Ispronicline (TC-1734) 是一种有效的，具有口服活性的大脑选择性的 α4β2 nAChR 部分激动剂，具有增强记忆的特性和良好的耐受性。Ispronicline 高亲和力与 α4β2 nAChR 结合，Ki= 11 nM。
货号:ajcx35898
CAS:252870-53-4
分子式:C14H22N2O
分子量：234.34
溶解度:DMSO : 100 mg/mL (426.73 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存： 现货

Background:

Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR[1][2].

Ispronicline (10-20 mg/kg; s.c.) induces c-Fos expression in selective regions of the rat forebrain[1]. Ispronicline pharmacokinetics (half-life of 2 h in rats) contrasts with the long-lasting improvement of working memory (18 h to 2 d)[2].

[1]. Julie Jacobsen, et al. The α4β2 nicotine acetylcholine receptor agonist ispronicline induces c-Fos expression in selective regions of the rat forebrain. Neurosci Lett. 2012 Apr 25;515(1):7-11.