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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Neuronal expression of TSPO has been observed in rodents but not in humans.
“Neuronal expression of TSPO has been observed in rodents [35;36;55] but not in humans”
From Expression of the translocator protein of 18 kDa by microglia, macrophages and astrocytes based on immunohistochemical localization in abnormal human brain (2009) · cites this paper as [35]
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Cosenza‐Nashat, M., Zhao, M. ‐., Suh, H. ‐., Morgan, J., Natividad, R., Morgello, S., & Lee, S. C. (2009) · Neuropathology and Applied Neurobiology · doi:10.1111/j.1365-2990.2008.01006.x · Cited by 459 · see citing works
- 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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