Cited by 64Neuroscience and Neuropharmacology ResearchEpilepsy research and treatmentSynthesis and pharmacology of benzodiazepine derivatives

Characterization of the Binding of [3H]Ro 5‐4864, a Convulsant Benzodiazepine, to Guinea Pig Brain

Abstract

The density of high affinity binding sites for [3H]4'-chlorodiazepam [( 3H]Ro 5-4864) in guinea pig cerebral cortex is significantly higher (3.8-fold) than the density reported in the rat, and is nearly equal to the density of binding sites for other [3H]benzodiazepines (e.g., diazepam, flunitrazepam). The density of these [3H]Ro 5-4864 binding sites was generally higher in guinea pig brain than in rat brain, with the exception of olfactory bulb. Both the subcellular distribution and pharmacologic profile of these sites in guinea pig brain appears qualitatively similar to observations previously reported in the rat. The high density of binding sites for [3H]Ro 5-4864, coupled with the potency of this compound as a convulsant in the guinea pig, suggest this species will be a valuable model for elucidating putative pharmacologic and physiologic functions of these sites in brain.

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Crossref · 10.1111/j.1471-4159.1984.tb12698.x

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Authors
Weissman, B. A., Bolger, G. T., Isaac, L., Paul, S. M., & Skolnick, P.
Affiliations
National Institutes of Health (US)
Corresponding author
Weissman, Ben Avi
Venue
Journal of Neurochemistry
Publisher
Wiley
Published
1984-04
Volume
42
Issue
4
Pages
969-975
ISSN
  • 0022-3042 (ISSN-L)
  • 1471-4159
OpenAlex
W2012304822
Cited by
64
References
0
Citations by year
2023: 1 · 2017: 2
FWCI
2.94
Type
journal article
Language
en
Open access
closed
Locations
  • Journal of Neurochemistry (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
  • Health Sciences › Medicine › Psychiatry and Mental health › Epilepsy research and treatment
  • Physical Sciences › Chemistry › Organic Chemistry › Synthesis and pharmacology of benzodiazepine derivatives
Keywords
Ro5-4864, benzodiazepine binding site, high-affinity binding sites, cerebral cortex, guinea pig brain, subcellular localization, convulsant activity, olfactory bulb, animal models
MeSH terms
Animals, Benzodiazepinones, Binding Sites, Brain, Cats, Convulsants, Diazepam, Flunitrazepam, Guinea Pigs, Kinetics, Male, Receptors, Cell Surface, Receptors, GABA-A, Species Specificity, Tissue Distribution, Mice, Rats

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