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pubmed-article:3121132pubmed:abstractTextThe ability of the imidazobenzodiazepine Ro 15-1788 to displace diazepam from brain membranes in vitro and to antagonize the anticonvulsant activity of diazepam in vivo was determined in epileptic fowl. At doses of 1.0 mg/kg and higher, Ro 15-1788 significantly attenuated the anticonvulsant action of diazepam (1.0 mg/kg) in epileptic chickens. Ro 15-1788 alone exerted no anticonvulsant activity even in doses as high as 10 mg/kg. Specific binding of 10 nM [3H]diazepam to whole homogenate fractions prepared from cerebral hemispheres of epileptic fowl was inhibited by Ro 15-1788 with an IC50 of 8.5 nM and the Ki was determined to be 4.25 nM. These results suggest that Ro 15-1788 competes directly with diazepam for a binding site involved in producing anticonvulsant activity.lld:pubmed
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pubmed-article:3121132pubmed:issn0006-8993lld:pubmed
pubmed-article:3121132pubmed:authorpubmed-author:JohnsonD DDDlld:pubmed
pubmed-article:3121132pubmed:authorpubmed-author:CrawfordR DRDlld:pubmed
pubmed-article:3121132pubmed:authorpubmed-author:TuchekJ MJMlld:pubmed
pubmed-article:3121132pubmed:authorpubmed-author:WilcoxRRlld:pubmed
pubmed-article:3121132pubmed:authorpubmed-author:PedderS CSClld:pubmed
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pubmed-article:3121132pubmed:volume424lld:pubmed
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pubmed-article:3121132pubmed:pagination139-43lld:pubmed
pubmed-article:3121132pubmed:dateRevised2006-11-15lld:pubmed
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pubmed-article:3121132pubmed:year1987lld:pubmed
pubmed-article:3121132pubmed:articleTitleBenzodiazepine antagonist Ro 15-1788 (flumazepil) attenuates the anticonvulsant activity of diazepam in epileptic fowl.lld:pubmed
pubmed-article:3121132pubmed:affiliationDepartment of Pharmacology, College of Medicine, University of Saskatchewan, Saskatoon, Canada.lld:pubmed
pubmed-article:3121132pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:3121132pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed