CP-601932 ((1S,5R)-CP-601927) 是 α3β4 nAChR 的高亲和力部分激动剂 (K_i=21; EC₅₀=~3 μM)。CP-601932 对 α3β4 和 α4β2 nAChR 具有相同的高结合亲和力，对 α6 和 α7 nAChR 亚型亲和力降低一个数量级。CP-601932 在长期暴露后选择性地减少乙醇消耗，但不减少蔗糖消耗和操作性自我给药。CP-601932 可透过血脑屏障。

CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (K i =21?nM; EC 50 =~ 3?μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (K i =21?nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 can penetrate the CNS.

Oil

CP-601932 (10?mg/kg; s.c; adult male Sprague-Dawley rats) decreases active lever presses for 10% ethanol, but not 5% sucrose in the operant self-administration paradigm.
CP-601932 (adult male Sprague-Dawley rats) readily penetrates the CNS and at 30?min reaches maximal C b,u values of 340?nM after 5?mg/kg and 710?nM after 10?mg/kg. Brain concentrations of CP-601932 decline very slowly and levels stay relatively high, eg, 530?nM at 5?h and 85?nM at 24?h after 10?mg/kg. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Pure form -20°C 3 years；4°C 2 years

[1]. Chatterjee S, et al. Partial agonists of the α3β4* neuronal nicotinic acetylcholine receptor reduce ethanol consumption and seeking in rats. Neuropsychopharmacology. 2011;36(3):603-615.

In Vitro: DMSO : 200 mg/mL (880.17 mM; Need ultrasonic)配制储备液