Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
Biphasic modulation of GABA(A) receptor binding by steroids suggests functional correlates
Autore:
Srinivasan, S; Sapp, DW; Tobin, AJ; Olsen, RW;
Indirizzi:
Univ Calif Los Angeles, Sch Med, Dept Mol & Med Pharmacol, Ctr Hlth Sci, Los Angeles, CA 90095 USA Univ Calif Los Angeles Los Angeles CA USA 90095 Los Angeles, CA 90095 USA Univ Calif Los Angeles, Brain Res Inst, Los Angeles, CA 90024 USA Univ Calif Los Angeles Los Angeles CA USA 90024 Los Angeles, CA 90024 USA Univ Calif Los Angeles, Inst Mol Biol, Los Angeles, CA 90024 USA Univ Calif Los Angeles Los Angeles CA USA 90024 Los Angeles, CA 90024 USA Univ Calif Los Angeles, Dept Physiol Sci, Los Angeles, CA 90024 USA Univ Calif Los Angeles Los Angeles CA USA 90024 Los Angeles, CA 90024 USA Univ Calif Los Angeles, Dept Neurol, Los Angeles, CA 90024 USA Univ Calif Los Angeles Los Angeles CA USA 90024 Los Angeles, CA 90024 USA Univ Calif Los Angeles, Dept Anesthesiol, Los Angeles, CA 90024 USA Univ Calif Los Angeles Los Angeles CA USA 90024 Los Angeles, CA 90024 USA Univ Calif Los Angeles, Mental Retardat Res Ctr, Los Angeles, CA 90024 USAUniv Calif Los Angeles Los Angeles CA USA 90024 Los Angeles, CA 90024 USA
Titolo Testata:
NEUROCHEMICAL RESEARCH
fascicolo: 11, volume: 24, anno: 1999,
pagine: 1363 - 1372
SICI:
0364-3190(199911)24:11<1363:BMOGRB>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
GAMMA-AMINOBUTYRIC-ACID; BENZODIAZEPINE RECEPTOR; A-RECEPTOR; NEUROACTIVE STEROIDS; SUBUNIT COMPOSITION; H-3 FLUNITRAZEPAM; RECOGNITION SITES; ION CHANNELS; TBPS BINDING; SUBTYPES;
Keywords:
neurosteroids; radioligand binding; GABA(A) receptor subtypes; allosteric modulators; conformational model;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
46
Recensione:
Indirizzi per estratti:
Indirizzo: Olsen, RW Univ Calif Los Angeles, Sch Med, Dept Mol & Med Pharmacol, Ctr Hlth Sci, Room 23-120,10833 LeConte Ave, Los Angeles, CA 90095 USA Univ Calif Los Angeles Room 23-120,10833 LeConte Ave Los Angeles CA USA 90095
Citazione:
S. Srinivasan et al., "Biphasic modulation of GABA(A) receptor binding by steroids suggests functional correlates", NEUROCHEM R, 24(11), 1999, pp. 1363-1372

Abstract

Neuroactive steroids and other positive modulators of GABA, receptors showed regional variation in both the efficacy and potency for modulation of [S-35]TBPS binding to rat brain membrane homogenates, with biphasic concentration-dependence. GABA present in the binding assays prevented the enhancement phase of the steroid concentration-dependence plot while the antagonistsbicuculline and RU5135 prevented the inhibition phase. Using recombinant GABAA receptors, expressed in insect cell line Sf9 using baculovirus, enhancement by steroids of [S-35]TBPS binding was sensitive to the presence of the gamma 2 subunit and the nature of the a subunit (alpha 1 beta 2 gamma 2S > alpha 1 beta 2, alpha 6 beta 2, alpha 6 beta 2 gamma 2S, and alpha 6 beta2 delta). As in cerebellum, addition of RU5135 reduced the inhibitory phase and revealed a small enhancement of TBPS binding by neuroactive steroids. The subunit-dependent interactions of steroid and GABA site ligands are consistent with a three-state model in which the receptor mono-liganded by GABA or steroid has a different affinity for TBPS than the resting state, andthe receptor biliganded by GABA, steroid, or both has little affinity for TBPS.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/03/20 alle ore 12:40:53