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Titolo:
APPARENT ANTINOCICEPTIVE AND ANTIINFLAMMATORY EFFECTS OF GYKI52466
Autore:
SZEKELY JI; KEDVES R; MATE I; TOROK K; TARNAWA I;
Indirizzi:
INST DRUG RES,POB 82 H-1325 BUDAPEST HUNGARY
Titolo Testata:
European journal of pharmacology
fascicolo: 2-3, volume: 336, anno: 1997,
pagine: 143 - 154
SICI:
0014-2999(1997)336:2-3<143:AAAAEO>2.0.ZU;2-6
Fonte:
ISI
Lingua:
ENG
Soggetto:
ACID RECEPTOR ANTAGONISTS; DORSAL HORN; NON-NMDA; THERMAL HYPERALGESIA; GLUTAMATE RECEPTORS; JOINT INFLAMMATION; AMPA RECEPTOR; CHRONIC PAIN; SPINAL RATS; GYKI 52466;
Keywords:
GYKI52466; GYKI53773; GYKI53784; 2,S-BENZODIAZEPINE; ANALGESIA; ANTIINFLAMMATORY DRUG;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
54
Recensione:
Indirizzi per estratti:
Citazione:
J.I. Szekely et al., "APPARENT ANTINOCICEPTIVE AND ANTIINFLAMMATORY EFFECTS OF GYKI52466", European journal of pharmacology, 336(2-3), 1997, pp. 143-154

Abstract

GYKI 52466 4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine) was examined in a battery of analgesia and anti-inflammatory tests in rats and mice, respectively. Its 3-N-acetyl (GYKI 53773) and 3-N-methylcarbamoyl (GYKI 53784) derivatives were also examined in some assays. These 2,3-benzodiazepines, known as prototypic non-competitive antagonists of AMPA receptors, showed a peculiar profile in some routinely used antinociceptive tests. They were found fairly potent in rat tail flick and mouse phenylquinone writhing assays but the dose-response curves were rather shallow as compared to that of morphine. Their action is stereoselective, i.e., the (+)isomers were found inactive, in agreement with the previous in vitro studies. Their antinociceptive effect could not be reversed by naloxone and the GYKI compounds did not potentiate significantly the morphine-induced analgesia. In the mouse hot plate assay the 2,3-benzodiazepines were active only in doses inducing visiblemotor incapacitation. In rats, GYKI 52466 weakly reduced the hypersensitivity accompanying acute carrageenan edema. However, it potently inhibited the hyperalgesia during Freund adjuvant-induced chronic arthritis. In the latter assay GYKI 52466 also attenuated the body weight loss without altering the paw edema. The present findings confirm reports in the literature which indicate AMPA receptors may contribute to certain forms of pathological hyperalgesia, e.g., to that detectable in inflamed tissues. (C) 1997 Elsevier Science B.V.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 31/03/20 alle ore 19:17:38