Facinicline hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

FaciniclineHCl 既是一种新型烟碱 α-7 受体 (alpha7nAChR) 部分激动剂 (Ki = 6 nM)，又是 5-HT3 拮抗剂 (Ki = 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.(In Vitro):Facinicline hydrochloride exhibits antagonist properties at the serotonin 3 receptor in oocytes(IC50 = 2.8 μM) and N1E-115 cells(IC50 = 32.7 μM).Facinicline hydrochloride activates human α7 nAChRs in oocytes(EC50 = 0.8 μM) and QM7 cells(EC50 = 7.7 μM).(In Vivo):In Male Sprague-Dawley rats, Facinicline hydrochloride (0.1–10 mg/kg p.o.) selectively enhances object recognition memory. 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.

Facinicline (RG3487) activates human α7 nAChRs with an EC50 of 0.8 μM (oocytes) and 7.7 μM (QM7 cells).Facinicline (RG3487) exhibits antagonist properties at the serotonin 3 receptor (IC50 2.8 nM (oocytes), 32.7 nM (N1E-115 cells)).

Facinicline (RG3487) improves object recognition memory in rats after acute [minimally effective dose (MED) 1.0 mg/kg p.o.] or repeated (10 day) administration at brain and plasma concentrations in the low-nanomolar range. RG3487 (0.1–10 mg/kg p.o.) selectively enhances object recognition memory. Animal Model:Male Sprague-Dawley rats.Dosage:0.1-10 mg/kg (Pharmacokinetic Analysis).Administration:Orally.Result:The mean Cmax was typically observed between 0.5 and 4 h.

RG3487 hydrochloride

Endocrinology/Hormones

5-HT Receptor

Reactive Oxygen Species|Fungal

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677305-02-1

306.79

C15H19ClN4O

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (407.44 mM)

Cl.O=C(N[C@@H]1CN2CCC1CC2)c1n[nH]c2ccccc12

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(-20℃)

With Ice Pack

≥ 2 years