the effect of inhibiting the enzyme catechol-O-methyltransferase (COMT) by a novel COMT inhibitor, entacapone, on the pharmacokinetics and metabolism of levodopa in 12 healthy male volunteers. entacapone 110-120 catechol-O-methyltransferase Homo sapiens 47-75 8477410-1 1993 We studied the effect of inhibiting the enzyme catechol-O-methyltransferase (COMT) by a novel COMT inhibitor, entacapone, on the pharmacokinetics and metabolism of levodopa in 12 healthy male volunteers. entacapone 110-120 catechol-O-methyltransferase Homo sapiens 77-81 8477410-1 1993 We studied the effect of inhibiting the enzyme catechol-O-methyltransferase (COMT) by a novel COMT inhibitor, entacapone, on the pharmacokinetics and metabolism of levodopa in 12 healthy male volunteers. entacapone 110-120 catechol-O-methyltransferase Homo sapiens 94-98 8477410-11 1993 The in vivo biochemical effects of entacapone indicate that it is an orally active COMT inhibitor and that it may improve the therapeutic efficacy of levodopa in Parkinson"s disease. entacapone 35-45 catechol-O-methyltransferase Homo sapiens 83-87 1628144-12 1992 OR-611 was primarily a peripherally acting COMT inhibitor, decreasing 3-OMD levels in the striatum (to 31-52%) and in the hypothalamus (to 16-27%) both in the control and pargyline-treated animals at 1 and 3 h. It did not have any effect on brain HVA and 3-MT. entacapone 0-6 catechol-O-methyltransferase Rattus norvegicus 43-47 8095232-0 1993 Identification of major metabolites of the catechol-O-methyltransferase inhibitor entacapone in rats and humans. entacapone 82-92 catechol-O-methyltransferase Rattus norvegicus 43-71 8095232-1 1993 Metabolites of entacapone [(E)-2-cyano-N,N-diethyl-3-(3,4-dihydroxy-5-nitrophenyl)propenamide++ +], a potent inhibitor of catechol-O-methyltransferase, were isolated from human and rat urine. entacapone 15-25 catechol-O-methyltransferase Homo sapiens 122-150 8112370-0 1993 Effect of entacapone, a COMT inhibitor, on the pharmacokinetics of levodopa and on cardiovascular responses in patients with Parkinson"s disease. entacapone 10-20 catechol-O-methyltransferase Homo sapiens 24-28 8112370-1 1993 In an open, randomised, cross-over study we investigated the effect of a single 200 mg oral dose of entacapone, a novel catechol-O-methyltransferase (COMT) inhibitor, on the pharmacokinetics and metabolism of levodopa/carbidopa, and on the cardiovascular responses (blood pressure and pulse rate variation to standard stimuli) in eight parkinsonian patients. entacapone 100-110 catechol-O-methyltransferase Homo sapiens 120-148 8112370-1 1993 In an open, randomised, cross-over study we investigated the effect of a single 200 mg oral dose of entacapone, a novel catechol-O-methyltransferase (COMT) inhibitor, on the pharmacokinetics and metabolism of levodopa/carbidopa, and on the cardiovascular responses (blood pressure and pulse rate variation to standard stimuli) in eight parkinsonian patients. entacapone 100-110 catechol-O-methyltransferase Homo sapiens 150-154 1407012-0 1992 Biochemical and pharmacological properties of a peripherally acting catechol-O-methyltransferase inhibitor entacapone. entacapone 107-117 catechol-O-methyltransferase Rattus norvegicus 68-96 1407012-1 1992 Entacapone, OR-611, was found to be a potent peripherally acting inhibitor of catechol-O-methyltransferase (COMT). entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 78-106 1407012-1 1992 Entacapone, OR-611, was found to be a potent peripherally acting inhibitor of catechol-O-methyltransferase (COMT). entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 108-112 1407012-1 1992 Entacapone, OR-611, was found to be a potent peripherally acting inhibitor of catechol-O-methyltransferase (COMT). entacapone 12-18 catechol-O-methyltransferase Rattus norvegicus 78-106 1407012-1 1992 Entacapone, OR-611, was found to be a potent peripherally acting inhibitor of catechol-O-methyltransferase (COMT). entacapone 12-18 catechol-O-methyltransferase Rattus norvegicus 108-112 1407012-4 1992 Entacapone showed reversible, tight-binding type of inhibition of soluble rat liver COMT with a Ki-value of 14 nmol/l and it also caused 50% inhibition of rat duodenal, erythrocyte, liver and striatal COMT activity 1 h after oral dosing with 1.1, 5.4, 6.7 and 24.2 mg/kg, respectively. