Probing the proposed phenyl-A region of the sigma-1 receptor.
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.
Ablordeppey
Seth Y
SY
College of Pharmacy and Pharmaceutical Sciences, Florida A&M University, Tallahassee, FL 32307, USA. seth.ablordeppey@famu.edu
Fischer
James B
JB
Law
Ho
H
Glennon
Richard A
RA
D000818:Animals; D006801:Humans; D015335:Molecular Probes / Q000138:chemical synthesis* / Q000378:metabolism; D010880:Piperidines / Q000138:chemical synthesis / Q000378:metabolism; D011485:Protein Binding; D011869:Radioligand Assay; D017480:Receptors, sigma / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship; D000097605:Sigma-1 Receptor
D015335:Molecular Probes; D010880:Piperidines; D017480:Receptors, sigma; D000097605:Sigma-1 Receptor; C106107:sigma-2 receptor