Vabicaserin hydrochloride 是一种选择性的 5-羟色胺2C (5-HT_2C) 受体激动剂，EC₅₀ 为 8 nM。

Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT 2C ) receptor-selective agonist with an EC 50 of 8 nM.

Solid

5-HT2C Receptor 8 nM (EC50)

Vabicaserin displaces I-(2,5-dimethoxy)phenylisopropylamine binding from human 5-HT2C receptor sites in Chinese hamster ovary cell membranes with a Ki value of 3 nM and is >50-fold selective over a number of serotonergic, noradrenergic, and dopaminergic receptors. Binding affinity determined for the human 5-HT2B receptor subtype using [H]5HT is 14 nM. Vabicaserin is a potent and full agonist (EC50, 8 nM; Emax, 100%) in stimulating 5-HT2C receptor-coupled calcium mobilization and exhibits 5-HT2A receptor antagonism and 5-HT2B antagonist or partial agonist activity in transfected cells, depending on the level of receptor expression. Vabicaserin exhibits lower affinity at the 5-HT2C antagonist binding site (22 nM) labeled with [H]mesulergine. Additional binding studies indicate t

After a single oral dose of [C]Vabicaserin at 50, 5, and 15 mg/kg, unchanged drug represents less than 19, 20, and 35% of total plasma radioactivity at all the time points examined in mice, rats, and dogs, respectively. The carbamoyl glucuronide (CG) represents approximately 7 to 36% of plasma radioactivity in mice and 2 to 28% of plasma radioactivity in dogs but is not detected in rat plasma after the single [C]Vabicaserin dose. However, the CG is observed in rat plasma after multiple-dose administration of Vabicaserin at higher doses, and the CG is approximately 20 times less than Vabicaserin based on steady-state AUC 0-24 values. The estimated plasma AUC 0-24 ratios of CG to the parent drug are 1.5 and 1.7 in mice and dogs after the single [C]Vabicaserin dose, respectively. The plasma AUC 0-24 ratios for the CG to Vabicaserin at steady state wi

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Dunlop J, et al. Characterization of Vabicaserin (SCA-136), a selective 5-hydroxytryptamine 2C receptor agonist. J Pharmacol Exp Ther. 2011 Jun;337(3):673-80.
[2]. Tong Z, et al. Species differences in the formation of Vabicaserin carbamoyl glucuronide. Drug Metab Dispos. 2010 Apr;38(4):581-90.

In Vitro: DMSO : 60 mg/mL (226.59 mM; ultrasonic and warming and heat to 80°C)H₂O : 4 mg/mL (15.11 mM; Need ultrasonic)配制储备液