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 84-88 1407012-4 1992 Entacapone showed reversible, tight-binding type of inhibition of soluble rat liver COMT with a Ki-value of 14 nmol/l and it also caused 50% inhibition of rat duodenal, erythrocyte, liver and striatal COMT activity 1 h after oral dosing with 1.1, 5.4, 6.7 and 24.2 mg/kg, respectively. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 201-205 1463794-0 1992 Liquid chromatographic determination of a new catechol-O-methyltransferase inhibitor, entacapone, and its Z-isomer in human plasma and urine. entacapone 86-96 catechol-O-methyltransferase Homo sapiens 46-74 1463794-7 1992 The assays were specific with respect to all known metabolites and selective, sensitive and precise enough for determination of entacapone and its Z-isomer in plasma and urine down to 10 ng ml-1. entacapone 128-138 interleukin 17F Homo sapiens 190-194 1875781-7 1991 The specific COMT inhibitors, nitecapone and OR-611, effectively inhibited in vitro the human intestinal COMT activity. entacapone 45-51 catechol-O-methyltransferase Homo sapiens 13-17 1875781-7 1991 The specific COMT inhibitors, nitecapone and OR-611, effectively inhibited in vitro the human intestinal COMT activity. entacapone 45-51 catechol-O-methyltransferase Homo sapiens 105-109 2289048-4 1990 COMT inhibitors nitecapone (OR-462) and OR-611 effectively inhibited human gastrointestinal COMT activity in vitro, the IC50 values ranging from 10-20 nM and 5-75 nM, respectively. entacapone 40-46 catechol-O-methyltransferase Homo sapiens 0-4 2289048-4 1990 COMT inhibitors nitecapone (OR-462) and OR-611 effectively inhibited human gastrointestinal COMT activity in vitro, the IC50 values ranging from 10-20 nM and 5-75 nM, respectively. entacapone 40-46 catechol-O-methyltransferase Homo sapiens 92-96 33269743-1 2021 Entacapone, a catechol-O-methyltransferase inhibitor, can strengthen the therapeutic effects of levodopa on the treatment of Parkinson"s disease. entacapone 0-10 catechol-O-methyltransferase Mus musculus 14-42 34619438-7 2021 In Period-2, the coadministration of entacapone with continuous ND0612 SC infusion translated to an increase in mean levodopa AUC0-10h compared to baseline. entacapone 37-47 period circadian regulator 2 Homo sapiens 3-11 34225162-4 2021 It has been reported that 1-tetralone and 1-indanone derivatives are potent and specific inhibitors of MAO-B, while compounds containing the nitrocatechol moiety (e.g. tolcapone and entacapone) are often potent COMT inhibitors. entacapone 182-192 catechol-O-methyltransferase Homo sapiens 211-215 33269743-5 2021 Immunohistochemical staining results revealed that after entacapone treatment, the numbers of Ki67-positive proliferating cells, doublecortin-positive immature neurons, and phosphorylated cAMP response element-binding protein (pCREB)-positive cells were significantly increased. entacapone 57-67 antigen identified by monoclonal antibody Ki 67 Mus musculus 94-98 33269743-5 2021 Immunohistochemical staining results revealed that after entacapone treatment, the numbers of Ki67-positive proliferating cells, doublecortin-positive immature neurons, and phosphorylated cAMP response element-binding protein (pCREB)-positive cells were significantly increased. entacapone 57-67 doublecortin Mus musculus 129-141 33269743-7 2021 Entacapone treatment antagonized the effects of TrkB receptor antagonist. entacapone 0-10 neurotrophic tyrosine kinase, receptor, type 2 Mus musculus 48-52 35463646-2 2022 However, there have been negative effects reported against entacapone, namely, gastrointestinal (GI) problems and drowsiness. entacapone 59-69 G protein subunit alpha i1 Homo sapiens 97-99 35563817-1 2022 The catechol-O-methyltransferase inhibitors entacapone and opicapone prolong the efficacy of conventional oral levodopa/dopa decarboxylase inhibitor formulations through an increase in levodopa plasma bioavailability. entacapone 44-54 catechol-O-methyltransferase Homo sapiens 4-32 35563817-1 2022 The catechol-O-methyltransferase inhibitors entacapone and opicapone prolong the efficacy of conventional oral levodopa/dopa decarboxylase inhibitor formulations through an increase in levodopa plasma bioavailability. entacapone 44-54 dopa decarboxylase Homo sapiens 120-138 35463646-1 2022 Background and Aims: Entacapone, one of the most common drugs distributed among patients with Parkinson"s disease, is a peripherally acting catechol-O-methyltransferase (COMT) inhibitor that is used in addition to levodopa to control symptoms. entacapone 21-31 catechol-O-methyltransferase Homo sapiens 140-168 35463646-1 2022 Background and Aims: Entacapone, one of the most common drugs distributed among patients with Parkinson"s disease, is a peripherally acting catechol-O-methyltransferase (COMT) inhibitor that is used in addition to levodopa to control symptoms. entacapone 21-31 catechol-O-methyltransferase Homo sapiens 170-174 35044481-3 2022 The available COMT inhibitors, entacapone, opicapone and tolcapone, differ pharmacokinetically in terms of their half-lives with implications for the dose frequency, in their indication requirements and in their spectrum of side effects, including diarrhea and yellow discoloration of urine. entacapone 31-41 catechol-O-methyltransferase Homo sapiens 14-18 34380879-6 2022 Here, we describe a subset of compounds containing a single aromatic ring, like dopamine, ZPDm, gallic acid, or entacapone, which act as molecular chaperones against alpha-synuclein aggregation. entacapone 112-122 synuclein alpha Homo sapiens 166-181 35121825-11 2022 Entacapone, a conventional drug for Parkinson"s disease, was confirmed to suppress OS via m6A-mediated regulation through the FTO/DACT1 axis. entacapone 0-10 FTO alpha-ketoglutarate dependent dioxygenase Homo sapiens 126-129 35121825-11 2022 Entacapone, a conventional drug for Parkinson"s disease, was confirmed to suppress OS via m6A-mediated regulation through the FTO/DACT1 axis. entacapone 0-10 dishevelled binding antagonist of beta catenin 1 Homo sapiens 130-135 2501597-4 1989 The effect of catechol-O-methyltransferase (COMT) inhibitor, OR-611, on the potentiation of L-dopa-induced contralateral rotation in 6-OHDA-lesioned rats was also studied. entacapone 61-67 catechol-O-methyltransferase Rattus norvegicus 14-42 2501597-4 1989 The effect of catechol-O-methyltransferase (COMT) inhibitor, OR-611, on the potentiation of L-dopa-induced contralateral rotation in 6-OHDA-lesioned rats was also studied. entacapone 61-67 catechol-O-methyltransferase Rattus norvegicus 44-48 34017338-5 2021 We herein show that nanoparticle-mediated Fto-siRNA delivery or FTO inhibitor entacapone administration dramatically inhibited macrophage activation, reduced the tissue damage and improved survival in a mouse model of LPS-induced endotoxic shock. entacapone 78-88 fat mass and obesity associated Mus musculus 64-67 33352833-1 2020 Entacapone, a reversible inhibitor of catechol-O-methyl transferase, is used for patients in Parkinson"s disease because it increases the bioavailability and effectiveness of levodopa. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 38-67 33675481-3 2021 Entacapone is a catechol-O-methyl transferase (COMT) inhibitor which elicits antioxidant activity by scavenging peroxynitrite. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 16-45 33675481-3 2021 Entacapone is a catechol-O-methyl transferase (COMT) inhibitor which elicits antioxidant activity by scavenging peroxynitrite. entacapone 0-10 catechol-O-methyltransferase Rattus norvegicus 47-51 33675481-9 2021 In addition, entacapone or FeTPPS significantly inhibited I/R-induced elevation in renal TNF-alpha levels (78% and 58%, respectively) and caspase-3 activity (72% and 56%, respectively) indicating the reduction of both inflammation and apoptosis in the kidney (P < 0.05). entacapone 13-23 tumor necrosis factor Rattus norvegicus 89-98 33675481-9 