Anxiolytic-like effects of PNU-101017, a partial agonist at the benzodiazepine receptor.
Psychopharmacology (Berl)
; 131(3): 255-63, 1997 Jun.
Article
em En
| MEDLINE
| ID: mdl-9203236
ABSTRACT
PNU-101017 is a chemically novel ligand at the benzodiazepine recognition site of cloned GABAA receptors. It was reported to potentiate GABA-mediated chloride current in cultured cells with a moderate intrinsic activity and a biphasic dose-response relationship. In this study, we confirmed that PNU-101017 has a partial agonist-like effect in the antagonism of metrazole-induced seizures in mice. It produced no sedation or ataxia, but did antagonize diazepam-induced motor deficit of mice in the rotarod test. PNU-101017 was weakly active in anti-conflict anxiolytic tests, but attenuated the plasma corticosteroid response to mild stress in rats. It also antagonized stress-induced elevation of cerebellar cGMP levels in mice. Like chlordiazepoxide, it increased drinking of saline solution in thirsty rats. PNU-101017 did not potentiate the CNS-depressant effects of ethanol, and produced no evidence of physical dependence when administered repeatedly. Agonists with low intrinsic activity at the benzodiazepine receptor, such as PNU-101017, should be further explored for therapeutic uses.
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Base de dados:
MEDLINE
Assunto principal:
Quinolinas
/
Ansiolíticos
/
Agonistas de Receptores de GABA-A
Limite:
Animals
Idioma:
En
Revista:
Psychopharmacology (Berl)
Ano de publicação:
1997
Tipo de documento:
Article
País de afiliação:
Estados Unidos