PMID: 40254May 1, 1979

Molecular mechanisms regulating the interactions between the benzodazepines and GABA receptors in the central nervous system

Pharmacology, Biochemistry, and Behavior
A GuidottiE Costa

Abstract

Using radioreceptor assay techniques to measure the kinetics of GABA and diazepam receptors, a relationship between GABA and benzodiazepine receptors has been firmly established in membranes of brain and neuroblastoma NB2a clonal cell lines. Occupancy of benzodiazepine receptors uncovers a new population of GABA receptors (GABA2 receptors) endowed with high affinity for GABA. Moreover, stimulation of GABA receptors increases the affinity of 1,4-benzodiazepine receptors for 1,4-benzodiazepines. This reciprocal interaction appears to be mediated by an endogenous regulatory protein (for details on this protein see [14 and 29]) which allosterically regulates GABA2 receptors while it competitively interacts with benzodiazepines for their specific binding sites. The rank order of potency of the various 1,4-benzodiazepines to block the action of this protein inhibitor on GABA receptors is related to their capacity to displace 3H-diazepam binding. These data suggest that the interaction between the 1,4-benzodiazepine receptors and the endogenous protein modulator of GABA2 receptors might play a role in the pharmacological action of the 1,4-benzodiazepines.

References

Jul 27, 1978·Nature·J F TallmanD W Gallager
Sep 12, 1978·Naunyn-Schmiedeberg's Archives of Pharmacology·H M GellerB J Hoffer
Jan 1, 1979·The Journal of Pharmacy and Pharmacology·J ArntJ Scheel-Krüger
Dec 1, 1978·Proceedings of the National Academy of Sciences of the United States of America·G D ColelloK Folkers
Oct 12, 1978·Nature·L L Iversen
Sep 1, 1978·The British Journal of Psychiatry : the Journal of Mental Science·E CostaG Toffano
Apr 21, 1977·Nature·R F Squires, C Brastrup

Citations

Mar 12, 1982·European Journal of Pharmacology·B A Meiners, A I Salama
Mar 12, 1985·European Journal of Pharmacology·F FaddaG L Gessa
Jan 1, 1989·Pharmacology & Therapeutics·V SaanoM Räty
Jan 1, 1983·Neurochemistry International·M Hamon, P Soubrié
Oct 19, 2010·Neuropharmacology·S J Enna
Jan 1, 1987·Annales Françaises D'anesthèsie Et De Rèanimation·J Kienlen, J du Cailar

Related Concepts

Metazoa
Benzodiazepines
Brain
Gammalon
Neuroblastoma
Receptors, Drug
Anti-Anxiety Effect
Mouse, Swiss

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