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Titolo:
ANTIBRONCHOSPASTIC ACTIVITY OF MEN10,627, A NOVEL TACHYKININ NK2 RECEPTOR ANTAGONIST, IN GUINEA-PIG AIRWAYS
Autore:
PERRETTI F; BALLATI L; MANZINI S; MAGGI CA; EVANGELISTA S;
Indirizzi:
IST FARMACOBIOL MALESCI SPA,DEPT PHARMACOL,VIA PORPORA 22 I-50144 FLORENCE ITALY IST FARMACOBIOL MALESCI SPA,DEPT PHARMACOL I-50144 FLORENCE ITALY MENARINI SUD,DEPT PHARMACOL POMEZIA ITALY MENARINI PHARMACEUT,DEPT PHARMACOL FLORENCE ITALY
Titolo Testata:
European journal of pharmacology
fascicolo: 1-2, volume: 273, anno: 1995,
pagine: 129 - 135
SICI:
0014-2999(1995)273:1-2<129:AAOMAN>2.0.ZU;2-X
Fonte:
ISI
Lingua:
ENG
Soggetto:
INDUCED BRONCHIAL HYPERRESPONSIVENESS; SUBSTANCE-P; INDUCED BRONCHOCONSTRICTION; NEUROGENIC INFLAMMATION; NEUTRAL ENDOPEPTIDASE; CAPSAICIN; POTENT; ACCUMULATION; CP-96,345; AGONISTS;
Keywords:
BRONCHOSPASM; (+/-)-CP96,345; MEN10,627; NEUROKININ A; PAF (PLATELET-ACTIVATING FACTOR); SUBSTANCE P; TACHYKININ;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
22
Recensione:
Indirizzi per estratti:
Citazione:
F. Perretti et al., "ANTIBRONCHOSPASTIC ACTIVITY OF MEN10,627, A NOVEL TACHYKININ NK2 RECEPTOR ANTAGONIST, IN GUINEA-PIG AIRWAYS", European journal of pharmacology, 273(1-2), 1995, pp. 129-135

Abstract

The antibronchospastic activity against acetylcholine, antigen, histamine plus platelet-activating factor (PAF) or the selective tachykininneurokinin (NK)(1) and NK2 receptor agonists of the novel tachykinin NK2 receptor antagonist, MEN10,627 (cyclo(Met-Asp-Trp-Phe-Dap-Leu)cyclo(2 beta-5 beta)), was studied in anesthetized guinea-pigs. MEN10,627 (30-100 nmol/kg i.v.) reduced in a dose-dependent manner the bronchospasm induced by the tachykinin NK2 receptor agonist [beta Ala(8)]neurokinin A-(4-10) and the effect of the highest dose lasted up to 5 h fromits administration. Conversely, airway constriction induced by the NK1 receptor agonist [Sar(9)]substance P sulfone or acetylcholine was unaffected by MEN10,627 up to a dose of 3 mu mol/kg i.v. In animals sensitized with ovalbumin and pretreated with the endopeptidase inhibitor phosphoramidon, the aerosolized antigen produced a bronchospasm which was inhibited by MEN10,627 (30-100 nmol/kg i.v.) but not by the tachykinin NK1 receptor antagonist, (+/-)-CP96,345 ([2R,3R-cis- and phenyl)-methyl]-1-azabicyclo[2.2.2]octan-3-amine]) (3 mu mol/kg i.v.). Both MEN10,627 (30-100 nmol/kg i.v.) and (+/-)-CP96,345 (30-300 nmol/kg i.v.)reduced the PAF-induced hyperresponsiveness to histamine, without affecting the hypotension induced by PAF or the bronchospasm induced by histamine in guinea-pigs not exposed to PAF, showing the involvement ofboth tachykinin NK1 and NK2 receptors in this model. In summary, MEN10,627 behaves as a potent, selective and long-lasting tachykinin NK2 receptor antagonist in vivo. Further, tachykinin NK2 receptors could beactivated during allergic responses and in the development of airway hyperresponsiveness.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/09/20 alle ore 18:28:19