Pharmacological activity of hyperforin acetate in rats.
Behav Pharmacol
; 13(8): 645-51, 2002 Dec.
Article
en En
| MEDLINE
| ID: mdl-12478215
ABSTRACT
Hyperforin, the main antidepressant component of Hypericum extract, is not stable with regard to heat and light. Therefore, we investigated a newly synthetized derivative, hyperforin acetate. Herein we demonstrate its efficacy in animal models sensitive to antidepressant and anxiolytic drugs. In the forced swimming test, triple administration of hyperforin (5-20 mg/kg) significantly reduced the immobility time of rats, while in the learned helplessness test a daily treatment of 10 mg/kg for seven consecutive days was necessary to elicit an antidepressant effect. In the elevated plus-maze and in the light-dark test, the acute administration of hyperforin acetate (3-5 mg/kg) exerted an anxiolytic activity, which, however, was smaller than that of diazepam. The effect was inhibited by the pretreatment of rats with metergoline, a serotoninergic antagonist, but not with CGS-8216, a benzodiazepine receptor antagonist. Hyperforin acetate (3-10 mg/kg) was also able to reduce locomotion in rats without eliciting myorelaxant activity. As Hypericum extract was claimed to exert a potential influence on the liver drug metabolizing system, we showed that neither acute nor repeated oral doses of hyperforin acetate altered pentobarbital sleeping time in rats. Taken together, the present results show that hyperforin acetate is a pharmacologically active derivative of hyperforin and may be a starting point from which to develop new compounds for therapeutic purposes.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Terpenos
/
Ansiolíticos
/
Conducta Animal
/
Actividad Motora
/
Antidepresivos
Tipo de estudio:
Prognostic_studies
Límite:
Animals
Idioma:
En
Revista:
Behav Pharmacol
Asunto de la revista:
CIENCIAS DO COMPORTAMENTO
/
FARMACOLOGIA
Año:
2002
Tipo del documento:
Article
País de afiliación:
Italia