PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 30031817-6 2018 Intravenous granisetron (1 or 2 mg/kg) produced the dose-dependent suppression of the ongoing and evoked firing of CRD-excited cells within both the CVLM and NTS in normal conditions as well as was able to substantially reduce excitability of the caudal medullary neurons in the presence of colonic inflammation, arguing for the potential efficacy of the 5-HT3 receptor blockade with granisetron against both acute and inflammatory abdominal pain. Granisetron 12-23 5-hydroxytryptamine receptor 3A Rattus norvegicus 355-369 31832222-11 2019 Conclusions: This study suggests that granisetron alone could be one treatment option in the management of CINV in patients with non-Hodgkin lymphoma receiving CHOP or R-CHOP regimen. Granisetron 38-49 DNA damage inducible transcript 3 Homo sapiens 160-164 31832222-11 2019 Conclusions: This study suggests that granisetron alone could be one treatment option in the management of CINV in patients with non-Hodgkin lymphoma receiving CHOP or R-CHOP regimen. Granisetron 38-49 DNA damage inducible transcript 3 Homo sapiens 170-174 30506577-12 2019 Both treatment with granisetron and genetic knockdown of the 5-HT3A receptor in cells suppressed nuclear factor kappa B (NF-kB) transactivation and phosphorylated p38 (p-p38) accumulation in macrophages. Granisetron 20-31 5-hydroxytryptamine (serotonin) receptor 3A Mus musculus 61-67 30506577-12 2019 Both treatment with granisetron and genetic knockdown of the 5-HT3A receptor in cells suppressed nuclear factor kappa B (NF-kB) transactivation and phosphorylated p38 (p-p38) accumulation in macrophages. Granisetron 20-31 mitogen-activated protein kinase 14 Mus musculus 163-166 30506577-12 2019 Both treatment with granisetron and genetic knockdown of the 5-HT3A receptor in cells suppressed nuclear factor kappa B (NF-kB) transactivation and phosphorylated p38 (p-p38) accumulation in macrophages. Granisetron 20-31 mitogen-activated protein kinase 14 Mus musculus 170-173 30336258-7 2019 The 5-HT3 receptor (5-HT3R) antagonist granisetron evoked a dose-dependent attenuation of both 5-HT- and T-2 toxin-induced anorectic responses. Granisetron 39-50 5-hydroxytryptamine (serotonin) receptor 3A Mus musculus 4-18 30336258-7 2019 The 5-HT3 receptor (5-HT3R) antagonist granisetron evoked a dose-dependent attenuation of both 5-HT- and T-2 toxin-induced anorectic responses. Granisetron 39-50 5-hydroxytryptamine (serotonin) receptor 3A Mus musculus 20-26 30336258-7 2019 The 5-HT3 receptor (5-HT3R) antagonist granisetron evoked a dose-dependent attenuation of both 5-HT- and T-2 toxin-induced anorectic responses. Granisetron 39-50 brachyury 2 Mus musculus 105-108 31832222-0 2019 Granisetron plus aprepitant versus granisetron in preventing nausea and vomiting during CHOP or R-CHOP regimen in malignant lymphoma: a retrospective study. Granisetron 0-11 DNA damage inducible transcript 3 Homo sapiens 88-92 31832222-0 2019 Granisetron plus aprepitant versus granisetron in preventing nausea and vomiting during CHOP or R-CHOP regimen in malignant lymphoma: a retrospective study. Granisetron 0-11 DNA damage inducible transcript 3 Homo sapiens 98-102 31199962-2 2019 Some antiemetic medications (AEM) (droperidol, domperidone, granisetron, metoclopramide and trifluoperazine) used to treat NVP have the unwanted side effect of hERG blockade. Granisetron 60-71 ETS transcription factor ERG Homo sapiens 160-164 30950278-0 2019 Highly Variable Expression of CYP1A1 in Human Liver and Impact on Pharmacokinetics of Riociguat and Granisetron in Humans. Granisetron 100-111 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 30-36 30950278-9 2019 Together with the high selectivity and especially the high metabolic efficiency of CYP1A1 shown for granisetron and riociguat, it is demonstrated that CYP1A1 plays an important role in the metabolic clearance of these drugs and is responsible for the clinically observed interindividual variability in their pharmacokinetics. Granisetron 100-111 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 83-89 30950278-9 2019 Together with the high selectivity and especially the high metabolic efficiency of CYP1A1 shown for granisetron and riociguat, it is demonstrated that CYP1A1 plays an important role in the metabolic clearance of these drugs and is responsible for the clinically observed interindividual variability in their pharmacokinetics. Granisetron 100-111 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 151-157 30797147-1 2019 5-HT3R antagonists such as ondansetron, granisetron and tropisetron have been clinically used to treat nausea and vomiting in chemotherapy patients. Granisetron 40-51 5-hydroxytryptamine receptor 3A Homo sapiens 0-6 30551881-5 2019 Granisetron administration reduced pulmonary neutrophil recruitment after CLP. Granisetron 0-11 hyaluronan and proteoglycan link protein 1 Mus musculus 74-77 30551881-7 2019 Additionally, granisetron could inhibit the activation of p38 MAPK and NLRP3 inflammasome both in vivo and in vitro. Granisetron 14-25 mitogen-activated protein kinase 14 Mus musculus 58-66 30551881-7 2019 