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Titolo:
The effects of benzodiazepines on human opioid receptor binding and function
Autore:
Cox, RF; Collins, MA;
Indirizzi:
GlaxoSmithKline, Syst Res, Dept Receptor Biochem, Res Triangle Pk, NC 27709 USA GlaxoSmithKline Res Triangle Pk NC USA 27709 es Triangle Pk, NC 27709 USA GlaxoSmithKline, Dept Mol Pharmacol, Res Triangle Pk, NC 27709 USA GlaxoSmithKline Res Triangle Pk NC USA 27709 es Triangle Pk, NC 27709 USA
Titolo Testata:
ANESTHESIA AND ANALGESIA
fascicolo: 2, volume: 93, anno: 2001,
pagine: 354 - 358
SICI:
0003-2999(200108)93:2<354:TEOBOH>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
INTRATHECAL MIDAZOLAM; INVERSE AGONIST; CELL-MEMBRANES; ANALGESIA; RAT; ANTINOCICEPTION; BUPIVACAINE; ACTIVATION; NG108-15; LIGANDS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
17
Recensione:
Indirizzi per estratti:
Indirizzo: Cox, RF GlaxoSmithKline, Syst Res, Dept Receptor Biochem, Res Triangle Pk,NC 27709 USA GlaxoSmithKline Res Triangle Pk NC USA 27709 gle Pk, NC 27709 USA
Citazione:
R.F. Cox e M.A. Collins, "The effects of benzodiazepines on human opioid receptor binding and function", ANESTH ANAL, 93(2), 2001, pp. 354-358

Abstract

We performed in vitro studies to investigate the potential interaction of benzodiazepines with cloned human opioid receptor subtypes. Midazolam, chlordiazepoxide, and diazepam directly displaced [H-3]diprenorphine binding from kappa and delta receptors, but not mu receptors, whereas flumazenil was inactive. These benzodiazepines also stimulated S-35-GTP gammaS binding in membranes containing human kappa receptors, and the effect of midazolam wasprevented by a selective kappa antagonist. Midazolam was also weakly active at delta -receptor activation, whereas all three were inactive at mu receptors. The results suggest that the analgesic efficacy reported for intrathecal benzodiazepines may be attributed, in part, to direct interaction withkappa -opioid receptors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 12:31:07