Abstract
Two distinct benzodiazepine receptors are solubilized differentially by various detergents. The receptor sites that resist solubilization, designated type I, are most highly concentrated in the cerebellum and corpus striatum whereas the more readily solubilized receptors, type II, are most enriched in the hippocampus. The type I receptors display higher affinity for beta-carboline esters and a triazolopyridazine whereas several benzodiazepines do not differentiate the two receptors. The type I receptors can be solubilized with 2% Triton X-100/1 M NaCl; they retain the same drug specificity as in the particulate state.
MeSH Terms
Animals
Benzodiazepines/metabolism
Binding, Competitive
Brain Chemistry
Brain Mapping
Cattle
Guinea Pigs
Membrane Proteins/isolation & purification
Rats
Receptors, Cell Surface/isolation & purification
Receptors, Drug/isolation & purification,metabolism
Receptors, GABA-A
Receptors, Neurotransmitter/isolation & purification
Solubility
Chemicals
Membrane Proteins
Receptors, Cell Surface
Receptors, Drug
Receptors, GABA-A
Receptors, Neurotransmitter
Benzodiazepines
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Lo M M
Strittmatter S M
Snyder S H
References (20)
20 references, click to expand
-
Benzodiazepine receptors in rat brain.
Nature. 1977 Apr 21;266(5604):732-4
PMID: 876354
-
Benzodiazepine receptor: demonstration in the central nervous system.
Science. 1977 Nov 25;198(4319):849-51
PMID: 918669
-
An endogenous protein modulates the affinity of GABA and benzodiazepine receptors in rat brain.
Nature. 1978 Oct 12;275(5680):553-5
PMID: 211441
-
Putative benzodiazepine receptor: a protein solubilised from brain.
FEBS Lett. 1979 Aug 1;104(1):149-53
PMID: 39001
-
Lectin-agarose immobilization, a new method for detecting soluble membrane receptors. Application to studies with epidermal growth factor-urogastrone and transcobalamin-II.
J Biol Chem. 1979 Sep 25;254(18):8740-3
PMID: 314449
-
Solubilization of benzodiazepine binding site from rat cortex.
Life Sci. 1979 Jul 30;25(5):463-9
PMID: 39215
-
Solubilization of histamine H-1, GABA and benzodiazepine receptors.
Life Sci. 1979 Aug 27;25(9):783-9
PMID: 491857
-
Some properties of brain specific benzodiazepine receptors: new evidence for multiple receptors.
Pharmacol Biochem Behav. 1979 May;10(5):825-30
PMID: 40257
-
A synthetic non-benzodiazepine ligand for benzodiazepine receptors: a probe for investigating neuronal substrates of anxiety.
Pharmacol Biochem Behav. 1979 Jul;11(1):99-106
PMID: 40260
-
Resolution of two biochemically and pharmacologically distinct benzodiazepine receptors.
Pharmacol Biochem Behav. 1979 Oct;11(4):457-62
PMID: 523502
-
Urinary and brain beta-carboline-3-carboxylates as potent inhibitors of brain benzodiazepine receptors.
Proc Natl Acad Sci U S A. 1980 Apr;77(4):2288-92
PMID: 6246535
-
Soluble benzodiazepine receptors: GABAergic regulation.
Life Sci. 1980 Feb 25;26(8):579-82
PMID: 7382735
-
Solubilization of the benzodiazepine receptor from rat brain.
Life Sci. 1980 Feb 25;26(8):607-13
PMID: 7382738
-
Molecular heterogeneity of benzodiazepine receptors.
Nature. 1980 Jul 17;286(5770):285-7
PMID: 6250054
-
Ethyl beta-carboline-3-carboxylate shows differential benzodiazepine receptor interaction.
Nature. 1980 Aug 7;286(5773):606-7
PMID: 6250077
-
Multiple benzodiazepine receptor localization by light microscopic radiohistochemistry.
J Pharmacol Exp Ther. 1981 Feb;216(2):425-30
PMID: 6257892
-
gamma-Aminobutyric acid and benzodiazepine receptors: copurification and characterization.
Proc Natl Acad Sci U S A. 1981 Mar;78(3):1939-42
PMID: 6112752
-
[3H]Propyl beta-carboline-3-carboxylate as a selective radioligand for the BZ1 benzodiazepine receptor subclass.
J Neurochem. 1981 Aug;37(2):333-41
PMID: 6267199
-
Characterization of benzodiazepine and gamma-aminobutyric recognition sites and their endogenous modulators.
J Neurosci. 1981 Apr;1(4):409-18
PMID: 6267225
-
Multiple benzodiazepine receptors and their regulation by gamma-aminobutyric acid.
Life Sci. 1981 Jul 20;29(3):235-48
PMID: 6270491