Design, synthesis, and structure− affinity relationships of regioisomeric N-benzyl alkyl ether piperazine derivatives as σ-1 receptor ligands

…, N Giboureau, AJ Reynolds, M Kassiou

Index: Moussa, Iman A.; Banister, Samuel D.; Beinat, Corinne; Giboureau, Nicolas; Reynolds, Aaron J.; Kassiou, Michael Journal of Medicinal Chemistry, 2010 , vol. 53, # 16 p. 6228 - 6239

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Citation Number: 41

Abstract

A series of N-(benzofuran-2-ylmethyl)-N′-benzylpiperazines bearing alkyl or fluoroalkyl aryl ethers were synthesized and evaluated at various central nervous system receptors. Examination of in vitro σ1 {[3H](+)-pentazocine} and σ2 ([3H] DTG) receptor binding profiles of piperazines 11− 13 and 25− 36 revealed several highly potent and σ1 selective ligands, notably, N-(benzofuran-2-ylmethyl)-N′-(4′-methoxybenzyl) piperazine (13, K i= 2.7 nM, ...

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