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Titolo:
PHARMACOLOGICAL CHARACTERIZATION OF A NOVEL LONG-ACTING HISTAMINE H-1RECEPTOR ANTAGONIST, KAA-276
Autore:
KOBAYASHI T; TAKEHANA Y; SHINAGAWA K; TSUYUKI S; TOKUTAKE Y; SATO M; MOMOSE D;
Indirizzi:
KISSEI PHARMACEUT CO LTD,CENT RES LAB,4365-1 KASHIWABARA MINAMIAZUMI NAGANO 3998304 JAPAN KISSEI PHARMACEUT CO LTD,CENT RES LAB MINAMIAZUMI NAGANO 3998304 JAPAN
Titolo Testata:
Biological & pharmaceutical bulletin
fascicolo: 4, volume: 21, anno: 1998,
pagine: 350 - 355
SICI:
0918-6158(1998)21:4<350:PCOANL>2.0.ZU;2-D
Fonte:
ISI
Lingua:
ENG
Soggetto:
NON-SEDATING ANTIHISTAMINE; ALLERGIC RHINITIS; PSEUDOEPHEDRINE; TRIPROLIDINE; ASTEMIZOLE;
Keywords:
HISTAMINE; ANTIHISTAMINE; AEROSOL; BRONCHOCONSTRICTION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
22
Recensione:
Indirizzi per estratti:
Citazione:
T. Kobayashi et al., "PHARMACOLOGICAL CHARACTERIZATION OF A NOVEL LONG-ACTING HISTAMINE H-1RECEPTOR ANTAGONIST, KAA-276", Biological & pharmaceutical bulletin, 21(4), 1998, pp. 350-355

Abstract

The pharmacological profile of a newly synthesized histamine H-1 receptor antagonist, KAA-276 (1-[1-(4-fluorophenylmethyl) thyl)-phenyl]ethyl]-1,5-diazacyclooctane-sulfate), was characterized. In a H-1 receptor binding assay in vitro, KAA-276 inhibited [H-3]mepyramine binding toguinea pig cerebellar membrane preparations with an IC50 of 0.66 nM. The inhibitory potency of KAA-276 was greater than that of terfenadine, but similar to that of astemizole and ketotifen. KAA-276 antagonizedthe histamine-induced constriction of ileum and trachea isolated fromguinea pigs in a dose-dependent manner with a concomitant reduction in the maximum response. Furthermore, the inhibitory effect of KAA-276 on histamine induced contraction was potentiated depending on the duration of preincubation time and revealed an irreversible property. KAA-276 given orally, intraduodenally, and by inhalation significantly inhibited histamine-induced bronchoconstriction dose-dependently in guinea pigs. Inhalation of KAA-276 exhibited inhibitory activity with a rapid onset and long duration, while intraduodenal administration resulted in action with a slow onset. Therefore, KAA-276, an irreversible andselective histamine H-1 receptor antagonist, was shown to be a usefuldrug for therapeutic strategies against bronchial asthma when administered by the aerosol route.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/09/18 alle ore 09:11:22