PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 34803706-8 2021 Lorcaserin did not change insulin synthesis ATP content, but lorcaserin decrease cytosolic free calcium level ((Ca2+)i) in MIN6 cells stimulated with glucose and also inhibit insulin secretion and (Ca2+)i in MIN6 treated with potassium chloride. lorcaserin 61-71 insulin Homo sapiens 175-182 34803706-1 2021 Lorcaserin is a serotonergic agonist specific to the 5-hydroxytryptamine 2c receptor (5-HT2CR) that is FDA approved for the long-term management of obesity with or without at least one weight-related comorbidity. lorcaserin 0-10 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 53-84 34803706-12 2021 These results highlight a novel signaling mechanism of lorcaserin and provide valuable insights into the further investigation of 5-HT2CR functions in beta-cell biology and it also provides guidance for the clinical application of lorcaserin. lorcaserin 55-65 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 130-137 34803706-1 2021 Lorcaserin is a serotonergic agonist specific to the 5-hydroxytryptamine 2c receptor (5-HT2CR) that is FDA approved for the long-term management of obesity with or without at least one weight-related comorbidity. lorcaserin 0-10 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 86-93 33418204-4 2021 The purpose of this trial was to determine if lorcaserin, a 5HT2c agonist, improves outpatient XR-NTX induction rates. lorcaserin 46-56 5-hydroxytryptamine receptor 2C Homo sapiens 60-65 34803706-2 2021 Lorcaserin can restrain patients" appetite and improve insulin sensitivity and hyperinsulinemia mainly through activating 5-HT2CR in the hypothalamus. lorcaserin 0-10 insulin Homo sapiens 55-62 34803706-2 2021 Lorcaserin can restrain patients" appetite and improve insulin sensitivity and hyperinsulinemia mainly through activating 5-HT2CR in the hypothalamus. lorcaserin 0-10 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 122-129 34803706-6 2021 Dose-dependent activation of 5-HT2CR by lorcaserin suppressed GSIS and SB242084 or knockdown of 5-HT2CR abolished lorcaserin"s effect in vitro. lorcaserin 40-50 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 29-36 34803706-6 2021 Dose-dependent activation of 5-HT2CR by lorcaserin suppressed GSIS and SB242084 or knockdown of 5-HT2CR abolished lorcaserin"s effect in vitro. lorcaserin 114-124 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 96-103 34803706-8 2021 Lorcaserin did not change insulin synthesis ATP content, but lorcaserin decrease cytosolic free calcium level ((Ca2+)i) in MIN6 cells stimulated with glucose and also inhibit insulin secretion and (Ca2+)i in MIN6 treated with potassium chloride. lorcaserin 0-10 insulin Homo sapiens 175-182 35599337-6 2022 We propose to test the hypothesis in a diet-induced obesity (DIO) rat model by treating animals with the 5-HT2C agonist lorcaserin and the H1 agonist and H3 antagonist betahistine. lorcaserin 120-130 5-hydroxytryptamine receptor 2C Rattus norvegicus 105-111 34031163-6 2021 Thus, our results prove the concept that inhibition of 5-HT2CR desensitization can be a valid strategy to improve the long-term weight loss effects of lorcaserin or other 5-HT2CR agonists, and also provide an intellectual framework to develop effective long-term management of weight by targeting 5-HT2CR desensitization.SIGNIFICANCE STATEMENT:By demonstrating that the combination of barbadin with a GPCR agonist can provide prolonged weight-lowering benefits in a preclinical setting, our work should call for additional efforts to validate barbadin as a safe and effective medicine or to use barbadin as a lead compound to develop more suitable compounds for obesity treatment. lorcaserin 151-161 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 55-62 34031163-7 2021 These results prove the concept that inhibition of 5-HT2CR desensitization can be a valid strategy to improve the long-term weight loss effects of lorcaserin or other 5-HT2CR agonists. lorcaserin 147-157 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 51-58 33928736-2 2021 Lorcaserin, a 5-HT2C receptor agonist, attenuates drug self-administration in animal models. lorcaserin 0-10 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 14-29 34130255-1 2021 Recent preclinical and clinical studies suggest that lorcaserin, a preferential serotonin 2C receptor (5-HT2CR) agonist that was approved for the treatment of obesity, possesses antiepileptic properties. lorcaserin 53-63 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 80-110 34130255-12 2021 If mice were treated with the selective 5-HT2CR antagonist SB 242084 (0.5 or 1 mg/kg) plus lorcaserin (3 mg/kg), a significantly increased HTR was observed, relative to vehicle (P = 0.01 and P = 0.03), however, the HTR was much lower than what was elicited by DOI or DOI plus lorcaserin. lorcaserin 91-101 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 40-47 35094259-1 2022 Lorcaserin, a selective serotonin 5-HT2C receptor agonist, was developed as an appetite suppressant with the rationale of minimizing the risk of cardiovascular toxicity associated with non-selective serotoninergic agents such as fenfluramine. