(.+-.)-(Z)-2-(Aminomethyl)-1-phenylcyclopropanecarboxamide Derivatives as a New Prototype of NMDA Receptor Antagonists

S Shuto, H Takada, D Mochizuki, R Tsujita…

Index: Shuto; Takada; Mochizuki; Tsujita; Hase; Ono; Shibuya; Matsuda Journal of medicinal chemistry, 1995 ,  vol. 38,  # 15  p. 2964 - 2968

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Citation Number: 52

Abstract

f)-(Z)-2-(Aminomethyl)-l-phenylcyclopropane-~~-diethylcarboxamide(milnacipran, l), a clinically useful antidepressant, and its derivatives were prepared by an improved method and were evaluated as NMDA receptor antagonists. Of these, milnacipran (l), its N-methyl and NJV-dimethyl derivatives, 7 and 8, respectively, and its homologue 12 at the aminomethyl moiety had binding affinity for the receptor in vitro (I&: 1, 6.3 f 0.3 pM; 7, 13 f ...