Additionally, granisetron could inhibit the activation of p38 MAPK and NLRP3 inflammasome both in vivo and in vitro. Granisetron 14-25 NLR family, pyrin domain containing 3 Mus musculus 71-76 30551881-8 2019 Collectively, granisetron protects against sepsis-induced ALI by suppressing macrophage Cxcl1/Cxcl2 expression and neutrophil recruitment in the lung. Granisetron 14-25 chemokine (C-X-C motif) ligand 1 Mus musculus 88-93 30551881-8 2019 Collectively, granisetron protects against sepsis-induced ALI by suppressing macrophage Cxcl1/Cxcl2 expression and neutrophil recruitment in the lung. Granisetron 14-25 chemokine (C-X-C motif) ligand 2 Mus musculus 94-99 30359082-6 2019 Alosetron (sc) and granisetron (antagonists) caused a paradoxical increase in the VMR to CRD in SERT-KO female rats. Granisetron 19-30 solute carrier family 6 member 4 Rattus norvegicus 96-100 31683487-8 2019 In addition, and supported by proteomics analysis, granisetron significantly reduced Abeta induced calcium influx in vitro, and rectified calcium dyshomeostasis in TgSwDI mice brains by restoring calmodulin-dependent protein kinase II/cAMP-response element binding protein pathway, which was associated with cognitive improvement. Granisetron 51-62 amyloid beta (A4) precursor protein Mus musculus 85-90 27838796-6 2017 Finally, the activity of antioxidant enzymes (SOD, CAT, and GPx) in the liver improved after cHb and cWb treatment under acute and chronic inflammation. Granisetron 101-104 catalase Mus musculus 51-54 29972203-7 2018 The CML-induced serotonin release was reduced by the HTR3 antagonist granisetron. Granisetron 69-80 5-hydroxytryptamine receptor 3A Homo sapiens 53-57 28853174-3 2018 Therefore, the objective of our work was to examine the impact of selective 5-HT3 receptor blockade with granisetron on migraine-related nociceptive transmission within the spinal trigeminal nucleus (STN) and the ventroposteromedial nucleus of the thalamus (VPM). Granisetron 105-116 5-hydroxytryptamine receptor 3A Rattus norvegicus 76-90 29057666-5 2017 Expert opinion: According to current literature, granisetron 2 mg orally or 0,01mg/kg (1 mg) intravenously per day, co-administered with dexamethasone and NK-1 antagonists is the recommended regime for highly emetogenic chemotherapy. Granisetron 49-60 tachykinin receptor 1 Homo sapiens 155-159 27838796-6 2017 Finally, the activity of antioxidant enzymes (SOD, CAT, and GPx) in the liver improved after cHb and cWb treatment under acute and chronic inflammation. Granisetron 101-104 peroxiredoxin 6 pseudogene 2 Mus musculus 60-63 27108935-7 2016 The reverse experiment revealed that granisetron also competitively bound to muscarinic receptors (Ki = 6.5 muM). Granisetron 37-48 latexin Homo sapiens 108-111 27809336-4 2016 Granisetron is primarily metabolized by the cytochrome P450 (CYP) enzymes CYP1A1 and CYP3A and is likely a substrate of the ABCB1 transporter. Granisetron 0-11 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 74-80 27809336-4 2016 Granisetron is primarily metabolized by the cytochrome P450 (CYP) enzymes CYP1A1 and CYP3A and is likely a substrate of the ABCB1 transporter. Granisetron 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 85-90 27809336-4 2016 Granisetron is primarily metabolized by the cytochrome P450 (CYP) enzymes CYP1A1 and CYP3A and is likely a substrate of the ABCB1 transporter. Granisetron 0-11 ATP binding cassette subfamily B member 1 Homo sapiens 124-129 27809336-15 2016 CONCLUSIONS: Polymorphisms in CYP3A5 and CYP1A1 account for some of the variability in systemic clearance and exposure of granisetron in pregnant women. Granisetron 122-133 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 30-36 27809336-15 2016 CONCLUSIONS: Polymorphisms in CYP3A5 and CYP1A1 account for some of the variability in systemic clearance and exposure of granisetron in pregnant women. Granisetron 122-133 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 41-47 27392852-10 2016 Only 3 (etodolac, granisetron, and beclomethasone) out of the 5 effective drugs in the bEnd3-based BBB model demonstrated a promising effect to protect the hCMEC/D3-based BBB model integrity. Granisetron 18-29 BEN domain containing 3 Homo sapiens 87-92 22873819-4 2012 Here we heterologously express mouse 5-HT(3)A receptors in Xenopus oocytes and use unnatural amino acid mutagenesis to establish a cation-pi interaction for both ondansetron and granisetron to tryptophan 183 in the ligand binding pocket. Granisetron 178-189 5-hydroxytryptamine (serotonin) receptor 3A Mus musculus 37-45 25960846-9 2015 Also our study showed that controlled CINV episodes in patients who received CMF regimen were better than the regimen including adriamycin (CAF, CHOP) into both granisetron (p=0.06) and metoclopramid (p=0.04). Granisetron 161-172 DNA damage inducible transcript 3 Homo sapiens 145-149 24813296-6 2014 This effect was abrogated by the 5-HT 3 receptor (5-HT3R) antagonist granisetron, which was luminally delivered to preferentially target vagal terminals. Granisetron 69-80 5-hydroxytryptamine receptor 3A Rattus norvegicus 33-48 24813296-6 2014 This effect was abrogated by the 5-HT 3 