+ Site Statistics
+ Search Articles
+ PDF Full Text Service
How our service works
Request PDF Full Text
+ Follow Us
Follow on Facebook
Follow on Twitter
Follow on LinkedIn
+ Subscribe to Site Feeds
Most Shared
PDF Full Text
+ Translate
+ Recently Requested

Benzodiazepine receptor binding: the interactions of some non-benzodiazepine drugs with specific [3H] diazepam binding to rat brain synaptosomal membranes

Benzodiazepine receptor binding: the interactions of some non-benzodiazepine drugs with specific [3H] diazepam binding to rat brain synaptosomal membranes

Naunyn-Schmiedeberg's Archives of Pharmacology 305(1): 23-26

The interaction of several non-benzodiazepine drugs with [3H] diazepam binding to benzodiazepine receptors in rat brain synaptosomal membranes was investigated. Baclofen, benzoctamine, hydroxyzine, chlorpromazine, haloperidol, imipramine, and amitriptyline displace specific [3H] diazepam binding, but the concentrations needed are too high to explain pharmacological effects of these drugs by an interaction with benzodiazepine receptors. The most potent non-benzodiazepine drug for inhibiting specific [3H] diazepam binding was methaqualone (IC50 value of 150 micrometer). It is suggested that interactions with benzodiazepine receptors may account for the anxiolytic and anticonvulsive side effects of this drug. The analeptic drug pentylenetetrazole interacts with benzodiazepine receptor binding with an IC50 value of about 1 mM, which is possibly too high to explain its convulsive properties by an antagonism at the benzodiazepine receptor.

Please choose payment method:

(PDF emailed within 0-6 h: $19.90)

Accession: 039379117

Download citation: RISBibTeXText

PMID: 723967

DOI: 10.1007/bf00497002

Related references

Benzo diazepine receptor binding the interactions of some nonbenzodiazepine drugs with specific tritiated diazepam binding to rat brain synaptosomal membranes. Naunyn Schmiedeberg's Archives of Pharmacology 305(1): 23-26, 1978

Interactions of some anaesthetic, convulsant, and anticonvulsant drugs at GABA-benzodiazepine receptor-ionophore complexes in rat brain synaptosomal membranes. Neurochemical Research 8(10): 1351-1362, 1983

Benzodiazepine receptor binding by membranes from brain cell cultures following chronic treatment with diazepam. Brain Research 288(1-2): 354-358, 1983

Diazepam receptor characterization: specific binding of a benzodiazepine to macromolecules in various areas of rat brain. Febs Letters 82(2): 368-372, 1977

Specific 3H-DMCM binding to a non-benzodiazepine binding site after silver ion treatment of rat brain membranes. Life Sciences 35(22): 2257-2267, 1984

Participation of a diazepam-binding inhibitor in the interaction between NAD and GABA-benzodiazepine receptor complex in synaptic membranes. Voprosy Meditsinskoi Khimii 41(6): 44-48, 1995

Tetrazepam: a benzodiazepine which dissociates sedation from other benzodiazepine activities. II. In vitro and in vivo interactions with benzodiazepine binding sites. Journal of Pharmacology and Experimental Therapeutics 245(2): 699-705, 1988

Biotinylated 1012-S conjugate as a probe ligand for benzodiazepine receptors: characterization of receptor binding sites and receptor assay for benzodiazepine drugs. Analytical Biochemistry 203(1): 158-162, 1992

Specific benzodiazepine receptors in rat brain characterized by high-affinity (3H)diazepam binding. Proceedings of the National Academy of Sciences of the United States of America 74(9): 3805-3809, 1977

Interaction of piracetam with tritiated imipramine specific binding sites and gamma aminobutyric acid benzodiazepine receptor complex of brain membranes. Byulleten' Eksperimental'noi Biologii i Meditsiny 101(1): 40-42, 1986

Post natal development in the effects of pento barbital on tritium labeled diazepam binding to the central type benzodiazepine receptors and the peripheral type benzodiazepine binding sites. Japanese Journal of Pharmacology 33(Suppl.): 245P, 1983

Photoaffinity labeling of benzodiazepine receptors in rat brain with flunitrazepam alters the affinity of benzodiazepine receptor agonist but not antagonist binding. Journal of Neurochemistry 41(5): 1407-1413, 1983

Reduced potentiation by gamma aminobutyric acid of benzodiazepine receptor binding in brain cell culture after chronic benzodiazepine exposure. Society for Neuroscience Abstracts 10(2): 971, 1984

Comparison of benzodiazepine receptor binding in membranes from human or rat brain. Neuropharmacology 24(8): 751-760, 1985

Diazepam-binding inhibitor/acyl-CoA-binding protein mRNA and peripheral benzodiazepine receptor mRNA in endocrine and immune tissues after prenatal diazepam exposure of male and female rats. Journal of Endocrinology 166(1): 163-171, 2000