Ispronicline

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

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。

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.

——

Ispronicline (10-20 mg/kg; s.c.) induces c-Fos expression in selective regions of the rat forebrain. Ispronicline pharmacokinetics (half-life of 2 h in rats) contrasts with the long-lasting improvement of working memory (18 h to 2 d).Animal Model:Male Wistar rats weighting 180-200 g Dosage:10 and 30 mg/kg Administration:s.c. Result:Induced c-Fos in medial paraventricular nucleus of hypothalamus. Treatment with 30 mg/kg ispronicline, but not 10 mg/kg, increased the number of c-Fos immunoreactive cells significantly as compared to controls within the medial parvocellular part of paraventricular nucleus (PVN).

——

Cell Cycle/DNA Damage

AChR

AChR

——

——

252870-53-4

234.34

C14H22N2O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (426.73 mM; 超声助溶 )

CN[C@@H](C)C\C=C\c1cncc(OC(C)C)c1

——

(-20℃)

With Ice Pack

≥ 2 years