| Autor: |
Tang, A. H., Franklin, S. R., Carter, D. B., Sethy, V. H., Needham, L. M., Jacobsen, E. J., Voigtlander, P. F. Von |
| Předmět: |
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| Zdroj: |
Psychopharmacology; 1997, Vol. 131 Issue 3, p255, 9p |
| Abstrakt: |
Abstract PNU-101017 is a chemically novel ligand at the benzodiazepine recognition site of cloned GABA[sub A] 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. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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