| Interaction of abecarnil, bretazenil, and RO 19-8022 with diazepam-sensitive and -insensitive benzodiazepine sites in the rat cerebellum and cerebral cortex. | |
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MedLine Citation:
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PMID: 7475974 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Abecarnil, bretazenil, and Ro 19-8022 inhibited the binding of [3H]Ro 15-4513 to diazepamsensitive and -insensitive sites in the rat cerebellum and cerebral cortex, but all three had a much higher affinity for the diazepam-sensitive sites in both tissues. The GABA-shift for bretazenil and Ro 19-8022 was low ( < 2) for all sites studied, consistent with their partial agonistic profile. The GABA-shift for abecarnil was appreciably higher for diazepam-sensitive binding in the cerebellum than in the cerebral cortex (1.97 vs 1.18). Furthermore, the GABA-shift for abecarnil was markedly different for the diazepam-sensitive and -insensitive sites in the cerebellum (1.97 vs 0.71). All three compounds inhibited [3H]Ro 15-4513 binding to the diazepam-sensitive sites with a slope factor > 1, suggestive of positive cooperativity in their binding to GABAA receptors. Abecarnil only partially inhibited diazepam-insensitive binding of [3H]Ro 15-4513 in the cerebellum, indicating that this site can be differentiated into abecarnil-sensitive and -insensitive components. |
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Authors:
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A K Mehta; R P Shank |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Life sciences Volume: 57 ISSN: 0024-3205 ISO Abbreviation: Life Sci. Publication Date: 1995 |
Date Detail:
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Created Date: 1995-12-21 Completed Date: 1995-12-21 Revised Date: 2003-11-14 |
Medline Journal Info:
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Nlm Unique ID: 0375521 Medline TA: Life Sci Country: ENGLAND |
Other Details:
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Languages: eng Pagination: 2215-22 Citation Subset: IM |
Affiliation:
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R.W. Johnson Pharmaceutical Research Institute, Spring House PA 19477-0776, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Anti-Anxiety Agents / pharmacology Benzodiazepinones / pharmacology* Binding Sites Brain / drug effects, metabolism* Carbolines / pharmacology* Cell Membrane / drug effects, metabolism Cerebellum / drug effects, metabolism Cerebral Cortex / drug effects, metabolism Diazepam / pharmacology* Male Pyrrolidines / pharmacology* Quinolizines / pharmacology* Rats Rats, Wistar Receptors, GABA-A / drug effects*, metabolism |
| Chemical | |
Reg. No./Substance:
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0/Anti-Anxiety Agents; 0/Benzodiazepinones; 0/Carbolines; 0/Pyrrolidines; 0/Quinolizines; 0/Receptors, GABA-A; 104604-66-2/Ro 19-8022; 111841-85-1/abecarnil; 439-14-5/Diazepam; 84379-13-5/bretazenil |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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