receptor (5-HT3R) antagonist granisetron, which was luminally delivered to preferentially target vagal terminals. Granisetron 69-80 5-hydroxytryptamine receptor 3A Rattus norvegicus 50-56 23338487-0 2013 Aprepitant plus granisetron and dexamethasone for prevention of chemotherapy-induced nausea and vomiting in patients with gastric cancer treated with S-1 plus cisplatin. Granisetron 16-27 proteasome 26S subunit, non-ATPase 1 Homo sapiens 150-153 23358260-0 2013 Association of ABCB1 polymorphisms with the antiemetic efficacy of granisetron plus dexamethasone in breast cancer patients. Granisetron 67-78 ATP binding cassette subfamily B member 1 Homo sapiens 15-20 23358260-3 2013 We evaluated the association between the antiemetic efficacy of granisetron plus dexamethasone and ABCB1 polymorphisms 3435C>T and 2677G>T/A. Granisetron 64-75 ATP binding cassette subfamily B member 1 Homo sapiens 99-104 26576669-10 2016 Selective 5-HT3R antagonists (ondansetron, tropisetron and granisetron) showed positive results on negative symptoms and/or cognitive impairments in phase II trials. Granisetron 59-70 5-hydroxytryptamine receptor 3A Homo sapiens 10-16 24718779-8 2014 Further, levels of NK-1R in the cisplatin, thalidomide, and granisetron group were significantly increased at both 5 and 33 h (p < 0.05 vs. control group), with no obvious difference among these three groups. Granisetron 60-71 tachykinin receptor 1 Rattus norvegicus 19-24 24618127-5 2014 This inhibition was blocked by the 5-HT1A antagonist N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinylcyclohexanecarboxamide (WAY-100635), which was ineffective on its own, whereas the excitation was reversed by granisetron. Granisetron 223-234 5-hydroxytryptamine receptor 1A Rattus norvegicus 35-41 22683863-7 2012 We first studied the inhibition of SP-induced Ca(2+) mobilization in NG108-15 cells by palonosetron, ondansetron and granisetron. Granisetron 117-128 tachykinin 1 Mus musculus 35-37 21737202-8 2011 Sumatriptan, ketanserin, and granisetron treatment attenuated calcium accumulation and 5HT enhancement of capsaicin-evoked CGRP release. Granisetron 29-40 calcitonin-related polypeptide alpha Rattus norvegicus 123-127 22209919-7 2012 We report that 5HT pretreatment enhances TRPV1-evoked thermal hyperalgesia, which is attenuated with local pretreatment with ketanserin, granisetron, or sumatriptan. Granisetron 137-148 transient receptor potential cation channel, subfamily V, member 1 Rattus norvegicus 41-46 19902987-23 2009 An alternative is to use a serotonin agent that is metabolized independently of CYP2D6, such as granisetron, which would obviate the need for genotyping and may lead to an improved drug response. Granisetron 96-107 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 80-86 21427712-11 2011 The area under the curve, but not peak sensory afferent discharge evoked by IBS samples in rat jejunum, was significantly inhibited by the 5-HT3 receptor antagonist granisetron (P<0.005). Granisetron 165-176 5-hydroxytryptamine receptor 3A Rattus norvegicus 139-153 20724042-2 2010 With respect to the many other drugs already in use, such as the first generation 5-HT(3)R antagonist granisetron, palonosetron, a second generation antagonist, clearly demonstrates superior inhibition potency towards the 5-HT(3)Rs. Granisetron 102-113 5-hydroxytryptamine receptor 3A Homo sapiens 82-90 20724042-6 2010 The results of docking studies of the natural agonist serotonin and the antagonists palonosetron and granisetron into the modelled homomeric and heteromeric 5-HT(3)R binding interfaces, provide a possible rationalization both of the higher potency of palonosetron with respect to other antagonists, and of its previously reported allosteric binding and positive cooperativity properties. Granisetron 101-112 5-hydroxytryptamine receptor 3A Homo sapiens 157-165 20154102-7 2010 Granisetron or dexamethasone significantly (p < .05) improved macroscopic and histologic scores, curtailed myeloperoxidase activity and diminished colonic levels of inflammatory cytokines and malondialdehyde. Granisetron 0-11 myeloperoxidase Rattus norvegicus 110-125 17182287-11 2007 Intraluminal administration of the 5-HT(3) receptor antagonist granisetron, or the 5-HT(4) receptor antagonist SB 204070 blocked the increase in colonic motility induced by i.c.v. Granisetron 63-74 5-hydroxytryptamine receptor 3A Rattus norvegicus 35-51 17679558-1 2007 Granisetron is a selective 5-HT3 receptor antagonist that is used therapeutically for the prevention of vomiting and nausea associated with emetogenic cancer chemotherapy. Granisetron 0-11 5-hydroxytryptamine receptor 3A Rattus norvegicus 27-41 16476833-5 2006 CYP2D6 is involved in the metabolism of all of the most commonly available agents, except granisetron, and their efficacy and side effects may therefore be affected by the CYP2D6 polymorphism. Granisetron 90-101 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-6 16551910-0 2006 Prevention of postoperative nausea and vomiting with granisetron and dolasetron in relation to CYP2D6 genotype. Granisetron 53-64 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 