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Titolo:
FPL-14294 - A NOVEL CCK-8 AGONIST WITH POTENT INTRANASAL ANORECTIC ACTIVITY IN THE RAT
Autore:
SIMMONS RD; BLOSSER JC; ROSAMOND JR;
Indirizzi:
FISONS PHARMACEUT PLC,DEPT BIOCHEM ROCHESTER NY 14603 FISONS PHARMACEUT PLC,DEPT MED CHEM ROCHESTER NY 14603
Titolo Testata:
Pharmacology, biochemistry and behavior
fascicolo: 3, volume: 47, anno: 1994,
pagine: 701 - 708
SICI:
0091-3057(1994)47:3<701:F-ANCA>2.0.ZU;2-W
Fonte:
ISI
Lingua:
ENG
Soggetto:
CHOLECYSTOKININ OCTAPEPTIDE CCK-8; DECREASES FOOD-INTAKE; GUINEA-PIG; RECEPTORS; BINDING; GASTRIN; CELLS; GALLBLADDER; ANTAGONIST; L-364,718;
Keywords:
CHOLECYSTOKININ; OCTAPEPTIDE; FLP 14294; ANORECTIC ACTIVITY; INTRANASAL; CCK-A RECEPTOR; CCK-B RECEPTOR; AGONIST; ANTAGONIST;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
47
Recensione:
Indirizzi per estratti:
Citazione:
R.D. Simmons et al., "FPL-14294 - A NOVEL CCK-8 AGONIST WITH POTENT INTRANASAL ANORECTIC ACTIVITY IN THE RAT", Pharmacology, biochemistry and behavior, 47(3), 1994, pp. 701-708

Abstract

Cholecystokinin octapeptide (CCK-I) induces satiety in many species including man. However, its therapeutic utility is restricted due to its short biological half-life and poor bioavailability. FPL 14294 [4-(sulfoxy)-phenylacetyl(MePhe6)CCK-6] is a CCK analog with enhanced metabolic stability that was comparable to CCK-8 in potency to contract isolated gallbladder and in affinity at the CCK-A and CCK-B receptor. However, FPL 14294 was more than 200 times more potent than CCK-8 in inhibiting 3-h feeding in 21-h fasted rats. FPL 14294 also possessed intranasal anorectic activity at 5 mu g/kg, while CCK-I was inactive at doses up to 500 mu g/kg. Anorectic activity was inhibited by pretreatmentwith a CCK-A antagonist (MK-329) but not by a CCK-B antagonist (L365,260). The anorectic effects of CCK-I and FPL 14294 were the result of a direct effect on feeding and not caused indirectly by effects on water intake. These results indicate that FPL 14294 is a potent, intranasally active, anorectic agent whose enhanced in vivo potency over that of CCK-I may reflect differences in stability, bioavailability, or receptor kinetics.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 29/11/20 alle ore 00:28:04