+ 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

The separation of 3H-benzodiazepine binding sites in brain and of benzodiazepine pharmacological properties



The separation of 3H-benzodiazepine binding sites in brain and of benzodiazepine pharmacological properties



Pharmacology Biochemistry and Behavior 18(2): 311-318



In addition to anxiolytic and anticonvulsant properties, benzodiazepines (BDZ) produce sedation, ataxia, and muscular relaxation. In general, it was difficult to separate these properties within this chemical class during the search for clinically useful anxiolytics; and when BDZ's were used to characterize 3H-BDZ binding sites they indicated only a single homogenous class of receptors. A new chemical series was discovered, triazolopyridazines (TPZ, prototype CL 218,872), which showed anticonflict activity in rats and monkeys without sedation or ataxia and inhibited 3H-BDZ binding in brain membranes with kinetic characteristics suggesting the presence of multiple BDZ receptors. High affinity and low affinity sites for the TPZ were demonstrated, the former designated at Type 1 and the latter as Type 2. Anatomical and in vivo studies have supported different distributions of each receptor in brain. Lately, the physical separation of discrete proteins which bind 3H-BDZ has been reported. The multiple receptors and the variety of endogenous substances which have been proposed as modulators and ligands of the receptors might explain variability as well as selectivity in pharmacological properties in these drugs.

Please choose payment method:






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

Accession: 044747851

Download citation: RISBibTeXText

PMID: 6132409

DOI: 10.1016/0091-3057(83)90385-4


Related references

The separation of tritium labeled benzodiazepine binding sites in brain and of benzodiazepine pharmacological properties. Pharmacology Biochemistry & Behavior 18(2): 311-318, 1983

Binding of several benzodiazepines to benzodiazepine receptors and peripheral benzodiazepine binding sites in the mouse brain in vivo. Naunyn Schmiedeberg'S Archives Of Pharmacologyuppl: R91, 1985

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

Pharmacological and physiological properties of benzodiazepine binding sites in rodent brown adipose tissue. Comparative Biochemistry & Physiology C Pharmacology Toxicology & Endocrinology 77(2): 339-344, 1984

Heterogeneity in the allosteric interaction between the gamma-aminobutyric acid (GABA) binding site and three different benzodiazepine binding sites of the GABAA/benzodiazepine receptor complex in the rat nervous system. Journal of Neurochemistry 58(2): 485-493, 1992

Radioligands for PET studies of central benzodiazepine receptors and PK (peripheral benzodiazepine) binding sites--current status. Nuclear Medicine and Biology 20(4): 503-525, 1993

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, 1978

Chronic exposure of cells expressing recombinant GABAA receptors to benzodiazepine antagonist flumazenil enhances the maximum number of benzodiazepine binding sites. Life Sciences 76(3): 303-317, 2004

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

Phylogenetic conservation of the benzodiazepine binding sites pharmacological evidence. Neuropharmacology 27(2): 163-170, 1988

Increase in tritium labeled flunitrazepam binding in vitro and in vivo to rat brain benzodiazepine receptors by tofisopam a 3 4 benzodiazepine. Pharmacological Research Communications 13(1): 75-86, 1981

The increase in the binding of tritium labeled flunitrazepam to rat brain benzodiazepine receptors in vitro and in vivo by tofisopam a 3 4 benzodiazepine. Naunyn-Schmiedeberg's Archives of Pharmacology 313(Suppl.): R34, 1980

The demonstration of benzodiazepine binding sites and of pharmacological effects of benzodiazepines in retina. Unknown, 1985

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

The Mr 18,000 subunit of the peripheral-type benzodiazepine receptor exhibits both benzodiazepine and isoquinoline carboxamide binding sites in the absence of the voltage-dependent anion channel or of the adenine nucleotide carrier. Journal of Biological Chemistry 272(44): 28102-6, 1997