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[3H]Diazepam binding in mammalian central nervous system: a pharmacological characterization.
Two types of benzodiazepine binding sites for [3H]diazepam in mammalian central nervous tissue were identified using selective in vitro tissue culture and in situ kainic acid lesion techniques. These two binding sites were pharmacologically distinguished by differential displacement of the [3H]diazepam radioligand using the centrally active benzodiazepine, clonazepam, and the centrally inactive benzodiazepine, RO5-4864. Clonazepam-displaceable binding sites were found to be located principally on neuronal membranes, while RO5-4864-displaceable binding sites were found to be located on non-neuronal elements. These pharmacological distinctions can be used to characterize the predominant cell types which bind benzodiazepines in nervous tissue. It is suggested that one quantitative measure of different cell populations is the ratio of clonazepam- to RO5-4864-displaceable [3H]diazepam binding within a single neuronal tissue simple.
PMID: 6267221 [PubMed - indexed for MEDLINE]
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Cited by 6 PubMed Central articles
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Antianxiety and antidepressant-like effects of AC-5216, a novel mitochondrial benzodiazepine receptor ligand.
Kita A, Kohayakawa H, Kinoshita T, Ochi Y, Nakamichi K, Kurumiya S, Furukawa K, Oka M.
Br J Pharmacol. 2004 Aug; 142(7):1059-72. Epub 2004 Jul 12.
[Br J Pharmacol. 2004]
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Interaction of calcium channel blockers with non-neuronal benzodiazepine binding sites.
Cantor EH, Kenessey A, Semenuk G, Spector S.
Proc Natl Acad Sci U S A. 1984 Mar; 81(5):1549-52.
[Proc Natl Acad Sci U S A. 1984]
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Imaging of a glioma using peripheral benzodiazepine receptor ligands.
Starosta-Rubinstein S, Ciliax BJ, Penney JB, McKeever P, Young AB.
Proc Natl Acad Sci U S A. 1987 Feb; 84(3):891-5.
[Proc Natl Acad Sci U S A. 1987]
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Patient Drug Information
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Diazepam (Diazepam Intensol® , Valium® )
Diazepam is used to relieve anxiety, muscle spasms, and seizures and to control agitation caused by alcohol withdrawal.
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Clonazepam (Klonopin® )
Clonazepam is used alone or in combination with other medications to control certain types of seizures. It is also used to relieve panic attacks (sudden, unexpected attacks of extreme fear and worry about these attacks)....