What is Securinine alkaloids

There had been experiments to determine the site of action of securinine and related spasmodic Indolizidinen. All these compounds induced tonic induced in mice with CD50 values ​​of 11 to 87 mg / kg. The CD50 for bicuculline was at 8 mg / kg found. Equilibrium binding assays have shown that dihydrosecurinin securinin and [3H] GABA binding to rat brain membranes with an inhibitory IC of about 50 μM, which is about 7-fold less potent than Bicuculline. Allosecurinin Virosecurinin and have IC50 values ​​greater than 1 mM. Both dihydrosecurinin and securinin inhibited GABA-stimulated Benzodiazepinbindung in rat brain membranes, although they were a little weaker in this regard than bicuculline. Other binding assays have shown that securinin and its analogs are inactive as inhibitors of bicuculline insensitive to GABA binding, a benzodiazepine, and the cholinergic receptor beta-adrenergic binding Muskarinin. In addition, while thiocyanate apparent bicuculline cohesion increased by 10-fold, it had little effect on the securinin. Extracellular electrophysiological studies on neurons in the spinal cord of the cat showed that securinin dihydrosecurinin and the inhibitory effect of GABA blocked, without this affected the action of glycine. Allografts and Virosecurinin were significantly less active in this assay than GABA receptor antagonists. These results suggest that, as bicuculline and securinine dihydrosecurinin are selective antagonists of GABA recognition sites in central mammalian neurons.