Probing the proposed phenyl-A region of the sigma-1 receptor Original Research Article

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