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 ...