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Title Amoxapine inhibition of GABA-stimulated chloride conductance: Investigations of potential sites of activity
Creator/Author Ikeda, M. ; Knapp, R.J. ; Yamamura, H.I. (Univ. of Arizona, Tucson (USA)) ; Malatynska, E. (Ohio State Univ., Columbus (USA))
Publication Date1989 Jan 01
OSTI IdentifierOSTI ID: 7027108
Other Number(s)Journal ID: ISSN 0024-3205; CODEN: LIFSA
Resource TypeJournal Article
Resource RelationJournal Name: Life Sciences; (USA); Journal Volume: 45:20
Subject59 BASIC BIOLOGICAL SCIENCES; AMINOBUTYRIC ACID; RECEPTORS; ANTIDEPRESSANTS; BIOCHEMICAL REACTION KINETICS; CHLORIDES; MEMBRANE TRANSPORT; CELL MEMBRANES; CEREBRAL CORTEX; CHLORINE 36; DOSE-RESPONSE RELATIONSHIPS; INHIBITION; RATS; TRACER TECHNIQUES; TRITIUM COMPOUNDS; AMINO ACIDS; ANIMALS; AUTONOMIC NERVOUS SYSTEM AGENTS; BETA DECAY RADIOISOTOPES; BETA-MINUS DECAY RADIOISOTOPES; BODY; BRAIN; CARBOXYLIC ACIDS; CELL CONSTITUENTS; CENTRAL NERVOUS SYSTEM; CENTRAL NERVOUS SYSTEM AGENTS; CEREBRUM; CHLORINE COMPOUNDS; CHLORINE ISOTOPES; DRUGS; ELECTRON CAPTURE RADIOISOTOPES; HALIDES; HALOGEN COMPOUNDS; HYDROGEN COMPOUNDS; ISOTOPE APPLICATIONS; ISOTOPES; KINETICS; LIGHT NUCLEI; MAMMALS; MEMBRANE PROTEINS; MEMBRANES; NERVOUS SYSTEM; NEUROREGULATORS; NUCLEI; ODD-ODD NUCLEI; ORGANIC ACIDS; ORGANIC COMPOUNDS; ORGANS; PROTEINS; PSYCHOTROPIC DRUGS; RADIOISOTOPES; REACTION KINETICS; RODENTS; VERTEBRATES; YEARS LIVING RADIOISOTOPES
Description/AbstractAmoxapine inhibits GABA-stimulated chloride conductance by acting on the GABA{sub A}-receptor chloride-ionophore complex which can be studied using membrane vesicles prepared from rat cerebral cortex. Amoxapine produces a right shift in the GABA concentration-response curve for the stimulation of {sup 36}Cl{sup {minus}} uptake into these vesicles with no apparent change in the maximum response. Schild analysis of these data gave a pA{sub 2} value of 5.52 with a slope of 0.79. Amoxapine inhibits the binding of the GABA{sub A} receptor selective antagonist ({sup 3}H)SR 95531 with an IC{sub 50} value of 3.45 {mu}M and a pseudo Hill coefficient of 0.83. In contrast, 10 {mu}M amoxapine inhibits ({sup 3}H) flunitrazepam binding by less than 25% while the benzodiazepine antagonist Ro 15-1788 reduces the amoxapine inhibition of GABA-stimulated chloride conductance only at high concentrations.
Country of PublicationUnited States
LanguageEnglish
FormatMedium: X; Size: Pages: 1903-1910
System Entry Date2008 Feb 12

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