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CP-601932
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CP-601932图片
CAS NO:357425-68-4
包装与价格:
包装价格(元)
5mg询价
10mg询价

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。
Cas No.357425-68-4
别名(1S,5R)-CP-601927
分子式C12H12F3N
分子量227.23
溶解度DMSO : 200 mg/mL (880.17 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.

 
 
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