95-101 16476833-5 2006 CYP2D6 is involved in the metabolism of all of the most commonly available agents, except granisetron, and their efficacy and side effects may therefore be affected by the CYP2D6 polymorphism. Granisetron 90-101 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 172-178 15259496-6 2004 Prior administration of granisetron, a 5-HT3 receptor antagonist, inhibited stress-induced changes in defecation in the visceral hypersensitivity group as well as the controls. Granisetron 24-35 5-hydroxytryptamine receptor 3A Rattus norvegicus 39-53 16497179-4 2006 This rise in permeability was enhanced 25% by 5-HT (3 x 10(-3) m), reduced by the 5-HT(3)-receptor antagonists granisetron (10(-4)-3 x 10(-4) m) or ondansetron (10(-5)-10(-4) m) or by the 5-HT(4) receptor antagonist SB 203186 (10(-4) m). Granisetron 111-122 5-hydroxytryptamine receptor 3A Rattus norvegicus 82-98 16613665-4 2006 Granisetron, a selective antagonist of the 5-hydroxytryptamine3 receptor, also undergoes hepatic metabolism via cytochrome P450 3A4. Granisetron 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 112-131 16192915-8 2005 Instead, granisetron is metabolized via the CYP3A4 isoform, which is not subject to significant genetic polymorphism. Granisetron 9-20 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 44-50 16192915-10 2005 An alternative is to use a 5-HT3 agent that is metabolized independently of the CYP2D6 isoform, such as granisetron, that would obviate the need for genotyping and may lead to improved prophylaxis of PONV. Granisetron 104-115 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 80-86 16115980-8 2005 Conversely, ondansetron, dolasetron, and granisetron also reversibly inhibited nAChR currents in a dose-dependent manner with IC(50)s of 14.2, 7.8, and 4.4 microM for the adult nAChR and 16.0, 18.6, and 13.9 microM for the embryonic nAChR. Granisetron 41-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 79-84 16115980-8 2005 Conversely, ondansetron, dolasetron, and granisetron also reversibly inhibited nAChR currents in a dose-dependent manner with IC(50)s of 14.2, 7.8, and 4.4 microM for the adult nAChR and 16.0, 18.6, and 13.9 microM for the embryonic nAChR. Granisetron 41-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 177-182 16115980-8 2005 Conversely, ondansetron, dolasetron, and granisetron also reversibly inhibited nAChR currents in a dose-dependent manner with IC(50)s of 14.2, 7.8, and 4.4 microM for the adult nAChR and 16.0, 18.6, and 13.9 microM for the embryonic nAChR. Granisetron 41-52 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 177-182 15740177-4 2005 Furthermore, although dolasetron, granisetron, ondansetron and tropisetron are all extensively metabolised by the cytochrome P450 (CYP) system, different components of this system predominate in the metabolism of each of these agents. Granisetron 34-45 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 114-129 15740177-4 2005 Furthermore, although dolasetron, granisetron, ondansetron and tropisetron are all extensively metabolised by the cytochrome P450 (CYP) system, different components of this system predominate in the metabolism of each of these agents. Granisetron 34-45 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 131-134 12788344-3 2003 This stimulant effect was abolished by pretreatment with the 5-HT(3) receptor antagonist granisetron and was subject to a rapid and pronounced tachyphylaxis, due to desensitization of the peripheric cardiac 5-HT(3) receptor. Granisetron 89-100 5-hydroxytryptamine receptor 3A Rattus norvegicus 61-77 14684379-6 2004 Intravenous injection of 5-HT3 receptor antagonist granisetron blocked c-fos expression in all brain nuclei examined, although intracerebroventricular injection of granisetron had no effect, suggesting that 5-HT released from the stomach may activate 5-HT3 receptors located in the peripheral vagal afferent nerve terminals and then induce brain c-fos expression. Granisetron 51-62 5-hydroxytryptamine receptor 3A Rattus norvegicus 25-39 14684379-6 2004 Intravenous injection of 5-HT3 receptor antagonist granisetron blocked c-fos expression in all brain nuclei examined, although intracerebroventricular injection of granisetron had no effect, suggesting that 5-HT released from the stomach may activate 5-HT3 receptors located in the peripheral vagal afferent nerve terminals and then induce brain c-fos expression. Granisetron 51-62 Fos proto-oncogene, AP-1 transcription factor subunit Rattus norvegicus 71-76 14684379-6 2004 Intravenous injection of 5-HT3 receptor antagonist granisetron blocked c-fos expression in all brain nuclei examined, although intracerebroventricular injection of granisetron had no effect, suggesting that 5-HT released from the stomach may activate 5-HT3 receptors located in the peripheral vagal afferent nerve terminals and then induce brain c-fos expression. Granisetron 51-62 Fos proto-oncogene, AP-1 transcription factor subunit Rattus norvegicus 346-351 12943486-6 2003 Granisetron and other 5-HT(3)-receptor antagonists are first-line agents for acute chemotherapy-induced nausea and vomiting (CINV), whereas