Benzodiazepine agonist-type activity of raubasine, a rauwolfia serpentina alkaloid.

Abstract

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.

• Authors: M Charveron, M B Assié, A Stenger, M Briley
• Journal: European journal of pharmacology (Eur J Pharmacol) Vol. 106 Issue 2 Pg. 313-7 (Nov 13 1984) ISSN: 0014-2999 [Print] Netherlands
• PMID: 6099274 (Publication Type: Journal Article)

Chemical References

• Anticonvulsants
• Benzodiazepinones
• Receptors, GABA-A
• Secologanin Tryptamine Alkaloids
• Yohimbine
• Flumazenil
• raubasine
• Flurazepam
• Diazepam

Topics

• Animals
• Anticonvulsants
• Benzodiazepinones (pharmacology)
• Binding, Competitive
• Brain (metabolism)
• Diazepam (pharmacology)
• Flumazenil
• Flurazepam (metabolism)
• In Vitro Techniques
• Kinetics
• Male
• Mice
• Rats
• Receptors, GABA-A (drug effects, metabolism)
• Secologanin Tryptamine Alkaloids
• Yohimbine (pharmacology)