Effect of N-alkylation on the affinities of analogs of spiperone for dopamine D2 and serotonin 5-HT2 receptors

…, KJ Ivins, PB Molinoff, RL Ehrenkaufer

文献索引：Mach; Jackson; Luedtke; Ivins; Molinoff; Ehrenkaufer Journal of Medicinal Chemistry, 1992 , vol. 35, # 3 p. 423 - 430

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被引用次数: 25

摘要

Two series of N-substituted spiperone analogues were prepared and evaluated in vitro to measure their affinities for dopamine D2 and serotonin 5-HTz receptors. Substitution of the amide nitrogen with an alkyl group of five carbon units or less resulted in analogues displaying a low selectivity for D2 compared to 5-HT2 receptors. However, a moderate improvement in selectivity for D2 receptors was observed with N-benzylspiperone. ...