Initial characterization and autoradiographic localization of a novel sigma/opioid binding site in immune tissues

• Published in: Journal of neuroimmunology 1996-07, Vol.67 (2), p.83-96
• Main Authors: Whitlock, Ben B., Liu, Yuhong, Chang, Susie, Saini, Priya, Ha, Byeong Keun, Barrett, thomas W., Wolfe, Seth A.
• Format: Article
• Language: English
• Subjects: 3-PPP; Animals; Anticonvulsants - metabolism; Anticonvulsants - pharmacology; Autoradiography; Binding Sites - immunology; Binding, Competitive; Brain Chemistry - immunology; Cytochrome P-450 Enzyme System - metabolism; Cytochrome P-450 Enzyme System - pharmacology; Dopamine; Dopamine Agonists - metabolism; Dopamine Agonists - pharmacology; Dopamine Antagonists - metabolism; Dopamine Antagonists - pharmacology; Female; Guanidines - metabolism; Guanidines - pharmacology; Haloperidol - metabolism; Haloperidol - pharmacology; Human; Hydrogen-Ion Concentration; Immune; Kinetics; Leukocyte; Leukocytes - chemistry; Leukocytes - immunology; Monoamine Oxidase - metabolism; Monoamine Oxidase - pharmacology; Naltrexone; Naltrexone - metabolism; Naltrexone - pharmacology; Narcotic Antagonists - metabolism; Narcotic Antagonists - pharmacology; Narcotics - immunology; Narcotics - metabolism; Opioid; Pentazocine; Piperidines - metabolism; Piperidines - pharmacology; Radioligand Assay; Rat; Rats; Rats, Sprague-Dawley; Receptor; Receptors, N-Methyl-D-Aspartate - immunology; Receptors, N-Methyl-D-Aspartate - metabolism; Receptors, sigma - immunology; Receptors, sigma - metabolism; Sigma; Spleen; Spleen - chemistry; Spleen - cytology; Spleen - immunology; Tritium - metabolism
• ISSN: 0165-5728; 1872-8421
• DOI: 10.1016/0165-5728(96)00041-0

High concentrations of novel, haloperidol-and DTG-inaccessible ( + )-[ 3 H]-3-PPP binding sites were found in human peripheral blood leukocytes, rat spleen and splenocytes, but not in rat brain. Splenic sites were localized in a coarse punctate pattern in the marginal zones and red pulp. The pharmacology of the splenic sites was: (-)-SKF 10,047 ≥naltrexone = (-)-pentazocine > (+)-pentazocine = (-)-3-PPP = ( + )-SKF 10,047 > ( + )-3-PPP > dextrorphan > dextromethorphan > PCP > clorgyline. DIG, haloperidol, TCP, ( - )-deprenyl and SKF 525-A did not compete. Binding activity was destroyed by heating and phospholipase C, but not by proteases or glycosidases. These sites may be involved in immunomodulation by opiate and sigma receptor agonists.