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.
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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)
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Chemical References |
- Anticonvulsants
- Benzodiazepinones
- Receptors, GABA-A
- Secologanin Tryptamine Alkaloids
- Yohimbine
- Flumazenil
- raubasine
- Flurazepam
- Diazepam
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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)
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