CP-601932

CP-601932 是 α3β4 nAChR 的高亲和力部分激动剂 (Ki=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。

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5mg

￥6262.00

5010.00

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10mg

￥10575.00

8460.00

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货号: ajcx35966
CAS: 357425-68-4
别名: (1S,5R)-CP-601927
分子式: C12H12F3N
分子量: 227.23
纯度: >98%
溶解度: DMSO : 200 mg/mL (880.17 mM; Need ultrasonic)
储存: Store at -20°C
库存: 现货

Background

CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (Ki=21 nM; EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (Ki=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[1].

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[1].CP-601932 (adult male Sprague-Dawley rats) readily penetrates the CNS and at 30 min reaches maximal Cb,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[1].

[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.