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. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Oil