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Relative efficacies of 1,4-diazepines on GABA-stimulated chloride influx in rat brain vesicles

Journal Article · · Life Sci.; (United States)
; ; ; ;
The effects of 1,4-diazepines with two annelated heterocycles (brotizolam (WE 941), ciclotizolam (WE 973) and WE 1008) on gamma-aminobutyric acid (GABA)-stimulated chloride influx into rat brain membrane vesicles were examined. Brotizolam enhanced GABA-stimulated /sup 36/Cl/sup /minus// influx, while ciclotizolam and WE 1008 showed only a small enhancement of GABA-stimulated /sup 36/Cl/sup /minus// uptake. Brotizolam resulted in a left shift of the GABA dose response curve at lower concentrations of GABA, while at higher concentrations of GABA, brotizolam caused a reduction of the maximal response. The enhancement of GABA-stimulated /sup 36/Cl/sup /minus// uptake by brotizolam was antagonized by Ro 15-1788. At higher concentration of GABA (300 /mu/M), brotizolam inhibited GABA-stimulated /sup 36/Cl/sup /minus// uptake in a dose dependent manner and Ro 15-1788 failed to antagonize this effect.
Research Organization:
Univ. of Arizona Health Sciences Center, Tucson (USA)
OSTI ID:
5858007
Journal Information:
Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 45:4; ISSN LIFSA
Country of Publication:
United States
Language:
English

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Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
AMINO ACIDS
AMINOBUTYRIC ACID
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL EFFECTS
BODY
BRAIN
CARBOXYLIC ACIDS
CELL CONSTITUENTS
CELL MEMBRANES
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM AGENTS
CHLORIDES
CHLORINE 36
CHLORINE COMPOUNDS
CHLORINE ISOTOPES
DOSE-RESPONSE RELATIONSHIPS
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
HALIDES
HALOGEN COMPOUNDS
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LIGHT NUCLEI
MAMMALS
MEMBRANE TRANSPORT
MEMBRANES
NERVOUS SYSTEM
NEUROREGULATORS
NUCLEI
ODD-ODD NUCLEI
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANS
PSYCHOTROPIC DRUGS
RADIOISOTOPES
RATS
REACTION KINETICS
RODENTS
TRACER TECHNIQUES
TRANQUILIZERS
VERTEBRATES
YEARS LIVING RADIOISOTOPES