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Homo sapiens 24-49 34031163-0 2021 Barbadin potentiates long-term effects of lorcaserin on POMC neurons and weight loss. lorcaserin 42-52 proopiomelanocortin Homo sapiens 56-60 33909316-4 2021 The serotonin 2C receptor (5-HT2C R) is the primary receptor through which 5-HT impacts feeding and body weight and 5-HT2C R agonist lorcaserin was released for obesity treatment in 2012. lorcaserin 133-143 5-hydroxytryptamine receptor 2C Homo sapiens 27-33 33467149-5 2021 Analyses of brain slices from nicotine-withdrawn animals revealed that lorcaserin treatment recovered the reduced number of doublecortin (DCX)-positive cells, but it did not affect the number of Ki-67- or 5-bromo-2"-deoxyuridine (BrdU)-positive cells or the maturation of proliferating neurons in drug-weaned rats. lorcaserin 71-81 doublecortin Rattus norvegicus 124-136 33467149-5 2021 Analyses of brain slices from nicotine-withdrawn animals revealed that lorcaserin treatment recovered the reduced number of doublecortin (DCX)-positive cells, but it did not affect the number of Ki-67- or 5-bromo-2"-deoxyuridine (BrdU)-positive cells or the maturation of proliferating neurons in drug-weaned rats. lorcaserin 71-81 doublecortin Rattus norvegicus 138-141 32234370-0 2020 Lorcaserin Administration has Pro-Ejaculatory Effects in Rats via 5-HT2C Receptors Activation: A Putative Pharmacologic Strategy to Delayed Ejaculation? lorcaserin 0-10 5-hydroxytryptamine receptor 2C Rattus norvegicus 66-72 32642780-1 2020 Lorcaserin (LOR) is selective and potent antiobesity drug that targets the activation of the serotonin 5HT2C receptor. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Homo sapiens 93-117 32642780-1 2020 Lorcaserin (LOR) is selective and potent antiobesity drug that targets the activation of the serotonin 5HT2C receptor. lorcaserin 12-15 5-hydroxytryptamine receptor 2C Homo sapiens 93-117 32234370-1 2020 BACKGROUND: Lorcaserin is an anti-obesity drug whose weight loss effect results from 5-hydroxytryptamin (5-HT)2C receptors activation. lorcaserin 12-22 5-hydroxytryptamine receptor 2C Rattus norvegicus 105-112 32234370-8 2020 On the other hand, lorcaserin administration (0.3-1.0 mg/kg, intravenous) induced ejaculation in anesthetized rats, which was prevented by the 5-HT2C-selective antagonist SB 242084 (0.1 and 0.3 mg/kg, intravenous). lorcaserin 19-29 5-hydroxytryptamine receptor 2C Rattus norvegicus 143-149 32234370-15 2020 CONCLUSION: Our results demonstrate that the clinically approved 5-HT2C agonist lorcaserin is a strong facilitator of ejaculation in rats. lorcaserin 80-90 5-hydroxytryptamine receptor 2C Rattus norvegicus 65-71 32234370-17 2020 Lorcaserin Administration has Pro-Ejaculatory Effects in Rats via 5-HT2C Receptors Activation: A Putative Pharmacologic Strategy to Delayed Ejaculation? lorcaserin 0-10 5-hydroxytryptamine receptor 2C Rattus norvegicus 66-72 31987863-2 2020 Lorcaserin is a serotonin 5-HT2C receptor (5-HT2CR) agonist that has recently been reported to reduce abuse-related effects of the opioid analgesic oxycodone. lorcaserin 0-10 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 43-50 31880085-10 2020 Moreover, we identified that 95% 5-HT2c receptors were colocalized with NPY positive neurons, and increased Arc NPY mRNA expression induced by risperidone was markedly reduced by cotreatment with lorcaserin, a specific 5-HT2c receptor agonist. lorcaserin 196-206 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 33-39 31880085-10 2020 Moreover, we identified that 95% 5-HT2c receptors were colocalized with NPY positive neurons, and increased Arc NPY mRNA expression induced by risperidone was markedly reduced by cotreatment with lorcaserin, a specific 5-HT2c receptor agonist. lorcaserin 196-206 neuropeptide Y Mus musculus 72-75 31880085-10 2020 Moreover, we identified that 95% 5-HT2c receptors were colocalized with NPY positive neurons, and increased Arc NPY mRNA expression induced by risperidone was markedly reduced by cotreatment with lorcaserin, a specific 5-HT2c receptor agonist. lorcaserin 196-206 neuropeptide Y Mus musculus 112-115 31880085-10 2020 Moreover, we identified that 95% 5-HT2c receptors were colocalized with NPY positive neurons, and increased Arc NPY mRNA expression induced by risperidone was markedly reduced by cotreatment with lorcaserin, a specific 5-HT2c receptor agonist. lorcaserin 196-206 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 33-48 31987863-12 2020 Together, these data indicate that lorcaserin-mediated activation of the 5-HT2CR may represent a new pharmacological approach to augment opioid-induced antinociception. lorcaserin 35-45 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 73-80 32079105-4 2020 Lorcaserin, an appetite control drug, has demonstrated efficacy in appetite control by targeting 5-HT2C but causes undesirable side effects. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Homo sapiens 97-103 31544267-7 2020 Compared with placebo, lorcaserin not only reduced weight, BMI and waist circumference but also improved SBP, DBP, heart rate, LDL, triglycerides, fasting plasma glucose and HbA1c. lorcaserin 23-33 selenium binding protein 1 Homo sapiens 105-108 31544267-7 2020 Compared with placebo, lorcaserin not only reduced weight, BMI and waist circumference but also improved SBP, DBP, heart rate, LDL, triglycerides, fasting plasma glucose and HbA1c. lorcaserin 23-33 D-box binding PAR bZIP transcription factor Homo sapiens 110-113 30961494-0 2020 Chemistry, Analysis, Pharmacokinetics and Pharmacodynamics aspects of Lorcaserin, a selective serotonin 5-HT2C receptor agonist: An update. lorcaserin 70-80 5-hydroxytryptamine receptor 2C Homo sapiens 94-119 30622024-7 2019 Similar effect of compound 58 was observed with synthetic orthosteric agonist lorcaserin on 5-HT2B. lorcaserin 78-88 5-hydroxytryptamine receptor 2B Rattus norvegicus 92-98 31127052-6 2019 Consistent with this, loss of the BBSome reduced cell surface expression of the 5-HT2CR, interfered with serotonin-evoked increase in intracellular calcium and membrane potential, and blunted the anorectic and weight-reducing responses evoked by the 5-HT2cR agonist, lorcaserin. lorcaserin 267-277 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 80-87 30689993-2 2019 For example, activation of serotonin 5-HT2C GPCRs is pharmacotherapeutic for obesity, but there is tolerance to the anorectic effect of the only approved 5-HT2C agonist, lorcaserin. lorcaserin 170-180 5-hydroxytryptamine receptor 2C Homo sapiens 37-43 30689993-2 2019 For example, activation of serotonin 5-HT2C GPCRs is pharmacotherapeutic for obesity, but there is tolerance to the anorectic effect of the only approved 5-HT2C agonist, lorcaserin. lorcaserin 170-180 5-hydroxytryptamine receptor 2C Homo sapiens 154-160 30689993-4 2019 Lorcaserin, which displays potency and efficacy equal to 5-HT, desensitized the 5-HT2C receptor significantly more than 5-HT (p<0.05). lorcaserin 0-10 5-hydroxytryptamine receptor 2C Homo sapiens 80-86 31019729-4 2019 Methods: This post hoc analysis evaluated the magnitude of weight loss in adults across age quartiles with lorcaserin, a serotonin (5-HT) 2C receptor agonist indicated as an adjunct to a reduced-caloric diet and increased physical activity for chronic weight management. lorcaserin 107-117 5-hydroxytryptamine receptor 2C Homo sapiens 121-149 31774584-0 2019 5-HT2c agonist, lorcaserin, reduces aggressive responding in intermittent explosive disorder: A pilot study. lorcaserin 16-26 5-hydroxytryptamine receptor 2C Homo sapiens 0-6 31774584-3 2019 OBJECTIVES: To test the hypothesis that pretreatment with the selective 5-HT2c agonist, lorcaserin, can reduce aggressive responding in impulsively aggressive individuals. lorcaserin 88-98 5-hydroxytryptamine receptor 2C Homo sapiens 72-78 31581577-5 2019 Due to limited drug options available and considering the adverse drug effects of Lorcaserin, the development of new drugs which are highly specific toward the 5HT2C target and with lesser side effects is essential. lorcaserin 82-92 5-hydroxytryptamine receptor 2C Homo sapiens 160-165 31087031-9 2019 These data have implications for our understanding of the aetiology of PWS-related behavioural traits and translational relevance for individuals with PWS who may seek to control appetite with the new obesity treatment 5-HT2CR agonist lorcaserin. lorcaserin 235-245 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 219-226 30929417-4 2019 Lorcaserin stimulates proopiomelanocortin (POMC)/cocaine- and amphetamine-regulated transcript (CART) neurons and inhibits neuropeptide Y (NPY)/agouti-related peptide (AgRP) neurons, which results in the activation of melanocortin 3/4 receptors. lorcaserin 0-10 proopiomelanocortin Homo sapiens 22-41 30929417-4 2019 Lorcaserin stimulates proopiomelanocortin (POMC)/cocaine- and amphetamine-regulated transcript (CART) neurons and inhibits neuropeptide Y (NPY)/agouti-related peptide (AgRP) neurons, which results in the activation of melanocortin 3/4 receptors. lorcaserin 0-10 proopiomelanocortin Homo sapiens 43-47 30929417-4 2019 Lorcaserin stimulates proopiomelanocortin (POMC)/cocaine- and amphetamine-regulated transcript (CART) neurons and inhibits neuropeptide Y (NPY)/agouti-related peptide (AgRP) neurons, which results in the activation of melanocortin 3/4 receptors. lorcaserin 0-10 neuropeptide Y Homo sapiens 123-137 30929417-4 2019 Lorcaserin stimulates proopiomelanocortin (POMC)/cocaine- and amphetamine-regulated transcript (CART) neurons and inhibits neuropeptide Y (NPY)/agouti-related peptide (AgRP) neurons, which results in the activation of melanocortin 3/4 receptors. lorcaserin 0-10 neuropeptide Y Homo sapiens 139-142 30929417-4 2019 Lorcaserin stimulates proopiomelanocortin (POMC)/cocaine- and amphetamine-regulated transcript (CART) neurons and inhibits neuropeptide Y (NPY)/agouti-related peptide (AgRP) neurons, which results in the activation of melanocortin 3/4 receptors. lorcaserin 0-10 agouti related neuropeptide Homo sapiens 168-172 30293771-18 2018 In patients with diabetes, lorcaserin resulted in a reduction of 0 33% (95% CI 0 29-0 38; p<0 0001) in HbA1c compared with placebo at 1 year from a mean baseline of 53 mmol/mol (7 0%). lorcaserin 27-37 hemoglobin subunit alpha 1 Homo sapiens 106-110 30419272-0 2019 Persistent attenuation of nicotine self-administration in rats by co-administration of chronic nicotine infusion with the dopamine D1 receptor antagonist SCH-23390 or the serotonin 5-HT2C agonist lorcaserin. lorcaserin 196-206 5-hydroxytryptamine receptor 2C Rattus norvegicus 181-187 30523523-6 2019 Preclinical models suggest that nociceptin receptor antagonists, the selective serotonin 5-HT2C receptor agonist lorcaserin, monoamine stabilizers, and selective orexin-1 receptor antagonists might be helpful. lorcaserin 113-123 5-hydroxytryptamine receptor 2C Homo sapiens 79-104 30233224-4 2018 Lorcaserin is thought to reduce weight by targeting the serotonin (5HT2c) system to induce satiety. