Benzodiazepine agonist-type activity of raubasine, a rauwolfia serpentina alkaloid.
Raubasine produced a dose-related inhibition of specific [3H]flunitrazepam binding to rat brain membranes. Scatchard analyses revealed a significant increase in the affinity constant but no change in the number of binding sites, suggesting that raubasine acts as a competitive inhibitor. Raubasine also inhibited the in vivo binding of [3H]flunitrazepam to mouse brain sites. Behavioral studies showed raubasine to possess anticonvulsant properties against pentylenetetrazol- and bicuculline-induced convulsions in mice. These effects were inhibited by the benzodiazepine antagonist, Ro 15-1788. The results suggest that raubasine interacts directly at benzodiazepine sites with a benzodiazepine agonist-type activity.
D000818:Animals; D000927:Anticonvulsants; D001570:Benzodiazepinones / Q000494:pharmacology; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D003975:Diazepam / Q000494:pharmacology; D005442:Flumazenil; D005479:Flurazepam / Q000378:metabolism; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D051379:Mice; D051381:Rats; D011963:Receptors, GABA-A / Q000187:drug effects* / Q000378:metabolism; D046948:Secologanin Tryptamine Alkaloids; D015016:Yohimbine / Q000494:pharmacology*
D000927:Anticonvulsants; D001570:Benzodiazepinones; D011963:Receptors, GABA-A; D046948:Secologanin Tryptamine Alkaloids; D015016:Yohimbine; D005442:Flumazenil; C005709:raubasine; D005479:Flurazepam; D003975:Diazepam