[Interaction of simple tetrahydroisoquinolines with opiate and high-affinity dopamine (D3) receptors in the rat corpus striatum].
The pharmacological activities of salsolinol (Sal) and salsoline (San) were compared by their abilities to displace 3H-dopamine and 3H-D-ala2-met-enkephalinamide from specific binding sites of rat striatal membrane preparations. Sal was more potent in receptor tests than San. Consequently, methylation by using catechol-O-methyltransferase is the process of its partial inactivation. Sal affinity for D3-receptors was higher than for opiate receptors (IC50 was 1.1 mumol/l for the former and 88 mumol/l for the latter). It was concluded that dopamine-like mechanisms of action of simple tetrahydroisoquinolines are possible to exist.
Patsenko
A A
AA
Grinevich
V P
VP
Ostrovskiĭ
Iu M
IuM
D000818:Animals; D003342:Corpus Striatum / Q000187:drug effects* / Q000378:metabolism; D004298:Dopamine / Q000378:metabolism; D004347:Drug Interactions; D004744:Enkephalin, Methionine / Q000031:analogs & derivatives / Q000378:metabolism; D007546:Isoquinolines / Q000493:pharmacokinetics / Q000494:pharmacology*; D008024:Ligands; D008297:Male; D051381:Rats; D011954:Receptors, Dopamine / Q000187:drug effects* / Q000378:metabolism; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; D011957:Receptors, Opioid / Q000187:drug effects* / Q000378:metabolism; D012490:Salsoline Alkaloids / Q000493:pharmacokinetics / Q000494:pharmacology; D044005:Tetrahydroisoquinolines
C493595:Drd3 protein, rat; D007546:Isoquinolines; D008024:Ligands; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; D011957:Receptors, Opioid; D012490:Salsoline Alkaloids; D044005:Tetrahydroisoquinolines; D004744:Enkephalin, Methionine; C022118:enkephalinamide-Met, Ala(2)-; C036617:salsolinol; C032837:salsoline; D004298:Dopamine
Vzaimodeĭstvie prostykh tetragidroizokhinolinov s opiatnymi i vysokospetsificheskimi dofaminovymi (D3) retseptorami polosatogo mozga krys.