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Titolo:
GV196771A, an NMDA receptor/glycine site antagonist, attenuates mechanicalallodynia in neuropathic rats and reduces tolerance induced by morphine inmice
Autore:
Quartaroli, M; Fasdelli, N; Bettelini, L; Maraia, G; Corsi, M;
Indirizzi:
GlaxoSmithKline SpA, Dept Biol, Med Res Ctr, I-37135 Verona, Italy GlaxoSmithKline SpA Verona Italy I-37135 Res Ctr, I-37135 Verona, Italy
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 2-3, volume: 430, anno: 2001,
pagine: 219 - 227
SICI:
0014-2999(20011102)430:2-3<219:GANRSA>2.0.ZU;2-4
Fonte:
ISI
Lingua:
ENG
Soggetto:
PROTEIN-KINASE-C; PERIPHERAL-NERVE INJURY; THERMAL HYPERALGESIA; GLYCINE SITE; SPINAL-CORD; AMINO-ACIDS; ASPARTATE; RECEPTORS; MONONEUROPATHY; INCREASES;
Keywords:
NMDA receptor/glycine site antagonist; chronic constrictive injury; mechanical allodynia; opioid; tolerance; GV196771A;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
44
Recensione:
Indirizzi per estratti:
Indirizzo: Quartaroli, M GlaxoSmithKline SpA, Dept Biol, Med Res Ctr, Via Fleming 4, I-37135 Verona, Italy GlaxoSmithKline SpA Via Fleming 4 Verona Italy I-37135 taly
Citazione:
M. Quartaroli et al., "GV196771A, an NMDA receptor/glycine site antagonist, attenuates mechanicalallodynia in neuropathic rats and reduces tolerance induced by morphine inmice", EUR J PHARM, 430(2-3), 2001, pp. 219-227

Abstract

The effects of the N-methyl-D-aspartate (NMDA) receptor/glycine site antagonist, GV196771A (E-4,6-dichloro-3-(2-oxo-1-phenyl-pyrrolidin-3-ylidenemethyl)-1H-indole-2-carboxylic acid sodium salt), on mechanical allodynia and on tolerance to the antinociceptive effects induced by morphine were evaluated. Its antiallodynic properties were studied in a model of chronic constriction injury applied to rat sciatic nerve. GV196771A (0.3-10 mg/kg, p.o.) dose-dependently inhibited established mechanical allodynia when tested 14 or 21 days after nerve ligation. In the formalin test in mice, GV196771A (10or 20 mg/kg, p.o.), administered for 8 days together with morphine 10 mg/kg, i.p. inhibited morphine tolerance development in both early and late phases of the test. This finding reinforces the key role of the NMDA receptorsin the plastic event, such as allodynia, which develops in some conditionsof painful neuropathy. Moreover, the capability to strongly reduce morphine-induced tolerance suggests that GV196771A could be an alternative agent for the treatment of difficult pain states not only when given alone, but also in combination, in order to prolong the analgesic effects of the opiates. (C) 2001 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/01/20 alle ore 18:41:47