Stereospecific opiate binding in living human polymorphonuclear leucocytes.
Living human polymorphonuclear leucocytes were incubated with various opiate agonists and antagonists in radioreceptor assays. Binding of the opiate antagonists 3H-naloxone and 3H-diprenorphine and of the benzomorphan 3H-ethylketocyclazocine was found at 4 degrees C and at 37 degrees C, 3H-naloxone binding was stereospecific. Binding of the opiate agonist 3H-dihydromorphine was present at 37 degrees C but not at 4 degrees C and had a different time course as compared to the antagonists. At both temperatures no specific binding of the proteolytic stable analogue 3H-D-Ala-D-Leu-enkephalin was found. Autoradiography showed an unspecific accumulation of 3H-naloxone inside the cells and a specific localization of grains at the cell membrane.
Falke
N E
NE
Fischer
E G
EG
Martin
R
R
D000701:Analgesics, Opioid / Q000097:blood; D003496:Cyclazocine / Q000031:analogs & derivatives / Q000097:blood; D004174:Diprenorphine / Q000097:blood; D004743:Enkephalin, Leucine / Q000031:analogs & derivatives / Q000097:blood; D016308:Enkephalin, Leucine-2-Alanine; D016314:Ethylketocyclazocine; D006098:Granulocytes / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D009270:Naloxone / Q000097:blood; D009504:Neutrophils / Q000378:metabolism*; D011957:Receptors, Opioid / Q000378:metabolism*
D000701:Analgesics, Opioid; D011957:Receptors, Opioid; D004174:Diprenorphine; D009270:Naloxone; D016314:Ethylketocyclazocine; D004743:Enkephalin, Leucine; D016308:Enkephalin, Leucine-2-Alanine; D003496:Cyclazocine