Volume 31, Issue 16
Heterocyclic Compounds
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ChemInform Abstract: Novel 3-Aminomethyl- and 4-Aminopiperidine Analogues of 1-[2-(Diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: Synthesis and Evaluation as Dopamine Transporter Ligands.

Sung-Woon Choi

Sung-Woon Choi

Dep. Radiol., Mass. Gen. Hosp., Boston, MA 02114, USA

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David R. Elmaleh

David R. Elmaleh

Dep. Radiol., Mass. Gen. Hosp., Boston, MA 02114, USA

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Robert N. Hanson

Robert N. Hanson

Dep. Radiol., Mass. Gen. Hosp., Boston, MA 02114, USA

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Alan J. Fischman

Alan J. Fischman

Dep. Radiol., Mass. Gen. Hosp., Boston, MA 02114, USA

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First published: 09 June 2010
Citations: 1

Abstract

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ChemInform Abstract

Investigation of a series of title compounds, e.g. (I)—(IV), concerning their substituent effects on cocaine binding and neurotransmitter reuptake, shows that although compound (Ib) exhibits the highest ratio of dopamine reuptake inhibition to binding it does not demonstrate cocaine antagonist effects in vitro. Compound (Ib) is selected for further evaluation, but additional modifications are necessary for development as cocaine antagonist.

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