Initial characterization and autoradiographic localization of a novel sigma/opioid binding site in immune tissues.
High concentrations of novel, haloperidol- and DTG-inaccessible (+)-[3H]-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 course punctate pattern in the marginal zones and red pulp. The pharmacology of the splenic sites was: (-)-SKF 10,047 > or = naltrexone = (-)-pentazocine > (+)-pentazocine = (-)-3-PPP = (+)-SKF 10,047 > or = (+)-3-PPP > or = dextrorphan > dextromethorphan > PCP > clorgyline. DTG, haloperidol, TCP, (-)-deprenyl and SKF 525-A did not complete. 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.
Whitlock
B B
BB
Department of Medical Microbiology and Immunology, Ohio State University College of Medicine, Columbus 43210, USA.
Liu
Y
Y
Chang
S
S
Saini
P
P
Ha
B K
BK
Barrett
T W
TW
Wolfe
S A
SA
D000818:Animals; D000927:Anticonvulsants / Q000378:metabolism / Q000494:pharmacology; D001345:Autoradiography; D001665:Binding Sites / Q000276:immunology; D001667:Binding, Competitive; D001923:Brain Chemistry / Q000276:immunology; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism / Q000494:pharmacology; D018491:Dopamine Agonists / Q000378:metabolism / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000378:metabolism / Q000494:pharmacology; D005260:Female; D006146:Guanidines / Q000378:metabolism / Q000494:pharmacology; D006220:Haloperidol / Q000378:metabolism / Q000494:pharmacology; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D007962:Leukocytes / Q000737:chemistry* / Q000276:immunology*; D008995:Monoamine Oxidase / Q000378:metabolism / Q000494:pharmacology; D009271:Naltrexone / Q000378:metabolism / Q000494:pharmacology; D009292:Narcotic Antagonists / Q000378:metabolism / Q000494:pharmacology; D009294:Narcotics / Q000276:immunology / Q000378:metabolism; D010880:Piperidines / Q000378:metabolism / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D017207:Rats, Sprague-Dawley; D016194:Receptors, N-Methyl-D-Aspartate / Q000276:immunology / Q000378:metabolism; D017480:Receptors, sigma / Q000276:immunology / Q000378:metabolism*; D013154:Spleen / Q000737:chemistry / Q000166:cytology / Q000276:immunology; D014316:Tritium / Q000378:metabolism
D000927:Anticonvulsants; D018491:Dopamine Agonists; D018492:Dopamine Antagonists; D006146:Guanidines; D009292:Narcotic Antagonists; D009294:Narcotics; D010880:Piperidines; D016194:Receptors, N-Methyl-D-Aspartate; D017480:Receptors, sigma; D014316:Tritium; D009271:Naltrexone; D003577:Cytochrome P-450 Enzyme System; C026539:preclamol; D008995:Monoamine Oxidase; D006220:Haloperidol; C050232:1,3-ditolylguanidine