产品
编 号:F334958
分子式:C12H12F3N
分子量:227.23
产品类型
结构图
CAS No: 357425-68-4
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产品详情
生物活性:
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.
体内研究:
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 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.