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Homo sapiens 67-72 30282043-3 2018 (2018) demonstrate that a small and often overlooked population of POMC neurons in the brainstem contributes to satiation induced by the FDA-approved drug lorcaserin. lorcaserin 155-165 proopiomelanocortin Homo sapiens 67-71 30574343-6 2018 Results: According to this mediation analysis, lorcaserin 10 mg BID improved a spectrum of adiposopathic metabolic abnormalities with varying contributions attributable to weight loss. lorcaserin 47-57 BH3 interacting domain death agonist Homo sapiens 64-67 30574343-9 2018 Conclusions: Across Phase III clinical trials, lorcaserin 10 mg BID improved multiple cardiometabolic parameters through both weight-loss dependent and independent mechanisms. lorcaserin 47-57 BH3 interacting domain death agonist Homo sapiens 64-67 29217539-0 2018 Inhibition of Cocaine and 3,4-Methylenedioxypyrovalerone (MDPV) Self-Administration by Lorcaserin Is Mediated by 5-HT2C Receptors in Rats. lorcaserin 87-97 5-hydroxytryptamine receptor 2C Homo sapiens 113-119 29217539-1 2018 Lorcaserin is a serotonin (5-HT)2C receptor-preferring agonist approved by the US Food and Drug Administration to treat obesity. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Homo sapiens 16-43 29217539-3 2018 Although this effect is partially inhibited by a 5-HT2C receptor antagonist (SB242084), lorcaserin also has effects at 5-HT2A and 5-HT1A receptors, and the relative contribution of these receptors to its anti-cocaine effects has not been investigated. lorcaserin 88-98 5-hydroxytryptamine receptor 2A Homo sapiens 119-125 29217539-3 2018 Although this effect is partially inhibited by a 5-HT2C receptor antagonist (SB242084), lorcaserin also has effects at 5-HT2A and 5-HT1A receptors, and the relative contribution of these receptors to its anti-cocaine effects has not been investigated. lorcaserin 88-98 5-hydroxytryptamine receptor 1A Homo sapiens 130-136 28805659-6 2017 Finally, we showed that treatment with the HTR2C-specific agonist lorcaserin suppressed olanzapine-induced hyperphagia and weight gain. lorcaserin 66-76 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 43-48 29217539-9 2018 Antagonism of 5-HT2C (but not 5-HT1A or 5-HT2A) receptors blocked the effects of lorcaserin on cocaine and MDPV self-administration. lorcaserin 81-91 5-hydroxytryptamine receptor 2C Homo sapiens 14-20 29217539-10 2018 Taken together, these data provide additional support for further development of 5-HT2C receptor agonists, such as lorcaserin, for the treatment of stimulant abuse. lorcaserin 115-125 5-hydroxytryptamine receptor 2C Homo sapiens 81-87 29040827-1 2017 BACKGROUND: Accumulating evidence suggests that the FDA-approved serotonin 5-HT2C receptor agonist, lorcaserin (Belviq ), may be a promising candidate for the management of substance use disorders, including nicotine addiction. lorcaserin 100-110 5-hydroxytryptamine receptor 2C Homo sapiens 65-90 29031711-6 2017 Examining the mechanism of this effect, we reveal a necessary and sufficient neurochemical mediator of lorcaserin"s glucoregulatory effects, brain pro-opiomelanocortin (POMC) peptides. lorcaserin 103-113 pro-opiomelanocortin-alpha Mus musculus 147-167 29031711-6 2017 Examining the mechanism of this effect, we reveal a necessary and sufficient neurochemical mediator of lorcaserin"s glucoregulatory effects, brain pro-opiomelanocortin (POMC) peptides. lorcaserin 103-113 pro-opiomelanocortin-alpha Mus musculus 169-173 29031711-7 2017 To clarify further lorcaserin"s therapeutic brain circuit, we examined the receptor target of POMC peptides. lorcaserin 19-29 pro-opiomelanocortin-alpha Mus musculus 94-98 28294132-8 2017 Somewhat similar effects were observed with lorcaserin, a 5-HT2C agonist with potent 5-HT2B and 5-HT2A agonist activities, which is approved for treating obesity. lorcaserin 44-54 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 58-64 28294132-8 2017 Somewhat similar effects were observed with lorcaserin, a 5-HT2C agonist with potent 5-HT2B and 5-HT2A agonist activities, which is approved for treating obesity. lorcaserin 44-54 5-hydroxytryptamine (serotonin) receptor 2B Mus musculus 85-97 28099839-5 2017 We also demonstrate that the Ht2Cr agonist lorcaserin-induced improvements in glucose and insulin tolerance are blocked by TrpC5 deficiency in Pomc neurons. lorcaserin 43-53 transient receptor potential cation channel subfamily C member 5 Homo sapiens 123-128 28338324-0 2017 Studies To Examine Potential Tolerability Differences between the 5-HT2C Receptor Selective Agonists Lorcaserin and CP-809101. lorcaserin 101-111 5-hydroxytryptamine receptor 2C Rattus norvegicus 66-72 28338324-1 2017 Lorcaserin (LOR) is a selective 5-HT2C receptor agonist that has been FDA approved as a treatment for obesity. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Rattus norvegicus 32-38 28338324-1 2017 Lorcaserin (LOR) is a selective 5-HT2C receptor agonist that has been FDA approved as a treatment for obesity. lorcaserin 12-15 5-hydroxytryptamine receptor 2C Rattus norvegicus 32-38 27516377-4 2017 Notably, 5-HT medications, including fluoxetine, d-fenfluramine, and lorcaserin (a selective 5-HT2CR agonist), act on 5-HT2CRs expressed by DA neurons to inhibit binge-like eating in mice. lorcaserin 69-79 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 93-100 28099839-5 2017 We also demonstrate that the Ht2Cr agonist lorcaserin-induced improvements in glucose and insulin tolerance are blocked by TrpC5 deficiency in Pomc neurons. lorcaserin 43-53 proopiomelanocortin Homo sapiens 143-147 27241709-0 2016 Lorcaserin and CP-809101 reduce motor impulsivity and reinstatement of food seeking behavior in male rats: Implications for understanding the anti-obesity property of 5-HT2C receptor agonists. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Rattus norvegicus 167-173 27931246-8 2016 Furthermore, these findings have translational relevance for individuals with PWS who may seek to control appetite with another 5-HT2CR agonist, the new obesity treatment lorcaserin. lorcaserin 171-181 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 128-135 27085605-7 2016 The 5-HT2C agonists lorcaserin and CP-809,101 dose-dependently suppressed ASs, an effect blocked by the selective 5-HT2C antagonist SB 242984. lorcaserin 20-30 5-hydroxytryptamine receptor 2C Rattus norvegicus 4-10 27085605-7 2016 The 5-HT2C agonists lorcaserin and CP-809,101 dose-dependently suppressed ASs, an effect blocked by the selective 5-HT2C antagonist SB 242984. lorcaserin 20-30 5-hydroxytryptamine receptor 2C Rattus norvegicus 114-120 27241709-1 2016 RATIONALE: The 5-HT2C receptor agonist lorcaserin (Belviq ) has been approved by the FDA for the treatment of obesity. lorcaserin 39-49 5-hydroxytryptamine receptor 2C Rattus norvegicus 15-21 27241709-1 2016 RATIONALE: The 5-HT2C receptor agonist lorcaserin (Belviq ) has been approved by the FDA for the treatment of obesity. lorcaserin 51-57 5-hydroxytryptamine receptor 2C Rattus norvegicus 15-21 27241709-5 2016 RESULTS: Lorcaserin (0.3-0.6 mg/kg SC) and CP-809101 (0.6-1 mg/kg SC) reduced premature responding in rats trained on the 5-CSRTT and improved accuracy in a Go-NoGo task by reducing false alarms. lorcaserin 9-19 reticulon 4 Rattus norvegicus 160-164 27116910-1 2016 OBJECTIVES: Lorcaserin is a selective 5-HT2C (5-hydroxytryptamine 2C) receptor agonist indicated for weight management. lorcaserin 12-22 5-hydroxytryptamine receptor 2C Homo sapiens 38-44 27206567-3 2016 The potency of lorcaserin for the 5-HT2C receptor is 14-fold greater than its potency for the 5-HT2A receptor and 61-fold greater than its potency for the 5-HT2B receptor. lorcaserin 15-25 5-hydroxytryptamine receptor 2A Homo sapiens 94-109 27206567-3 2016 The potency of lorcaserin for the 5-HT2C receptor is 14-fold greater than its potency for the 5-HT2A receptor and 61-fold greater than its potency for the 5-HT2B receptor. lorcaserin 15-25 5-hydroxytryptamine receptor 2B Homo sapiens 155-170 26384326-4 2015 The 5-HT2C receptor selective agonist 1-(3-chlorophenyl)piperazine (mCPP, 0.032-1.0 mg/kg) and lorcaserin induced yawning which was attenuated by the 5-HT2C receptor selective antagonist 6-chloro-5-methyl-N-(6-[(2-methylpyridin-3-yl)oxy]pydidin-3-yl)indoline-1-carboxamide (1.0 mg/kg). lorcaserin 95-105 5-hydroxytryptamine receptor 2C Rattus norvegicus 150-156 26375926-4 2015 The present study examined the effect of a selective 5-HT2CR agonist lorcaserin on behavioral sensitization and naloxone-precipitated withdrawal symptoms in heroin-treated mice. lorcaserin 69-79 5-hydroxytryptamine (serotonin) receptor 2C Mus musculus 53-60 26384326-7 2015 At larger doses, lorcaserin produced forepaw treading, which was attenuated by the 5-HT1A receptor selective antagonist N-(2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl)-N-(2-pyridyl)cyclohexanecarboxamide (0.178 mg/kg). lorcaserin 17-27 5-hydroxytryptamine receptor 1A Rattus norvegicus 83-89 26384326-8 2015 While the behavioral effects of lorcaserin in rats are consistent with it having agonist activity at 5-HT2C receptors, these data suggest that at larger doses it also has agonist activity at 5-HT2A and possibly 5-HT1A receptors. lorcaserin 32-42 5-hydroxytryptamine receptor 2C Rattus norvegicus 101-107 25727097-10 2015 In contrast, the specific 5-HT2C receptor agonist lorcaserin, recently approved for the treatment of obesity, attenuates ghrelin-induced food intake. lorcaserin 50-60 5-hydroxytryptamine receptor 2C Rattus norvegicus 26-32 25727097-10 2015 In contrast, the specific 5-HT2C receptor agonist lorcaserin, recently approved for the treatment of obesity, attenuates ghrelin-induced food intake. lorcaserin 50-60 ghrelin and obestatin prepropeptide Rattus norvegicus 121-128 25109272-2 2014 The purpose of this