combination therapy with 5-HT(3)-receptor antagonists, dexamethasone and neurokinin (NK)-1 receptor antagonism (i.e., with the recently approved aprepitant) is an effective approach to prevent delayed CINV. Granisetron 0-11 tachykinin receptor 1 Homo sapiens 213-239 11819027-5 2002 The paroxetine-induced increase in extracellular dopamine concentration, but not 5-HT concentration, was inhibited by the 5-HT(3)-receptor antagonist granisetron. Granisetron 150-161 5-hydroxytryptamine receptor 3A Rattus norvegicus 122-138 12546311-0 2002 Comparative study of low-dose oral granisetron plus dexamethasone and high-dose metoclopramide plus dexamethasone in prevention of nausea and vomiting induced by CHOP-therapy in young patients with non-Hodgkin"s lymphoma. Granisetron 35-46 DNA damage inducible transcript 3 Homo sapiens 162-166 12680915-7 2003 Either granisetron (5-HT3 receptor antagonist, 1 micromol L(-1)) or SB204070 (5-HT4 receptor antagonist, 1 micromol L(-1)) in the stimulation chamber significantly decreased IJPs; these decreases were not additive. Granisetron 7-18 5-hydroxytryptamine receptor 3A Rattus norvegicus 20-34 15041274-9 2003 When baseline samples were excluded, the correlation remained strong for CWB ENOX times and anti-Xa levels (r=0.84, p<0.001), but was only moderate for NCWB (r=0.73, p<0.001). Granisetron 73-76 JPX transcript, XIST activator Homo sapiens 77-81 15041274-11 2003 A CWB ENOX time >/=200 s corresponded to anti-Xa levels >/=0.8 IU/ml in 96% (93/96) of patients. Granisetron 2-5 JPX transcript, XIST activator Homo sapiens 6-10 12546311-7 2002 In conclusion, low-dose oral granisetron combined with intravenous dexamethasone had significantly higher protective effects against both acute and delayed nausea and vomiting induced by CHOP-therapy. Granisetron 29-40 DNA damage inducible transcript 3 Homo sapiens 187-191 12077173-11 2002 The number of APs evoked by ATP was reduced, but not abolished, by the selective 5-HT3 receptor antagonist granisetron (1 microm in the bath). Granisetron 107-118 ATPase phospholipid transporting 8A2 Homo sapiens 28-31 11742289-0 2001 IgE-mediated allergy to granisetron and safe use of ondansetron. Granisetron 24-35 immunoglobulin heavy constant epsilon Homo sapiens 0-3 11833417-3 2001 The Con A- and LPS-stimulated SPR was enhanced in a dose-dependent manner by 5-HT3 receptor antagonist granisetron (GNT) (0.1-0.4 mg/kg, i.p.). Granisetron 103-114 5-hydroxytryptamine receptor 3A Rattus norvegicus 77-91 11762972-2 2001 This is particularly relevant with the high-cost 5HT3 antiemetics, which include ondansetron, dolasetron and granisetron. Granisetron 109-120 5-hydroxytryptamine receptor 3A Homo sapiens 49-53 9729402-1 1998 The 5-HT3 receptor antagonists, ondansetron, MDL 72222 and granisetron (0.01-1 microM), produced a concentration-dependent increase of K+-evoked [3H]ACh efflux in slices from rat entorhinal cortex preloaded with [3H]choline. Granisetron 59-70 5-hydroxytryptamine receptor 3A Rattus norvegicus 4-18 10739360-7 2000 When CDP/ ADM and IFO are delivered on multiple days by CI, granisetron, ondansetron and tropisetron have the same antiemetic efficacy, which declines from the first day onward through successive days. Granisetron 60-71 adrenomedullin Homo sapiens 10-21 9884318-10 1999 Because granisetron has been reported to be metabolized primarily by the cytochrome P-450 (CYP) 3A isozyme family in humans, it is possible that cigarette smoke could be an inducer of CYP3A or that CYP1A2, also implicated in the metabolism of granisetron and known to be induced by smoking, is more important in the biotransformation of granisetron than previously thought. Granisetron 8-19 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 73-98 9884318-10 1999 Because granisetron has been reported to be metabolized primarily by the cytochrome P-450 (CYP) 3A isozyme family in humans, it is possible that cigarette smoke could be an inducer of CYP3A or that CYP1A2, also implicated in the metabolism of granisetron and known to be induced by smoking, is more important in the biotransformation of granisetron than previously thought. Granisetron 8-19 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 184-189 9884318-10 1999 Because granisetron has been reported to be metabolized primarily by the cytochrome P-450 (CYP) 3A isozyme family in humans, it is possible that cigarette smoke could be an inducer of CYP3A or that CYP1A2, also implicated in the metabolism of granisetron and known to be induced by smoking, is more important in the biotransformation of granisetron than previously thought. Granisetron 8-19 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 198-204 9884318-10 1999 Because granisetron has been reported to be metabolized primarily by the cytochrome P-450 (CYP) 3A isozyme family in humans, it is possible that cigarette smoke could be an inducer of CYP3A or that CYP1A2, also implicated in the metabolism of granisetron and known to be induced by smoking, is more important in the biotransformation of granisetron than previously thought. Granisetron 243-254 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 73-98 9884318-10 