WAY-100635对5-羟色胺5-HT(1A)受体的选择性高于对多巴胺D(4)受体的选择性。
WAY-100635 has high selectivity for serotonin 5-HT(1A) versus dopamine D(4) receptors.
作者信息
Martel Jean-Claude, Leduc Nathalie, Ormière Anne-Marie, Faucillon Valérie, Danty Nathalie, Culie Charlène, Cussac Didier, Newman-Tancredi Adrian
机构信息
Division of Neurobiology 2 Centre de recherche Pierre Fabre, 17 avenue Jean Moulin, 81106 Castres cedex, France.
出版信息
Eur J Pharmacol. 2007 Nov 21;574(1):15-9. doi: 10.1016/j.ejphar.2007.07.015. Epub 2007 Jul 13.
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.
血清素5-HT(1A)受体拮抗剂WAY-100635最近被报道在多巴胺D(4)受体上具有强效激动剂特性（Chemel等人，2006年，《精神药理学》188卷，244 - 251页）。在此，WAY-100635（对人（h）血清素5-HT(1A)受体的pK(i)=9.51；对多巴胺hD(4.4)受体的pK(i)=7.42）刺激表达多巴胺hD(4.4)受体的中国仓鼠卵巢细胞的膜中[(35)S]GTPγS的掺入，其效力中等且效能适度（pEC(50)=6.63；E(max)=多巴胺的19%）。此外，在拮抗实验中，WAY-100635在多巴胺hD(4.4)受体上的效力（pK(B)=7.09）远低于在血清素h5-HT(1A)受体上的效力（pK(B)=9.47）。这些数据表明WAY-100635对血清素h5-HT(1A)受体相对于多巴胺hD(4.4)受体具有高选择性。
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