study was to evaluate the efficacy of a novel 5-HT2c receptor agonist, lorcaserin for reducing alcohol consumption in alcohol-preferring (P) rats. lorcaserin 91-101 5-hydroxytryptamine receptor 2C Rattus norvegicus 66-72 24953434-9 2014 The 5HT2C agonist lorcaserin significantly decreased nicotine self-administration in the licking paradigm at the same dose threshold as with lever press responding. lorcaserin 18-28 5-hydroxytryptamine receptor 2C Rattus norvegicus 4-9 25109272-11 2014 These results show the efficacy of lorcaserin in reducing alcohol intake without a significant effect on water intake and locomotion suggesting the involvement of 5-HT2c receptors in alcohol seeking behavior. lorcaserin 35-45 5-hydroxytryptamine receptor 2C Rattus norvegicus 163-169 24935789-4 2014 RESULTS: The 5-HT2C agonists mCPP (1 mg/kg, i.p) and lorcaserin (3 mg/kg, i.p), but not RO60-0175 (1-3 mg/kg i.p. lorcaserin 53-63 5-hydroxytryptamine receptor 2C Rattus norvegicus 13-19 24064009-5 2014 Lorcaserin, a 5HT2C agonist has moderate efficacy with an acceptable safety profile. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Homo sapiens 14-19 24935789-8 2014 CONCLUSIONS: In our animal model of TLE, mCPP and lorcaserin were anticonvulsant; likely acting on receptor subtypes other than 5-HT2C. lorcaserin 50-60 5-hydroxytryptamine receptor 2C Rattus norvegicus 128-134 24041919-1 2013 The recent US Food and Drug Administration (FDA) approval of the serotonin (5-hydroxytryptamine, 5-HT) 5-HT2C receptor agonist lorcaserin for the treatment of obesity represents a new therapeutic drug class available to the clinic. lorcaserin 127-137 5-hydroxytryptamine receptor 2C Homo sapiens 103-109 24292660-6 2013 This review provides an overview of 5-HT receptor pharmacology and discusses two recent 5-HT receptor subtype-selective drugs, lorcaserin and pimavanserin, which target the 5HT2C and 5HT2A receptors and provide new treatments for obesity and Parkinson"s disease psychosis, respectively. lorcaserin 127-137 5-hydroxytryptamine receptor 2C Homo sapiens 173-178 24273398-0 2013 Lorcaserin (Belviq): A Selective Serotonin 5-HT2C Agonist In the Treatment of Obesity. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Homo sapiens 43-49 23661689-1 2013 BACKGROUND: Lorcaserin is a selective 5-HT2C agonist evaluated for weight management in clinical trials. lorcaserin 12-22 5-hydroxytryptamine receptor 2C Homo sapiens 38-44 23800750-10 2013 Lorcaserin is a selective serotonin 5-HT2C agonist that regulates food intake, while the combination of phentermine/topiramate causes appetite suppression and enhanced satiety. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Homo sapiens 36-42 23184281-1 2013 RATIONALE: Selective 5-HT2C receptor agonists, such as lorcaserin, are being developed for the treatment of obesity. lorcaserin 55-65 5-hydroxytryptamine receptor 2C Rattus norvegicus 21-27 23184281-10 2013 Finally, there may be differences in the side effect profiles between lorcaserin and CP-809101, raising the possibility for tolerability differences amongst 5-HT2C agonists. lorcaserin 70-80 5-hydroxytryptamine receptor 2C Homo sapiens 157-163 22266842-0 2012 Identification of human cytochrome P450 and flavin-containing monooxygenase enzymes involved in the metabolism of lorcaserin, a novel selective human 5-hydroxytryptamine 2C agonist. lorcaserin 114-124 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 24-39 22259019-6 2012 With recombinant UGT enzymes, lorcaserin N-carbamoyl glucuronidation was predominantly catalyzed by three UGT2Bs (UGT2B7, UGT2B15, and UGT2B17), whereas two UGT1As (UGT1A6 and UGT1A9) played a minor role. lorcaserin 30-40 UDP glucuronosyltransferase family 2 member B7 Homo sapiens 114-120 23529825-1 2013 Oral lorcaserin (BELVIQ( )), a selective serotonin 5-HT2C receptor agonist, is indicated in the US as an adjunct to diet and exercise in the chronic weight management of obese adults, or overweight adults with at least one weight-related comorbidity (e.g. dyslipidaemia, hypertension, type 2 diabetes). lorcaserin 5-15 5-hydroxytryptamine receptor 2C Homo sapiens 41-66 23529825-1 2013 Oral lorcaserin (BELVIQ( )), a selective serotonin 5-HT2C receptor agonist, is indicated in the US as an adjunct to diet and exercise in the chronic weight management of obese adults, or overweight adults with at least one weight-related comorbidity (e.g. dyslipidaemia, hypertension, type 2 diabetes). lorcaserin 17-23 5-hydroxytryptamine receptor 2C Homo sapiens 41-66 22421927-10 2012 More patients lost >=5% body weight with lorcaserin BID (37.5%; P < 0.001) or lorcaserin QD (44.7%; P < 0.001) vs. placebo (16.1%; modified intent to treat (MITT)/last observation carried forward (LOCF)). lorcaserin 44-54 BH3 interacting domain death agonist Homo sapiens 55-58 22266842-2 2012 The oxidative metabolism of lorcaserin, mediated by recombinant human cytochrome P450 (P450) and flavin-containing monooxygenase (FMO) enzymes, was examined in vitro to identify the enzymes involved in the generation of its primary oxidative metabolites, N-hydroxylorcaserin, 7-hydroxylorcaserin, 5-hydroxylorcaserin, and 1-hydroxylorcaserin. lorcaserin 28-38 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 