Description
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 ( K i =11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR.In VivoIspronicline (10-20 mg/kg; s.c.) induces c-Fos expression in selective regions of the rat forebrain. \nIspronicline pharmacokinetics (half-life of 2 h in rats) contrasts with the long-lasting improvement of working memory (18 h to 2 d). MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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).Form:Liquid