Kardos J, Blaskó G, Simonyi M, Szántay C
Arzneimittelforschung. 1984;34(12):1758-9.
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.
生物碱5,6,8,14-四脱氢-4-羟基-3,6-二甲氧基-17-甲基吗啡喃-7-酮[(±)-刺桐定]被发现具有在大鼠脑突触膜中置换3H-γ-氨基丁酸(3H-GABA)的活性(IC50小于1μmol/L)。通过增加(±)-刺桐定的浓度增强特异性3H-地西泮结合呈最大曲线,表明(±)-刺桐定是GABA/苯二氮䓬受体复合物的部分激动剂。