6-(4-Benzylpiperazin-1-yl) benzodioxanes as selective ligands at cloned primate dopamine D 4 receptors

KJ Hodgetts, A Kieltyka, R Brodbeck, JN Tran…

Index: Hodgetts; Kieltyka; Brodbeck; Tran; Wasley; Thurkauf Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 12 p. 3207 - 3213

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Citation Number: 17

Abstract

A series of novel 6-(4-benzylpiperazin-1-yl) benzodioxanes were prepared and screened at selected dopamine receptor subtypes. 6-(4-[4-Chlorobenzyl] piperazin-1-yl) benzodioxane (2d) had high affinity and selectivity for the D4 dopamine receptor subtype and was identified as a D4 antagonist via its attenuation of dopamine-induced GTPγ35S binding at the D4 receptor.