1999 Because granisetron has been reported to be metabolized primarily by the cytochrome P-450 (CYP) 3A isozyme family in humans, it is possible that cigarette smoke could be an inducer of CYP3A or that CYP1A2, also implicated in the metabolism of granisetron and known to be induced by smoking, is more important in the biotransformation of granisetron than previously thought. Granisetron 243-254 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 198-204 9884318-10 1999 Because granisetron has been reported to be metabolized primarily by the cytochrome P-450 (CYP) 3A isozyme family in humans, it is possible that cigarette smoke could be an inducer of CYP3A or that CYP1A2, also implicated in the metabolism of granisetron and known to be induced by smoking, is more important in the biotransformation of granisetron than previously thought. Granisetron 243-254 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 73-98 9884318-10 1999 Because granisetron has been reported to be metabolized primarily by the cytochrome P-450 (CYP) 3A isozyme family in humans, it is possible that cigarette smoke could be an inducer of CYP3A or that CYP1A2, also implicated in the metabolism of granisetron and known to be induced by smoking, is more important in the biotransformation of granisetron than previously thought. Granisetron 243-254 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 198-204 10974317-4 2000 The reduction by CPBG of the NMDA-evoked cardiac response was blocked by prior intra-NTS microinjection of granisetron, a 5-HT(3) receptor antagonist, as well as bicuculline, a GABA(A) receptor antagonist. Granisetron 107-118 5-hydroxytryptamine receptor 3A Rattus norvegicus 122-138 9932018-6 1998 At doses of granisetron and devazepide which completely block the response to exogenous 5-HT and CCK, the afferent fibres still responded to both mechanical and chemical stimulation of the mucosa. Granisetron 12-23 cholecystokinin Homo sapiens 97-100 9635896-4 1998 This action was markedly attenuated or completely blocked by the selective 5-HT3 receptor antagonists granisetron and BRL 46470A, but not other receptor antagonists. Granisetron 102-113 5-hydroxytryptamine receptor 3A Rattus norvegicus 75-89 9593908-2 1998 application of the 5-HT3 receptor antagonist granisetron (0.016-0.16 microg kg-1) and the agonist phenylbiguanide (0.3-3 microg kg-1) on reflex bradycardia evoked by injection of phenylbiguanide (i.v. Granisetron 45-56 5-hydroxytryptamine receptor 3A Rattus norvegicus 19-33 8814902-2 1996 The 5-HT3 receptor antagonists ondansetron and granisetron (0.01-10 microM) produced a concentration-dependent increase in both spontaneous and K(+)-evoked [3H]ACh release in the two brain regions studied. Granisetron 47-58 5-hydroxytryptamine receptor 3A Rattus norvegicus 4-18 8996183-3 1997 The selective 5-HT3 receptor antagonists GK-128, granisetron, ramosetron, azasetron and ondansetron depressed the increase in fecal pellet output caused by 2-methyl-5-HT and by wrap-restraint stress. Granisetron 49-60 5-hydroxytryptamine receptor 3A Rattus norvegicus 14-28 8829149-3 1996 Intrathecal administration of selective 5-HT3 receptor antagonists, granisetron (0.1-100 pmol/rat) and ondansetron (1-1000 pmol/rat), reduced the second phase of the formalin-induced aversive responses without affecting the first one. Granisetron 68-79 5-hydroxytryptamine receptor 3A Rattus norvegicus 40-54 9549649-1 1998 This study investigated whether granisetron, a 5-HT3 receptor antagonist, can alter the Bezold-Jarisch reflex (i.e., hypotension and inappropriate heart rate slowing). Granisetron 32-43 5-hydroxytryptamine receptor 3A Oryctolagus cuniculus 47-61 9490878-12 1998 5-HT response was completely abolished by the 5-HT3 receptor antagonist, granisetron (0.5 mg kg-1). Granisetron 73-84 5-hydroxytryptamine receptor 3A Rattus norvegicus 46-60 9341912-6 1997 1-(3,5-Dichlorophenyl)-3-[(5-methyl-1H-imidazol-4-yl)methyl]imidazoli din-2-one (58), in particular, displayed very high affinity for the 5-HT3 receptor (Ki of 0.038 nM) with a Kb of 5.62 nM in the GPI assay, being more potent than the reference compounds (ondansetron, tropisetron, granisetron, and BRL 46,470) tested. Granisetron 283-294 5-hydroxytryptamine receptor 3A Rattus norvegicus 138-152 9313899-8 1997 This study provides evidence that contrary to tropisetron, doses of granisetron able to inhibit the effect of a 5-HT3 receptor agonist failed to reduce that of 5-HT. Granisetron 68-79 5-hydroxytryptamine receptor 3A Rattus norvegicus 112-126 9087290-0 1997 [Antiemetic efficacy of granisetron in repeated CAF chemotherapy after breast cancer operation]. Granisetron 24-35 lysine acetyltransferase 2B Homo sapiens 48-51 9087290-1 1997 The antiemetic efficacy of granisetron in repeated CAF chemotherapy after breast cancer operation was investigated. Granisetron 27-38 lysine acetyltransferase 2B Homo sapiens 51-54 9087290-8 1997 The antiemetic efficacy of granisetron decreased significantly by repeated CAF chemotherapy. Granisetron 27-38 lysine acetyltransferase 2B Homo sapiens 75-78 8874143-7 1996 However, they are similar to those exhibited by granisetron [endo-1-methyl-N-(9-methyl-9-azabicyclo[3.3.1]non-3-yl)-1 H-indazole-3-carboxamide], a 5-HT3 receptor antagonist. Granisetron 48-59 5-hydroxytryptamine receptor 3A Rattus norvegicus 147-161 1966601-1 1990 The 5-HT3 receptor antagonists, ICS205-930, granisetron and zacopride, at low doses, inhibited the hyperactivity caused by a 13 day mesolimbic dopamine infusion in the rat. Granisetron 44-55 5-hydroxytryptamine receptor 3A Rattus norvegicus 4-18 8991800-0 1995 Effects of granisetron, a 5-HT3 receptor antagonist, on morphine-induced potentiation of brain stimulation reward. Granisetron 11-22 5-hydroxytryptamine receptor 3A Homo sapiens 26-31 7963267-7 1994 IV administration of the 5-HT3 receptor antagonist granisetron (50 micrograms/kg), after bilateral vagotomy had no effect on the response to central vagal stimulation. Granisetron 51-62 5-hydroxytryptamine receptor 3A Rattus norvegicus 25-39 7922584-4 1994 The selective 5-HT3 receptor antagonist, granisetron, when applied as a pretreatment completely prevented but did not reverse this action when given after administration of 2-methyl-5-HT while the non-specific 5-HT1,2 receptor antagonist, metergoline, was ineffective. Granisetron 41-52 5-hydroxytryptamine receptor 3A Rattus norvegicus 14-28 8507391-2 1993 Systemic administration of the 5-HT1A agonist ipsapirone (1.25-5.0 mg/kg) caused a dose-dependent decrease in ethanol preference and intake, while the 5-HT2 antagonist ritanserin (1.25-5.0 mg/kg) and the 5-HT3 antagonists ondansetron (0.01-1.0 mg/kg) and granisetron (0.5-1.0 mg/kg) failed to alter ethanol consumption. Granisetron 255-266 5-hydroxytryptamine receptor 1A Rattus norvegicus 31-37 8496821-2 1993 This compound, as well as ondansetron and granisetron, dose-dependently inhibited the von Bezold-Jarish reflex, a 5-HT3 receptor-mediated response, after intravenous (i.v.) Granisetron 42-53 5-hydroxytryptamine receptor 3A Rattus norvegicus 114-128 1682469-1 1991 Studies have been carried out on 7 male adult rats to investigate how the action of the selective 5-HT3 receptor antagonist, granisetron, influences gastrointestinal transit under control conditions and when it is delayed by ileal infusion of lipid. Granisetron 125-136 5-hydroxytryptamine receptor 3A Rattus norvegicus 98-112 8556268-8 1995 This release of 5-HT was significantly reduced by granisetron, a selective 5-HT3 receptor antagonist. Granisetron 50-61 5-hydroxytryptamine receptor 3A Rattus norvegicus 75-89 7758060-2 1995 On the first day of granisetron treatment, a statistically significant association between complete response and dose was seen (P = 0.001), with the maximum response (81.1%) achieved at a dose of 1 mg BID. Granisetron 20-31 BH3 interacting domain death agonist Homo sapiens 201-204 7758060-3 1995 The 24-hour complete response rate with granisetron 1 mg BID was significantly higher than with 0.25 mg BID (61.1%) or 0.5 mg BID (70.2%) (P < 0.009). Granisetron 40-51 BH3 interacting domain death agonist Homo sapiens 57-60 7758060-4 1995 The complete response rate for days 0 to 6 was significantly higher with granisetron at 1 mg BID (58.8%) than with 0.25 mg BID (43.7%) or 0.5 mg BID (53.6%) (P < 0.009). Granisetron 73-84 BH3 interacting domain death agonist Homo sapiens 93-96 7888294-13 1994 Studies using chemical inhibitors selective for individual P450 enzymes indicated the involvement of cytochrome P450 3A (CYP3A), both pathways of granisetron metabolism being very sensitive to ketoconazole inhibition. Granisetron 146-157 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 101-119 7888294-13 1994 Studies using chemical inhibitors selective for individual P450 enzymes indicated the involvement of cytochrome P450 3A (CYP3A), both pathways of granisetron metabolism being very sensitive to ketoconazole inhibition. Granisetron 146-157 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 121-126 7858893-12 1994 5-HT3 receptor antagonists such as ondansetron, granisetron and tropisetron (0.2 microM) significantly blocked the enhanced K(+)-evoked [3H]-DA efflux from rat olfactory tubercle slices induced by 2-methyl-5HT. Granisetron 48-59 5-hydroxytryptamine receptor 3A Rattus norvegicus 0-14 7988637-5 1994 In the presence of the 5-HT3 receptor antagonists, granisetron or ondansetron, 5-HT responses were diminished and exhibited an increased latency to peak. Granisetron 51-62 5-hydroxytryptamine receptor 3A Rattus norvegicus 23-37 7919451-1 1994 This review discusses the development and use of 5-hydroxytryptamine3 (5-HT3) antagonists, especially granisetron, for the treatment of chemotherapy-induced emesis. Granisetron 102-113 5-hydroxytryptamine receptor 3A Homo sapiens 71-76 7919451-3 1994 Granisetron, a new 5-HT3, is approximately 400 times more potent than metoclopramide and, unlike metoclopramide, does not produce extrapyramidal side effects. Granisetron 0-11 5-hydroxytryptamine receptor 3A Homo sapiens 19-24 8032707-1 1994 Granisetron, a potent and selective 5-hydroxytryptamine receptor (5-HT3) antagonist was reported to be an effective antiemetic agent both in animal studies and in patients given highly emetogenic chemotherapy. Granisetron 