Synthesis and structure–affinity relationship investigations of 5-aminomethyl and 5-carbamoyl analogues of the antipsychotic sertindole. A new class of selective α 1 …

…, MT Ramirez, KK Søby, T Liljefors, K Andersen

文献索引：Balle, Thomas; Perregaard, Jens; Larsen, Anna K.; Ramirez, Martha Teresa; Soby, Karina Krojer; Liljefors, Tommy; Andersen, Kim Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 6 p. 1065 - 1078

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被引用次数: 17

摘要

A new class of selective α1 adrenoceptor antagonists derived from the antipsychotic drug sertindole is described. The most potent and selective compound 1-(2-{4-[5-aminomethyl-1- (4-fluorophenyl)-1H-indol-3-yl]-1-piperidinyl} ethyl)-2-imidazolidinone (11) binds with 0.50 nM affinity for α1 adrenergic receptors and with more than 44 times lower affinity for dopamine D2, D3, D4 and serotonin 5-HT1A, 5-HT1B, 5-HT2A and 5-HT2C receptors. The ...