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Publication : Interactions between benzodiazepine antagonists, inverse agonists, and acute behavioral effects of ethanol in mice.

First Author  Syapin PJ Year  1990
Journal  Brain Res Bull Volume  24
Issue  5 Pages  705-9
PubMed ID  2162723 Mgi Jnum  J:26428
Mgi Id  MGI:75413 Doi  10.1016/0361-9230(90)90012-o
Citation  Syapin PJ, et al. (1990) Interactions between benzodiazepine antagonists, inverse agonists, and acute behavioral effects of ethanol in mice. Brain Res Bull 24(5):705-9
abstractText  The behavioral manifestations of acute ethanol intoxication resemble those of benzodiazepines, barbiturates and general anesthetics. This has led to speculation that these drugs share common mechanisms or sites of actions within the brain. The discovery of a specific benzodiazepine receptor site, and the subsequent development of selective receptor antagonist and inverse agonist drugs, provides a framework to test the involvement of the benzodiazepine receptor complex in mediating ethanol's behavioral effects. The partial inverse agonist Ro15-4513, an analog of the benzodiazepine receptor antagonist Ro15-1788 (flumazenil), has been reported to block or reduce some of ethanol's acute effects in rodents by a benzodiazepine receptor-mediated action. There has been some controversy over whether the antialcohol effect of Ro15-4513 is a unique property of this compound or is shared by other benzodiazepine antagonists with inverse agonist activity. We have studied the effects of Ro15-4513 and other benzodiazepine receptor antagonists on acute ethanol intoxication in mice and have obtained evidence that 1) Ro15-4513 differentially affects acute effects of ethanol, 2) an antialcohol property is not a general feature of all benzodiazepine antagonists and inverse agonists, and 3) antialcohol activity may not be unique to Ro15-4513.
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