"目录号: HY-15368
GPCR/G ProteinNeuronal Signaling-
Lorcaserin Hydrochloride 是一种具有选择性的人5-HT2C的完全激动剂，Ki值为 15 nM。
5-HT Receptor
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生物活性
Description
Lorcaserin (Hydrochloride) is a selective full agonist of human5-HT2Creceptor withKiof 15 nM.
IC50& Target
Ki: 15 nM (5-HT2C)
In Vitro
Lorcaserin is 18-fold more potent at human 5-HT2C(EC50= 9 nM) than at human 5-HT2A?(EC50= 168 nM), and it is 104-fold more potent at human 5-HT2C?than human 5-HT2B(EC50= 943 nM)[1].
In Vivo
Lorcaserin decreases cumulative food intake at 2, 4, 6, and 22 h with a significant decrease continuing throughout the 22-h duration of the study at the highest dose (24 mg/kg) only. The reduction in food intake induced by lorcaserin (18 mg/kg, p.o.) is mediated by 5-HT2Cand not 5-HT2Areceptors. Lorcaserin significantly reduces active, and increased inactive counts, and increases the incidence of penile grooming, an effect mediated by the 5-HT2Creceptor[1]. Lorcaserin (20 mg/kg) doses causes a significant linear dose-related reduction in responses on the active lever but has no significant effect on the response to the inactive lever. Lorcaserin (0.3125, 0.625, 1.25, and 2.5 mg/kg) also produces a significant reduction in nicotine self-administration[2].
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Cocaine-Related Disorders-Opioid-Related Disorders
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References
[1].Thomsen WJ, et al. Lorcaserin, a novel selective human 5-hydroxytryptamine2C agonist: in vitro and in vivo pharmacological characterization. J Pharmacol Exp Ther. 2008 May;325(2):577-87.
[2].Levin ED, et al. Lorcaserin, a 5-HT2C agonist, decreases nicotine self-administration in female rats. J Pharmacol Exp Ther. 2011 Sep;338(3):890-6.
[3].Lord CC, et al. The atypical antipsychotic olanzapine causes weight gain by targeting serotonin receptor 2C. J Clin Invest. 2017 Sep 1;127(9):3402-3406.