0-11 5-hydroxytryptamine receptor 3A Homo sapiens 66-71 8103099-1 1993 Studies were carried out on 20 male adult rats to investigate how the action of the selective 5-HT3-receptor antagonists, granisetron and ondansetron, influence gastrointestinal transit under control conditions and when stomach-to-caecum transit was delayed by ileal infusion of lipid. Granisetron 122-133 5-hydroxytryptamine receptor 3A Rattus norvegicus 94-108 1665793-0 1991 The 5-HT3 receptor antagonists LY 277359 and granisetron potentiate the suppressant action of apomorphine on the basal firing rate of ventral tegmental dopamine cells. Granisetron 45-56 5-hydroxytryptamine receptor 3A Rattus norvegicus 4-18 1830236-13 1991 5-HT3 receptor antagonists competed for [3H]-quipazine binding with high nanomolar affinities in the three preparations and the rank order of affinity was: (S)-zacopride > quarternized ICS 205-930 2 granisetron > ondansetron > ICS 205-209 (R)-zacopride > quipazine > renzapride > MDL-72222 > butanopride > metoclopramide. Granisetron 202-213 5-hydroxytryptamine receptor 3A Rattus norvegicus 0-14 33399295-4 2021 Here, we sought to explore the antidyskinetic efficacy of granisetron, another clinically available 5-HT3 receptor antagonist. Granisetron 58-69 5-hydroxytryptamine receptor 3A Rattus norvegicus 100-114 33767348-7 2021 To gain further translational insights, we revealed that combined treatment of zonisamide (enhancing the GABAAR-alpha5 signaling) and granisetron (a selective 5-HT3R antagonist) alleviates mental dysfunction and yields a robust reversal of diet-induced obesity by reducing total calorie intake and altering food preference towards a healthy low-fat diet. Granisetron 134-145 5-hydroxytryptamine receptor 3A Homo sapiens 159-165 34663518-9 2021 Furthermore, granisetron administration significantly reduced TNF-alpha, IL-6, HMGB1 and NF-kappaB. Granisetron 13-24 tumor necrosis factor Rattus norvegicus 62-71 34663518-9 2021 Furthermore, granisetron administration significantly reduced TNF-alpha, IL-6, HMGB1 and NF-kappaB. Granisetron 13-24 interleukin 6 Rattus norvegicus 73-77 34663518-9 2021 Furthermore, granisetron administration significantly reduced TNF-alpha, IL-6, HMGB1 and NF-kappaB. Granisetron 13-24 high mobility group box 1 Rattus norvegicus 79-84 34663518-11 2021 Interestingly, granisetron inhibited pyroptosis as it reduced NLRP3, IL-1beta and caspase-1. Granisetron 15-26 NLR family, pyrin domain containing 3 Rattus norvegicus 62-67 34663518-11 2021 Interestingly, granisetron inhibited pyroptosis as it reduced NLRP3, IL-1beta and caspase-1. Granisetron 15-26 interleukin 1 alpha Rattus norvegicus 69-77 34663518-11 2021 Interestingly, granisetron inhibited pyroptosis as it reduced NLRP3, IL-1beta and caspase-1. Granisetron 15-26 caspase 1 Rattus norvegicus 82-91 34663518-12 2021 Granisetron was shown to increase Nrf2 and HO-1. Granisetron 0-11 NFE2 like bZIP transcription factor 2 Rattus norvegicus 34-38 34663518-12 2021 Granisetron was shown to increase Nrf2 and HO-1. Granisetron 0-11 heme oxygenase 1 Rattus norvegicus 43-47 34208557-5 2021 In HEK293 cells, the inhibition of ASP+ uptake by OCT2 listed in order of potency was palonosetron (IC50: 2.6 muM) > ondansetron > granisetron > tropisetron > dolasetron (IC50: 85.4 muM) and the inhibition of ASP+ uptake by MATE1 in order of potency was ondansetron (IC50: 0.1 muM) > palonosetron = tropisetron > granisetron > dolasetron (IC50: 27.4 muM). Granisetron 131-142 solute carrier family 22 member 2 Homo sapiens 50-54 34208557-5 2021 In HEK293 cells, the inhibition of ASP+ uptake by OCT2 listed in order of potency was palonosetron (IC50: 2.6 muM) > ondansetron > granisetron > tropisetron > dolasetron (IC50: 85.4 muM) and the inhibition of ASP+ uptake by MATE1 in order of potency was ondansetron (IC50: 0.1 muM) > palonosetron = tropisetron > granisetron > dolasetron (IC50: 27.4 muM). Granisetron 313-324 solute carrier family 22 member 2 Homo sapiens 50-54 35093429-4 2022 This assay adapted a CYP1A1 selective reaction of granisetron 7-hydroxylation in response to an AhR inducer, 6-formylindolo(3,2-b)carbazole (FICZ), in HepaRG and A549 cell lines. Granisetron 50-61 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 21-27 35093429-4 2022 This assay adapted a CYP1A1 selective reaction of granisetron 7-hydroxylation in response to an AhR inducer, 6-formylindolo(3,2-b)carbazole (FICZ), in HepaRG and A549 cell lines. Granisetron 50-61 aryl hydrocarbon receptor Homo sapiens 96-99 32859502-4 2020 METHODS: In this single-center, prospective, observational, real world study, GTDS plus dexamethasone was administered to MM patients receiving chemo-mobilization based on CY 2 g/m2 plus G-CSF in an outpatient setting. Granisetron 78-82 colony stimulating factor 3 Homo sapiens 187-192 33152452-2 2021 We have shown, in the hemi-parkinsonian rat model of PD, that the selective serotonin type 3 (5-HT3) receptor antagonists ondansetron and granisetron decreased the severity of established dyskinesia, and ondansetron even attenuated the development of dyskinesia. Granisetron 138-149 5-hydroxytryptamine receptor 3A Rattus norvegicus 76-109