2021 In addition, entacapone or FeTPPS significantly inhibited I/R-induced elevation in renal TNF-alpha levels (78% and 58%, respectively) and caspase-3 activity (72% and 56%, respectively) indicating the reduction of both inflammation and apoptosis in the kidney (P < 0.05). entacapone 13-23 caspase 3 Rattus norvegicus 138-147 33840171-2 2021 Additionally, several inhibitory drugs such as Entacapone and Opicapone are also cosupplemented to protect peripheral inactivation of exogenous L-DOPA (~80%) that occurs due to metabolic activity of the enzyme catechol-O-methyltransferase (COMT). entacapone 47-57 catechol-O-methyltransferase Homo sapiens 210-238 33840171-2 2021 Additionally, several inhibitory drugs such as Entacapone and Opicapone are also cosupplemented to protect peripheral inactivation of exogenous L-DOPA (~80%) that occurs due to metabolic activity of the enzyme catechol-O-methyltransferase (COMT). entacapone 47-57 catechol-O-methyltransferase Homo sapiens 240-244 33289420-0 2021 Tissue and interspecies comparison of catechol-O-methyltransferase mediated catalysis of 6-O-methylation of esculetin to scopoletin and its inhibition by entacapone and tolcapone. entacapone 154-164 catechol-O-methyltransferase Rattus norvegicus 38-66 33289420-3 2021 Furthermore, we compared the inhibition potencies and mechanisms of two clinically used COMT inhibitors, entacapone and tolcapone, in these species. entacapone 105-115 catechol-O-methyltransferase Rattus norvegicus 88-92 33289420-9 2021 Both entacapone and tolcapone are potent COMT inhibitors, but their inhibition mechanisms differ. entacapone 5-15 catechol-O-methyltransferase Rattus norvegicus 41-45 33136226-2 2021 The effect of entacapone on the pharmacokinetics of L-dopa differs between patients with high-activity (H/H) and low-activity (L/L) catechol-O-methyltransferase (COMT) Val158Met polymorphisms, but the effects are unclear in heterozygous (H/L) patients. entacapone 14-24 catechol-O-methyltransferase Homo sapiens 132-160 33136226-2 2021 The effect of entacapone on the pharmacokinetics of L-dopa differs between patients with high-activity (H/H) and low-activity (L/L) catechol-O-methyltransferase (COMT) Val158Met polymorphisms, but the effects are unclear in heterozygous (H/L) patients. entacapone 14-24 catechol-O-methyltransferase Homo sapiens 162-166 33136226-4 2021 Therefore, the present study aimed to clarify the effect of the COMT Val158Met polymorphism on the concentrations of L-dopa and 3-OMD in the presence of entacapone. entacapone 153-163 catechol-O-methyltransferase Homo sapiens 64-68 33352833-7 2020 In particular, entacapone significantly increased proteins related to synaptic trafficking and plasticity, such as dynamin 1, synapsin I, and Munc18-1. entacapone 15-25 dynamin 1 Homo sapiens 115-124 33352833-7 2020 In particular, entacapone significantly increased proteins related to synaptic trafficking and plasticity, such as dynamin 1, synapsin I, and Munc18-1. entacapone 15-25 synapsin I Homo sapiens 126-136 33352833-7 2020 In particular, entacapone significantly increased proteins related to synaptic trafficking and plasticity, such as dynamin 1, synapsin I, and Munc18-1. entacapone 15-25 syntaxin binding protein 1 Homo sapiens 142-150 32299731-7 2020 This is more potent than the reference COMT inhibitor, entacapone, which has an IC50 value of 0.23 muM. entacapone 55-65 catechol-O-methyltransferase Rattus norvegicus 39-43 33387482-10 2021 Interestingly, treatment with entacapone, which is used for the treatment of Parkinson"s disease and is an inhibitor of FTO, decreased HNF4alpha and UGT2B7 expression. entacapone 30-40 FTO alpha-ketoglutarate dependent dioxygenase Homo sapiens 120-123 33387482-10 2021 Interestingly, treatment with entacapone, which is used for the treatment of Parkinson"s disease and is an inhibitor of FTO, decreased HNF4alpha and UGT2B7 expression. entacapone 30-40 hepatocyte nuclear factor 4 alpha Homo sapiens 135-144 33387482-10 2021 Interestingly, treatment with entacapone, which is used for the treatment of Parkinson"s disease and