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ID: ALA1135051

Journal: Bioorg Med Chem Lett

Title: N-arylalkylpiperidines as high-affinity sigma-1 and sigma-2 receptor ligands: phenylpropylamines as potential leads for selective sigma-2 agents.

Authors: Maeda DY, Williams W, Kim WE, Thatcher LN, Bowen WD, Coop A.

Abstract: To delineate the differences between the structural requirements necessary for recognition at sigma-1 and sigma-2 receptors, a range of phenethyl- and phenylpropylpiperidines were evaluated in binding assays. Phenethylpiperidines were found to favor sigma-1 receptors, whereas phenylpropylpiperidines tend to favor sigma-2 receptors. It appears that phenylpropylamine is a potential pharmacophore for selective sigma-2 ligands.

CiteXplore: 11814827

DOI: 10.1016/s0960-894x(01)00788-0