Belviq (Lorcaserin): A 5-HT2C receptor agonist indicated to treat certain overweight or obese adultsNew molecular entity: FDA approved Lorcaserin (Belviq, Arena Pharmaceuticals GMBH), as an adjunct to a reduced-calorie diet and increased physical activity for chronic weight management in adults with...
参考文献: [1]. Wood MD, et al. SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety. Neuropharmacology. 2001 Aug;41(2):186-99. 品牌介绍: • MCE (MedChemExpress) 拥有200 多种全球独家化合物库,我们致力于为全球科...
5HT2C receptor agonistPyrazinobenoxazinoneAnorecticObesitySubstituted 2,3,4,4a-tetrahydropyrazino[2,1-c][1,4]benzoxazin-5-(1H)-ones were synthesized and evaluated as 5-HT(2C) receptor agonists for the possible treatment of obesity. A number of compounds exhibited 5-HT(2C) agonist binding ...
Zhang B, Zhao S, Yang D, Wu Y, Xin Y, Cao H, Huang XP, Cai X, Sun W, Ye N, Xu Y, Peng Y, Zhao S, Liu ZJ, Zhong G, Wang MW, Shui W. A Novel G Protein-Biased and Subtype-Selective Agonist for a G Protein-Coupled Receptor Discovered from Screening Herbal Extracts. ACS C...
Many high-affinity 5-HT2Creceptor agonistslack selectivity: for example, MK 212 and Ro 60-0175. More selective agonists are CP809191, WAY 163909, Org 12962, VER-3323, YM 348, or PNU 22394 (a partial agonist).Lorcaserin, anagonist, is on the market for obesity, and in clinical development...
The 5-HT2C receptor agonist, lorcaserin, and the 5-HT6 receptor antagonist, SB- -742457, promote satiety; a microstructural analysis of feeding behaviour. Psychopharmacology 233: 417–424. Hill AJ, Blundell JE (1990). Sensitivity of the appetite control system in obese subjects to nutritional ...
ABCD codes for the VSV variant of the 5-HT2CR, and has been shown to exhibit reductions in receptor signaling both in agonist-elicited and intrinsic activity [16, 31]. The major isoform ABD codes for the variant VNV together with the AD isoform, which was slightly increased in SERT -/...
[4]. Jaime M Monti, et al. Effects of the serotonin 5-HT2A/2C receptor agonist DOI and of the selective 5-HT2A or 5-HT2C receptor antagonists EMD 281014 and SB-243213, respectively, on sleep and waking in the rat. Eur J Pharmacol. 2006 Dec 28;553(1-3):163-70. ...
WO2005019179A2 2005-03-03 BENZAZEPINE DERIVATIVES USEFUL FOR THE TREATMENT OF 5HT2C RECEPTOR ASSOCIATED DISEASES WO2005019180A1 2005-03-03 6-(2,2,2-TRIFLUOROETHYLAMINO)-7-CHLORO-2,3,4,5-TETRAHYDRO-1H-BENZO[d]AZEPINE AS A 5-HT2c RECEPTOR AGONIST WO2005042490A1 2005-05-12 BENZAZEPINE DERIVA...
Specifically, the 5-HT2C receptor has been indicated to be involved in cancer progression and immune response (Herr et al., 2017; Karmakar and Lal, 2021). Indeed, lorcaserin (Belviq), a selective 5-HT2C receptor agonist used as an anti-obesity drug, was withdrawn from the market in 2020,...