Synthesis and transporter binding properties of bridged piperazine analogues of 1-{2-[bis (4-fluorophenyl) methoxy] ethyl}-4-(3-phenylpropyl) piperazine (GBR 12909)

…, CM Dersch, BR de Costa, AE Jacobson…

Index: Zhang; Rothman; Dersch; De Costa; Jacobson; Rice Journal of Medicinal Chemistry, 2000 , vol. 43, # 25 p. 4840 - 4849

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Citation Number: 39

Abstract

A series of analogues related to 1-[2-(diphenylmethoxy) ethyl]-4-(3-phenylpropyl) piperazine (2) and 1-{2-[bis (4-fluorophenyl) methoxy] ethyl}-4-(3-phenylpropyl) piperazine (3)(GBR 12935 and GBR 12909, respectively), in which the piperazine moiety was replaced by bridged piperazines for structural rigidity, has been designed, synthesized, and evaluated for their ability to bind to the dopamine transporter (DAT) and to inhibit the uptake of 3H- ...

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