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.
体内研究
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).
分子式
C14H22N2O
分子量
234.34
CAS号
252870-53-4
运输条件
Room temperature in continental US; may vary elsewhere.