is an inhibitor of FTO, decreased HNF4alpha and UGT2B7 expression. entacapone 30-40 UDP glucuronosyltransferase family 2 member B7 Homo sapiens 149-155 32750483-0 2020 Investigating the inhibitory effects of entacapone on amyloid fibril formation of human lysozyme. entacapone 40-50 lysozyme Homo sapiens 88-96 32750483-3 2020 In this study, we have investigated the inhibitory effect of entacapone (Ent) on human lysozyme (HL) amyloid fibrillation using a combination of biophysical techniques; Rayleigh scattering (RLS) data indicated that Ent can reduce the aggregation of HL amyloid fibrillation with the inhibition constant (Lambda) of (3.0 +- 0.5) x 103 M-1. entacapone 61-71 lysozyme Homo sapiens 87-95 32030869-10 2020 Additionally, the auxin response factor gene (GhARF3) located in inherited IBD segments from 108F and 611B, was highly correlated with fiber quality. entacapone 102-106 auxin response factor 18-like Gossypium hirsutum 46-52 32289635-5 2020 Second, in vitro assays confirmed the inhibitory effect of entacapone on maize COMT. entacapone 59-69 caffeic acid 3-O-methyltransferase Zea mays 79-83 31109396-10 2019 The known selective COMT inhibitor entacapone was used as test inhibitor. entacapone 35-45 catechol-O-methyltransferase Rattus norvegicus 20-24 31868682-10 2020 CONCLUSIONS: Independent from previous studies and prior assumptions we show that the currently-used LED conversion factors for immediate release levodopa, controlled release levodopa and amantadine are largely correct and that dopamine agonists, MAO-B inhibitors and entacapone, given in addition to levodopa, have little additional clinical value for PD patients with motor fluctuations. entacapone 268-278 small integral membrane protein 10 like 2A Homo sapiens 101-104 31837280-4 2020 Such biotransformation was completely blocked by entacapone, a well-known catechol-O-methyltransferase (COMT) inhibitor, demonstrating that the O-methylation was mediated by COMT. entacapone 49-59 catechol-O-methyltransferase Homo sapiens 74-102 31837280-4 2020 Such biotransformation was completely blocked by entacapone, a well-known catechol-O-methyltransferase (COMT) inhibitor, demonstrating that the O-methylation was mediated by COMT. entacapone 49-59 catechol-O-methyltransferase Homo sapiens 104-108 31837280-4 2020 Such biotransformation was completely blocked by entacapone, a well-known catechol-O-methyltransferase (COMT) inhibitor, demonstrating that the O-methylation was mediated by COMT. entacapone 49-59 catechol-O-methyltransferase Homo sapiens 174-178 31109396-11 2019 The results confirmed the ability of entacapone to inhibit COMT activity by decreasing the production of all the metabolites of norepinephrine. entacapone 37-47 catechol-O-methyltransferase Rattus norvegicus 59-63 30996080-0 2019 Identification of entacapone as a chemical inhibitor of FTO mediating metabolic regulation through FOXO1. entacapone 18-28 fat mass and obesity associated Mus musculus 56-59 30996080-0 2019 Identification of entacapone as a chemical inhibitor of FTO mediating metabolic regulation through FOXO1. entacapone 18-28 forkhead box O1 Mus musculus 99-104 30996080-3 2019 Here, we used a structure-based virtual screening of U.S. Food and Drug Administration-approved drugs to identify entacapone as a potential FTO inhibitor. entacapone 114-124 fat mass and obesity associated Mus musculus 140-143 30996080-4 2019 Using structural and biochemical studies, we showed that entacapone directly bound to FTO and inhibited FTO activity in vitro. entacapone 57-67 fat mass and obesity associated Mus musculus 86-89 30996080-4 2019 Using structural and biochemical studies, we showed that entacapone directly bound to FTO and inhibited FTO activity in vitro. entacapone 57-67 fat mass and obesity associated Mus musculus 104-107 30996080-6 2019 We identified the transcription factor forkhead box protein O1 (FOXO1) mRNA as a direct substrate of FTO, and demonstrated that entacapone elicited its effects on gluconeogenesis in the liver and thermogenesis in adipose tissues in mice by acting on an FTO-FOXO1 