Pharmacodynamic investigation of (+/-)-salutaridine.
The alkaloid 5,6,8,14-tetradehydro-4-hydroxy-3, 6-dimethoxy-17-methyl-morphinan-7-one[+/-)-salutaridine) was found to possess 3H-gamma-aminobutyric acid (3H-GABA) displacing activity (IC50 less than 1 mumol/l) in rat brain synaptic membranes. The enhancement of specific 3H-diazepam binding by increasing concentration of (+/-)-salutaridine follows a maximum curve indicating (+/-)-salutaridine to be a partial agonist at the GABA/benzodiazepine receptor complex.
D000818:Animals; D001640:Bicuculline / Q000494:pharmacology; D003975:Diazepam / Q000378:metabolism; D066298:In Vitro Techniques; D009019:Morphinans / Q000494:pharmacology*; D051381:Rats; D011963:Receptors, GABA-A / Q000378:metabolism*; D013570:Synaptic Membranes / Q000187:drug effects; D013574:Synaptosomes / Q000187:drug effects; D005680:gamma-Aminobutyric Acid / Q000378:metabolism
D009019:Morphinans; D011963:Receptors, GABA-A; D005680:gamma-Aminobutyric Acid; C009270:salutaridine; D003975:Diazepam; D001640:Bicuculline