Lorcaserin is an orally active, potent and selective 5-hydroxytryptamine receptor (5-HT2C) agonist (human/rat Ki = 15 /29 nM) with 18- and 104-fold higher potency than 5-HT2A and 5-HT2B by cellular inositol phosphate accumulation assay (EC50 = 9, 168, 943 nM, respectively) and good selectivity over 5-HT1A/3/4C/5A/6/7 and a panel of 67 other GPCRs and ion channels. Chronic daily treatment to rats (4.5-18 mg/kg p.o. b.i.d.) maintained on a high fat diet causes reductions in food intake and body weight gain.
Orally active, potent and selective 5-hydroxytryptamine receptor (5-HT2C) agonist in vitro and in vivo.
Drug and alcohol dependence, 227, 108991-108991 (2021-09-06)
The opioid epidemic continues despite the availability of medications, including buprenorphine, for opioid use disorder (OUD); identifying novel and effective treatments is critical for decreasing the prevalence of OUD and ending this crisis. Buprenorphine alone does not markedly attenuate abuse-related
The Journal of neuroscience : the official journal of the Society for Neuroscience, 41(26), 5734-5746 (2021-05-26)
Obesity is a serious global health problem because of its increasing prevalence and comorbidities, but its treatments are limited. The serotonin 2C receptor (5-HT2CR), a G-protein-coupled receptor, activates proopiomelanocortin (POMC) neurons in the arcuate nucleus of hypothalamus (ARH) to reduce
The Journal of pharmacology and experimental therapeutics, 325(2), 577-587 (2008-02-07)
5-Hydroxytryptamine (5-HT)(2C) receptor agonists hold promise for the treatment of obesity. 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 bound to human and rat
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. Here, we tested whether lorcaserin (1, 3, 5.6, 10 mg/kg) is prophylactic against audiogenic
The serotonin (5-HT) system has been implicated in the pathophysiology of alcohol (ethanol; EtOH) use disorders. Lorcaserin, a 5-HT2C receptor agonist, attenuates drug self-administration in animal models. We investigated the effects of lorcaserin on EtOH intake using the drinking-in-the-dark (DID)
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