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1: Bioorg Med Chem. 2002 Aug;10(8):2759-65.Click here to read Links

Probing the proposed phenyl-A region of the sigma-1 receptor.

Ablordeppey SY, Fischer JB, Law H, Glennon RA.

College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL 32307, USA. seth.ablordeppey@famu.edu

The proposed phenyl-A region of sigma (sigma) receptors accommodates several structural features. In this study we explored the possibility that appropriate structural features located at the phenyl-A region of sigma receptor sites could lead to more potent and selective agents for the sigma receptor subtypes. By keeping the phenyl-B substituent as the optimum omega-phenylpentyl moiety, and varying substituents in the phenyl-A region, we have observed changes in binding potency and selectivity at the sigma receptor subtypes. SAR for the binding of these compounds at sigma-2 sites was also examined.

PMID: 12057665 [PubMed - indexed for MEDLINE]