Facinicline hydrochloride 是一种口服有效的烟碱α7 receptor部分激动剂，对人nAChR 的Ki值为 6 nM。它可改善啮齿类动物的认知和感觉运动门控。它与5-HT3受体结合的Ki为 1.2 nM。

Facinicline hydrochloride is both a novel nicotinic alpha-7 receptor (alpha7nAChR) partial agonist (Ki = 6 nM) and an antagonist of 5-HT3(Ki = 1.2 nM). Facinicline hydrochloride improves cognition and sensorimotor gating in rodents.

Facinicline hydrochloride exhibits antagonist properties at the serotonin 3 receptor in oocytes(IC50 = 2.8 μM) and N1E-115 cells(IC50 = 32.7 μM)[2].Facinicline hydrochloride activates human α7 nAChRs in oocytes(EC50 = 0.8 μM) and QM7 cells(EC50 = 7.7 μM)[2].

In Male Sprague-Dawley rats, Facinicline hydrochloride (0.1–10 mg/kg p.o.) selectively enhances object recognition memory[1]. Facinicline hydrochloride improves object recognition memory in rats after acute(1.0 mg/kg p.o.) or repeated (10 day) administration at brain and plasma concentrations in the low-nanomolar range[2].

677305-02-1

C15H19ClN4O

306.79

RG3487;Facinicline hydrochloride

H2O:100 mg/mL (325.96 mM)
DMSO:125 mg/mL (407.44 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years