Patsenko A A, Grinevich V P, Ostrovskiĭ Iu M
Farmakol Toksikol. 1987 Jul-Aug;50(4):33-5.
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.
