Opiate receptor binding and analgesic effects of the tetrahydroisoquinolines salsolinol and tetrahydropapaveroline.
Salosolinol and tetrahydropapaveroline bind to opiate receptors in rat brain with affinities of 6.2 and 1.95 x 10(-5)M respectively. Their ability to displace 3H-naloxone is decreased about 4-fold by 100 mM sodium ion. Both of these agents have antinociceptive effects when given to rats intraventricularly. Their potency is comparable to the enkephalins, and their effect is blocked by naloxone.
D000700:Analgesics; D000818:Animals; D007546:Isoquinolines / Q000494:pharmacology*; D008297:Male; D009270:Naloxone / Q000494:pharmacology; D010208:Papaverine / Q000031:analogs & derivatives*; D051381:Rats; D011930:Reaction Time / Q000187:drug effects; D011957:Receptors, Opioid / Q000378:metabolism*; D012490:Salsoline Alkaloids / Q000378:metabolism / Q000494:pharmacology*; D013765:Tetrahydropapaveroline / Q000378:metabolism / Q000494:pharmacology*; D013997:Time Factors
D000700:Analgesics; D007546:Isoquinolines; D011957:Receptors, Opioid; D012490:Salsoline Alkaloids; D009270:Naloxone; D013765:Tetrahydropapaveroline; D010208:Papaverine