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
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CP-601932
CAS number:357425-68-4 molecular formula:C12H12F3N
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| Chinese alias | - | ||
| English alias | SCHEMBL5911646 | MS-23286 | 8EQZ26LUCA | RNOBTWYQAWEZHH-SFYZADRCSA-N | 1,5-Methano-1H-3-benzazepine, 2,3,4,5-tetrahydro-7-(trifluoromethyl)-, (1S,5R)-(-)- | CP-601932 | 1,5-Methano-1H-3-benzazepine, 2,3,4,5-tetrahydro-7-(trifluoromethyl)-, (1S,5R)- | Q272 | ||
| CAS number | 357425-68-4 | molecular formula | C12H12F3N |
| molecular weight | 227.23 g/mol | Exact mass | ≥99% |
| PSA | 12.000 Ų | logp | 2.400 |
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