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Titolo:
4-[(ALKYLAMINO)METHYL]FURO[3,2-C]PYRIDINES - A NEW SERIES OF SELECTIVE KAPPA-RECEPTOR AGONISTS
Autore:
NAYLOR A; JUDD DB; SCOPES DIC; HAYES AG; BIRCH PJ;
Indirizzi:
GLAXO GRP RES LTD,DEPT MED CHEM WARE SG12 0DP HERTS ENGLAND GLAXO GRP RES LTD,DEPT NEUROPHARMACOL WARE SG12 0DP HERTS ENGLAND
Titolo Testata:
Journal of medicinal chemistry
fascicolo: 14, volume: 37, anno: 1994,
pagine: 2138 - 2144
SICI:
0022-2623(1994)37:14<2138:4-ANSO>2.0.ZU;2-B
Fonte:
ISI
Lingua:
ENG
Soggetto:
NALORPHINE-LIKE DRUGS; CHRONIC SPINAL DOG; OPIOID RECEPTOR; VAS-DEFERENS; OPIATE RECEPTORS; HIGHLY POTENT; MORPHINE-LIKE; ANTINOCICEPTION; DERIVATIVES; ANALGESICS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
28
Recensione:
Indirizzi per estratti:
Citazione:
A. Naylor et al., "4-[(ALKYLAMINO)METHYL]FURO[3,2-C]PYRIDINES - A NEW SERIES OF SELECTIVE KAPPA-RECEPTOR AGONISTS", Journal of medicinal chemistry, 37(14), 1994, pp. 2138-2144

Abstract

The synthesis of acetyl)-4-[(alkylamino)methyl]furo[3,2-c]pyridines (16-23, 26, 27) and their activities as kappa-opioid receptor agonists are described. kappa-Agonist potency was particularly sensitive to thenature of the basic moiety. In particular, in the rabbit vas deferens(kappa-specific tissue), the 3-pyrrolidinol analogue 17 (IC50 = 2.7 nM) was found to be approximately 5-fold more potent than the corresponding pyrrolidine analogue 16 (IC50 15 nM). In the rat and hamster vasadeferentia (mu-specific and delta-specific tissues, respectively), 17showed only weak antagonist activity (PKB > 5.5), underlining its selectivity for the kappa-opioid receptor. The major activity for 17 is resident in the 4S,3'S-isomer 26 (rabbit vas deferens IC50 = 1.1 nM). Compound 26 displays excellent antinociceptive activity, as determined in the mouse acetylcholine-induced abdominal constriction test (ED(50)= 0.001 mg/kg, sc).

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/12/20 alle ore 22:21:34