70-92 22259019-6 2012 With recombinant UGT enzymes, lorcaserin N-carbamoyl glucuronidation was predominantly catalyzed by three UGT2Bs (UGT2B7, UGT2B15, and UGT2B17), whereas two UGT1As (UGT1A6 and UGT1A9) played a minor role. lorcaserin 30-40 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 122-129 21795446-9 2011 RESULTS: Significantly more patients treated with lorcaserin 10 mg BID and QD lost at least 5% of baseline body weight (47.2 and 40.2%, respectively) as compared with placebo (25.0%, P < 0.001 vs. lorcaserin BID). lorcaserin 50-60 BH3 interacting domain death agonist Homo sapiens 67-70 22259019-6 2012 With recombinant UGT enzymes, lorcaserin N-carbamoyl glucuronidation was predominantly catalyzed by three UGT2Bs (UGT2B7, UGT2B15, and UGT2B17), whereas two UGT1As (UGT1A6 and UGT1A9) played a minor role. lorcaserin 30-40 UDP glucuronosyltransferase family 2 member B17 Homo sapiens 135-142 22259019-6 2012 With recombinant UGT enzymes, lorcaserin N-carbamoyl glucuronidation was predominantly catalyzed by three UGT2Bs (UGT2B7, UGT2B15, and UGT2B17), whereas two UGT1As (UGT1A6 and UGT1A9) played a minor role. lorcaserin 30-40 UDP glucuronosyltransferase family 1 member A6 Homo sapiens 165-171 22259019-6 2012 With recombinant UGT enzymes, lorcaserin N-carbamoyl glucuronidation was predominantly catalyzed by three UGT2Bs (UGT2B7, UGT2B15, and UGT2B17), whereas two UGT1As (UGT1A6 and UGT1A9) played a minor role. lorcaserin 30-40 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 176-182 22259019-8 2012 The rank order of catalytic efficiency of human UGT enzymes for lorcaserin N-carbamoyl glucuronidation was UGT2B15 > UGT2B7 > UGT2B17 > UGT1A9 > UGT1A6. lorcaserin 64-74 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 107-114 22259019-8 2012 The rank order of catalytic efficiency of human UGT enzymes for lorcaserin N-carbamoyl glucuronidation was UGT2B15 > UGT2B7 > UGT2B17 > UGT1A9 > UGT1A6. lorcaserin 64-74 UDP glucuronosyltransferase family 2 member B7 Homo sapiens 120-126 22259019-8 2012 The rank order of catalytic efficiency of human UGT enzymes for lorcaserin N-carbamoyl glucuronidation was UGT2B15 > UGT2B7 > UGT2B17 > UGT1A9 > UGT1A6. lorcaserin 64-74 UDP glucuronosyltransferase family 2 member B17 Homo sapiens 132-139 22259019-8 2012 The rank order of catalytic efficiency of human UGT enzymes for lorcaserin N-carbamoyl glucuronidation was UGT2B15 > UGT2B7 > UGT2B17 > UGT1A9 > UGT1A6. lorcaserin 64-74 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 145-151 22259019-8 2012 The rank order of catalytic efficiency of human UGT enzymes for lorcaserin N-carbamoyl glucuronidation was UGT2B15 > UGT2B7 > UGT2B17 > UGT1A9 > UGT1A6. lorcaserin 64-74 UDP glucuronosyltransferase family 1 member A6 Homo sapiens 157-163 22259019-9 2012 Inhibition of lorcaserin N-carbamoyl glucuronidation activities of UGT2B7, UGT2B15, and UGT2B17 in human liver microsomes by mefenamic acid, bisphenol A, and eugenol further substantiated the involvement of these UGT2B isoforms. lorcaserin 14-24 UDP glucuronosyltransferase family 2 member B7 Homo sapiens 67-73 22259019-9 2012 Inhibition of lorcaserin N-carbamoyl glucuronidation activities of UGT2B7, UGT2B15, and UGT2B17 in human liver microsomes by mefenamic acid, bisphenol A, and eugenol further substantiated the involvement of these UGT2B isoforms. lorcaserin 14-24 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 75-82 22259019-9 2012 Inhibition of lorcaserin N-carbamoyl glucuronidation activities of UGT2B7, UGT2B15, and UGT2B17 in human liver microsomes by mefenamic acid, bisphenol A, and eugenol further substantiated the involvement of these UGT2B isoforms. lorcaserin 14-24 UDP glucuronosyltransferase family 2 member B17 Homo sapiens 88-95 22266842-4 2012 In 16 individual human liver microsomal preparations (HLM), formation of N-hydroxylorcaserin was correlated with CYP2B6, 7-hydroxylorcaserin was correlated with CYP2D6, 5-hydroxylorcaserin was correlated with CYP1A2 and CYP3A4, and 1-hydroxylorcaserin was correlated with CYP3A4 activity at 10.0 muM lorcaserin. lorcaserin 82-92 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 113-119 22266842-10 2012 Multiple human P450 and FMO enzymes catalyze the formation of four primary oxidative metabolites of lorcaserin, suggesting that lorcaserin has a low probability of drug-drug interactions by concomitant medications. lorcaserin 100-110 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 15-27 22266842-10 2012 Multiple human P450 and FMO enzymes catalyze the formation of four primary oxidative metabolites of lorcaserin, suggesting that lorcaserin has a low probability of drug-drug interactions by concomitant medications. lorcaserin 128-138 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 15-27 22085383-7 2011 The serotonin 5-HT(2C)-receptor selective agonist lorcaserin, a drug specifically developed to target satiety without producing the side effect profiles of its predecessors, has been shown to significantly reduce energy intake and body weight. lorcaserin 50-60 5-hydroxytryptamine receptor 2C Homo sapiens 4-31 21795446-9 2011 RESULTS: Significantly more patients treated with lorcaserin 10 mg BID and QD lost at least 