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Identification Of The Binding Subunit Of The Sigma-Type Opiate Receptor By Photoaffinity Labeling With 1-(4-Azido-2-Methyl[6-3h]Phenyl)-3-(2-Methyl[4,6-3h]Phenyl)Guanidine, Michael Kavanaugh, Barbara C. Tester, Michael W. Scherz, John F. W. Keana, Eckard Weber
Identification Of The Binding Subunit Of The Sigma-Type Opiate Receptor By Photoaffinity Labeling With 1-(4-Azido-2-Methyl[6-3h]Phenyl)-3-(2-Methyl[4,6-3h]Phenyl)Guanidine, Michael Kavanaugh, Barbara C. Tester, Michael W. Scherz, John F. W. Keana, Eckard Weber
Biomedical and Pharmaceutical Sciences Faculty Publications
The sigma-type opiate receptor is a distinct binding site in the brain that may mediate some of the psychotomimetic effects caused by benzomorphan opiates and phencyclidine in humans. We have developed a synthetic, highly selective ligand for this receptor, 1,3-di-o-tolylguanidine (DTG). To identify the binding protein(s) of the sigma receptor, we have now synthesized a radiolabeled azide derivative of DTG, 1-(4-azido-2-methyl[6-3H]phenyl)-3-(2-methyl[4,6-3H]phenyl)-guanidine ([3H]N3DTG). In guinea pig brain membrane binding assays conducted in the dark, [3H]N3DTG bound reversibly, selectively, and with high affinity (Kd = 10 nM) to sigma receptors. The drug specificity profile of reversible [3H]-N3DTG binding was identical to that …