| Pharmacodynamics and pharmacokinetics of AHR-11748, a new antiepileptic agent, in rodents. | |
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MedLine Citation:
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PMID: 2384074 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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AHR-11748, the desmethyl metabolite of fluzinamide (an effective antiepileptic), was active in preventing maximal seizures induced in mice or rats by electroshock and threshold seizures induced in mice by Metrazol, bicuculline, and picrotoxin. The compound showed a profile of anticonvulsant activity similar to those of phenobarbital and valproic acid and different from those of phenytoin and ethosuximide. ED50s were less than those of valproic acid, but greater than those of phenobarbital. Analysis of plasma and whole brain homogenates of mice indicated that AHR-11748 has an apparent terminal half-life (t1/2, beta) of 1.0 h. The brain:plasma ratio of AHR-11748 was 3.4:1 from 0.5 h to 6 h. |
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Authors:
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D N Johnson; M A Osman; L K Cheng; E A Swinyard |
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Publication Detail:
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Type: Journal Article; Research Support, U.S. Gov't, P.H.S. |
Journal Detail:
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Title: Epilepsy research Volume: 5 ISSN: 0920-1211 ISO Abbreviation: Epilepsy Res. Publication Date: 1990 Apr |
Date Detail:
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Created Date: 1990-09-20 Completed Date: 1990-09-20 Revised Date: 2007-11-14 |
Medline Journal Info:
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Nlm Unique ID: 8703089 Medline TA: Epilepsy Res Country: NETHERLANDS |
Other Details:
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Languages: eng Pagination: 185-91 Citation Subset: IM |
Affiliation:
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Department of Pharmacology, A.H. Robins Research Laboratories, Richmond, VA 23220. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Oral Animals Anticonvulsants / pharmacokinetics, therapeutic use* Azetidines / administration & dosage, pharmacokinetics, therapeutic use* Azetines / therapeutic use* Epilepsy / chemically induced, drug therapy* Female Injections, Intraperitoneal Male Mice Mice, Inbred ICR |
| Grant Support | |
ID/Acronym/Agency:
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N01-NS-4-2361/NS/NINDS NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Anticonvulsants; 0/Azetidines; 0/Azetines; 91077-32-6/AHR 11748 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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