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N-{[1-(2-Phenylethyl)pyrrolidin-2-yl]methyl}cyclohexane-carboxamides as selective 5-HT1A receptor agonists

2000; Elsevier BV; Volume: 10; Issue: 5 Linguagem: Inglês

10.1016/s0960-894x(00)00030-5

1464-3405

Masakazu Fujio, Yoshifumi Togo, Hideo Tomozane, Takanobu Kuroita, Yasunori Morio, Jiro Katayama, Yasuhiro Matsumoto,

Advanced Synthetic Organic Chemistry

A series of benzamides was synthesized as selective agonists for the 5-HT1A receptor. It was found that (S)-N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]cyclohexanecarb oxamide(7-(S)) has potent and selective agonistic activity for the 5-HT1A receptor (5-HT1A; Ki 0.49 nmol/L, D2; IC50 = >1000 nmol/L, 5-HT2; Ki = 240 nmol/L).