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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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