regulatory axis. entacapone 128-138 forkhead box O1 Mus musculus 39-62 30996080-6 2019 We identified the transcription factor forkhead box protein O1 (FOXO1) mRNA as a direct substrate of FTO, and demonstrated that entacapone elicited its effects on gluconeogenesis in the liver and thermogenesis in adipose tissues in mice by acting on an FTO-FOXO1 regulatory axis. entacapone 128-138 forkhead box O1 Mus musculus 64-69 30996080-6 2019 We identified the transcription factor forkhead box protein O1 (FOXO1) mRNA as a direct substrate of FTO, and demonstrated that entacapone elicited its effects on gluconeogenesis in the liver and thermogenesis in adipose tissues in mice by acting on an FTO-FOXO1 regulatory axis. entacapone 128-138 fat mass and obesity associated Mus musculus 101-104 30996080-6 2019 We identified the transcription factor forkhead box protein O1 (FOXO1) mRNA as a direct substrate of FTO, and demonstrated that entacapone elicited its effects on gluconeogenesis in the liver and thermogenesis in adipose tissues in mice by acting on an FTO-FOXO1 regulatory axis. entacapone 128-138 fat mass and obesity associated Mus musculus 253-256 30996080-6 2019 We identified the transcription factor forkhead box protein O1 (FOXO1) mRNA as a direct substrate of FTO, and demonstrated that entacapone elicited its effects on gluconeogenesis in the liver and thermogenesis in adipose tissues in mice by acting on an FTO-FOXO1 regulatory axis. entacapone 128-138 forkhead box O1 Mus musculus 257-262 30111624-4 2018 In this study, we expressed recombinant human UGT1A10 in human embryonic kidney (HEK)293 and Chinese hamster ovary (CHO) cells to examine its oligomeric states and characterize its enzymatic activities against two therapeutically interesting substrates, morphine and entacapone, including determination of the catalytic rate constant (kcat) values for the first time. entacapone 267-277 UDP glucuronosyltransferase family 1 member A10 Homo sapiens 46-53 30135178-6 2018 All but two drugs showed substrate affinity to OAT2, whereas four (bromfenac, entacapone, fluorescein, and nateglinide) also showed OATP1B1 activity in transfected cells. entacapone 78-88 solute carrier organic anion transporter family member 1B1 Homo sapiens 132-139 30111624-6 2018 Owing to the formation of the covalently crosslinked higher-order oligomers, the UGT1A10 protein expressed in HEK293 cells had much lower catalytic activity (particularly the catalytic rate constant kcat) against both morphine and entacapone, compared with the UGT1A10 protein form expressed in CHO cells against the same substrates. entacapone 231-241 UDP glucuronosyltransferase family 1 member A10 Homo sapiens 81-88 30070707-5 2018 Entacapone is a clinically used inhibitor of COMT, and has been shown to modulate the methylation of food-derived polyphenols. entacapone 0-10 catechol-O-methyltransferase Homo sapiens 45-49 29688484-1 2018 Tolcapone and entacapone are catechol-O-methyltransferase inhibitors used in patients with Parkinson"s disease. entacapone 14-24 catechol-O-methyltransferase Homo sapiens 29-57 29696585-4 2018 In commercial oral formulations, LD is co-administrated with an AADC inhibitor (carbidopa) and a COMT inhibitor (entacapone) to enhance its bioavailability. entacapone 113-123 catechol-O-methyltransferase Homo sapiens 97-101 29697034-7 2018 The chalcone class of compounds is well known to potently inhibit MAO-B, while nitrocatechol derivatives (e.g. tolcapone and entacapone) are clinically used COMT inhibitors. entacapone 125-135 catechol-O-methyltransferase Homo sapiens 157-161 29614697-6 2018 OBJECTIVE: The primary aim of this study was to investigate the efficacy and safety of the two available COMT inhibitors; entacapone and tolcapone and the recently introduced opicapone. entacapone 122-132 catechol-O-methyltransferase Homo sapiens 105-109 28526448-0 2017 The catechol-O-methyltransferase inhibitors tolcapone and entacapone uncouple and inhibit the mitochondrial respiratory chain in HepaRG cells. entacapone 58-68 catechol-O-methyltransferase Homo sapiens 4-32