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Titolo:
EFFECT OF BAY-X-7195, AN ORAL RECEPTOR ANTAGONIST OF CYSTEINYL-LEUKOTRIENES, ON LEUKOTRIENE-D-4 INDUCED BRONCHOCONSTRICTION IN NORMAL VOLUNTEERS
Autore:
WENSING G; HEINIG R; PRIESNITZ M; KUHLMANN J;
Indirizzi:
BAYER AG,INST CLIN PHARMACOL INT,RES & DEV,PHARMA D-42096 WUPPERTAL GERMANY
Titolo Testata:
European Journal of Clinical Pharmacology
fascicolo: 3, volume: 47, anno: 1994,
pagine: 227 - 230
SICI:
0031-6970(1994)47:3<227:EOBAOR>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
INHALED LEUKOTRIENE-D4; D4-INDUCED BRONCHOCONSTRICTION; URINARY LEUKOTRIENE-E4; AIRWAY RESPONSIVENESS; ASTHMA; METHACHOLINE; INHALATION; CHALLENGE; HISTAMINE; RELEASE;
Keywords:
BAY X 7195; LEUKOTRIENE D-4 BRONCHIAL CHALLENGE, PHARMACODYNAMICS, CONCENTRATION-EFFECT RELATIONSHIP;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
20
Recensione:
Indirizzi per estratti:
Citazione:
G. Wensing et al., "EFFECT OF BAY-X-7195, AN ORAL RECEPTOR ANTAGONIST OF CYSTEINYL-LEUKOTRIENES, ON LEUKOTRIENE-D-4 INDUCED BRONCHOCONSTRICTION IN NORMAL VOLUNTEERS", European Journal of Clinical Pharmacology, 47(3), 1994, pp. 227-230

Abstract

Leukotrienes (LT) have been proposed to play an important role in thepathogenesis of asthma. This paper reports the results of two studiesinvestigating the effect of BAY x 7195, a new oral receptor antagonist of cysteinyl-leukotrienes, on LTD(4)-induced bronchoconstriction in healthy male volunteers. Using a double-blind, placebo-controlled, crossover design, volunteers received 250 mg (n = 6; study 1) and 100 and500 mg (n = 6; study 2) of BAY x 7195. Bronchoprovocation with nebulized LTD, was performed 2 (250 mg) and 2 and 8 (100 and 500 mg) h p. a. The specific airway's conductance (SGaw) was used to assess the airway's response. Blood samples to determine plasma concentrations of BAY x 7195 were taken at the end of bronchoprovocation. BAY x 7195 showed no effect on baseline lung function. Compared to placebo, the different doses of BAY x 7195 increased the concentration of LTD(4) needed to produce a 35% decrease in SGaw 2 h p. a. between 1- and 23-fold. Eighthours p. a., 100 and 500 mg caused shifts in the concentration-response curve of between 1- and 13-fold. There was no predictive relationship between plasma concentrations of BAY x 7195 and the response to LTD(4) challenge. However, there was a relationship between dose and effect. No relevant adverse effects were reported. In conclusion, the present results suggest that BAY x 7195 is an effective LTD(4)-receptor antagonist in man.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/09/20 alle ore 16:38:44