| Chemical Properties | Back Directory | [Boiling point ]
272.1±35.0 °C(Predicted) | [density ]
1.246±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 200 mg/mL (880.17 mM; Need ultrasonic) | [form ]
Oil | [pka]
9.95±0.20(Predicted) | [color ]
Light yellow to light brown |
| Hazard Information | Back Directory | [Uses]
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]. | [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[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]. | [References]
[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. DOI:10.1038/npp.2010.191 |
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