5% of baseline body weight (47.2 and 40.2%, respectively) as compared with placebo (25.0%, P < 0.001 vs. lorcaserin BID). lorcaserin 50-60 BH3 interacting domain death agonist Homo sapiens 211-214 21795446-10 2011 Least squares mean (95% confidence interval) weight loss with lorcaserin BID and QD was 5.8% (5.5-6.2%) and 4.7% (4.3-5.2%), respectively, compared with 2.8% (2.5-3.2%) with placebo (P < 0.001 vs. lorcaserin BID; least squares mean difference, 3.0%). lorcaserin 62-72 BH3 interacting domain death agonist Homo sapiens 73-76 21795446-10 2011 Least squares mean (95% confidence interval) weight loss with lorcaserin BID and QD was 5.8% (5.5-6.2%) and 4.7% (4.3-5.2%), respectively, compared with 2.8% (2.5-3.2%) with placebo (P < 0.001 vs. lorcaserin BID; least squares mean difference, 3.0%). lorcaserin 62-72 BH3 interacting domain death agonist Homo sapiens 211-214 21795446-11 2011 Weight loss of at least 10% was achieved by 22.6 and 17.4% of patients receiving lorcaserin 10 mg BID and QD, respectively, and 9.7% of patients in the placebo group (P < 0.001 vs. lorcaserin BID). lorcaserin 81-91 BH3 interacting domain death agonist Homo sapiens 98-101 21795446-13 2011 U.S. Food and Drug Administration-defined echocardiographic valvulopathy occurred in 2.0% of patients on placebo and 2.0% on lorcaserin 10 mg BID. lorcaserin 125-135 BH3 interacting domain death agonist Homo sapiens 142-145 19900026-0 2009 Lorcaserin and adiposopathy: 5-HT2c agonism as a treatment for "sick fat" and metabolic disease. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Homo sapiens 29-35 21636655-0 2011 Lorcaserin, a 5-HT2C agonist, decreases nicotine self-administration in female rats. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Rattus norvegicus 14-20 21181547-6 2011 A number of new preparations, including combinations of the existing drugs topiramate plus phentermine, bupropion plus naltrexone, and the selective 5-HT(2C) agonist lorcaserin have recently been filed for approval. lorcaserin 166-176 5-hydroxytryptamine receptor 2C Homo sapiens 149-156 19900026-3 2009 Lorcaserin (APD-356) is a selective 5-HT2c receptor agonist that promotes weight loss. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Homo sapiens 36-42 19900026-3 2009 Lorcaserin (APD-356) is a selective 5-HT2c receptor agonist that promotes weight loss. lorcaserin 12-19 5-hydroxytryptamine receptor 2C Homo sapiens 36-42 18252809-2 2008 In this study, we describe the in vitro and in vivo characteristics of lorcaserin [(1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3 benzazepine], a selective, high affinity 5-HT(2C) full agonist. lorcaserin 71-81 5-hydroxytryptamine receptor 2C Homo sapiens 171-178 18095642-0 2008 Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity. lorcaserin 49-107 5-hydroxytryptamine receptor 2C Rattus norvegicus 144-150 18095642-0 2008 Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity. lorcaserin 109-119 5-hydroxytryptamine receptor 2C Rattus norvegicus 144-150 18095642-2 2008 Compound 7d (lorcaserin, APD356) was identified as one of the more potent and selective compounds in vitro (pEC50 values in functional assays measuring [(3)H]phosphoinositol turnover: 5-HT2C = 8.1; 5-HT2A = 6.8; 5-HT2B = 6.1) and was potent in an acute in vivo rat food intake model upon oral administration (ED50 at 6 h = 18 mg/kg). lorcaserin 13-23 5-hydroxytryptamine receptor 2C Rattus norvegicus 184-190 18095642-2 2008 Compound 7d (lorcaserin, APD356) was identified as one of the more potent and selective compounds in vitro (pEC50 values in functional assays measuring [(3)H]phosphoinositol turnover: 5-HT2C = 8.1; 5-HT2A = 6.8; 5-HT2B = 6.1) and was potent in an acute in vivo rat food intake model upon oral administration (ED50 at 6 h = 18 mg/kg). lorcaserin 25-31 5-hydroxytryptamine receptor 2C Rattus norvegicus 184-190 18252809-3 2008 Lorcaserin bound to human and rat 5-HT(2C) receptors with high affinity (K(i) = 15 +/- 1 nM, 29 +/- 7 nM, respectively), and it was a full agonist for the human 5-HT(2C) receptor in a functional inositol phosphate accumulation assay, with 18- and 104-fold selectivity over 5-HT(2A) and 5-HT(2B) receptors, respectively. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Homo sapiens 34-41 18252809-3 2008 Lorcaserin bound to human and rat 5-HT(2C) receptors with high affinity (K(i) = 15 +/- 1 nM, 29 +/- 7 nM, respectively), and it was a full agonist for the human 5-HT(2C) receptor in a functional inositol phosphate accumulation assay, with 18- and 104-fold selectivity over 5-HT(2A) and 5-HT(2B) receptors, respectively. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Homo sapiens 161-168 18252809-4 2008 Lorcaserin was also highly selective for human 5-HT(2C) over other human 5-HT receptors (5-HT(1A), 5-HT(3), 5-HT(4C), 5-HT5(5A), 5-HT(6), and 5-HT(7)), in addition to a panel of 67 other G protein-coupled receptors and ion channels. lorcaserin 0-10 5-hydroxytryptamine receptor 2C Homo sapiens 47-54 18252809-10 2008 These data demonstrate lorcaserin to be a potent, selective, and efficacious agonist of the 5-HT(2C) receptor, with potential for the treatment of obesity. lorcaserin 23-33 5-hydroxytryptamine receptor 2C Homo sapiens 92-99