A dopamine D4 receptor agonist
CP 226,269 is a dopamine D4 receptor agonist.1 It induces calcium flux in HEK293 cells co-expressing human dopamine D4, but not D2L or D3, receptors and Gαqo5 (EC50s = 32, >10,000, and 985 nM, respectively). CP 226,269 induces phospholipid methylation in SK-N-MC neuroblastoma cells, which endogenously express dopamine D1 and D4 receptors (EC50 = 2.9 nM).2
1.Moreland, R.B., Nakane, M., Donnelly-Roberts, D., et al.Comparative pharmacology of human dopamine D2-like receptor stable cell lines coupled to calcium flux through Gqo5Biochem. Pharmacol.68(4)761-772(2004) 2.Sharma, A., Kramer, M.L., Wick, P.F., et al.D4 dopamine receptor-mediated phospholipid methylation and its implications for mental illnesses such as schizophreniaMol. Psychiatry4(3)235-246(1999)
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