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Literature DB >> 17854799

WAY-100635 has high selectivity for serotonin 5-HT(1A) versus dopamine D(4) receptors.

Jean-Claude Martel¹, Nathalie Leduc, Anne-Marie Ormière, Valérie Faucillon, Nathalie Danty, Charlène Culie, Didier Cussac, Adrian Newman-Tancredi.

Abstract

The serotonin 5-HT(1A) receptor antagonist WAY-100635 was recently reported to have potent agonist properties at dopamine D(4) receptors (Chemel et al., 2006, Psychopharmacology 188, 244-251.). Herein WAY-100635 (pK(i) at human (h) serotonin 5-HT(1A) receptors=9.51; pK(i) at dopamine hD(4.4) receptors=7.42) stimulated [(35)S]GTPgammaS incorporation in membranes of Chinese Hamster Ovary cells expressing dopamine hD(4.4) receptors with only moderate potency and modest efficacy (pEC(50)=6.63; E(max)=19% of dopamine). Moreover, in antagonism experiments, WAY-100635 had a much lower potency at dopamine hD(4.4) receptors (pK(B)=7.09), than at serotonin h5-HT(1A) receptors (pK(B)=9.47). These data demonstrate that WAY-100635 has high selectivity for serotonin h5-HT(1A)versus dopamine hD(4.4) receptors.

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Year: 2007 PMID： 17854799 DOI： 10.1016/j.ejphar.2007.07.015

Source DB: PubMed Journal: Eur J Pharmacol ISSN： 0014-2999 Impact factor: 4.432

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