Document Detail


Bronchodilating effect of KC-404, a novel anti-asthmatic agent, and its derivatives in monkey.
MedLine Citation:
PMID:  3800509     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The inhibitory effect of 3-isobutyryl-2-isopropylpyrazolo[1,5-alpha]pyridine (KC-404) on aerosolized methacholine- and histamine-induced increase in total respiratory resistance (Rrs) was determined in monkeys using the forced 3 Hz oscillation method and was compared with the effect of aminophylline. The effects of several derivatives of KC-404 on methacholine-induced bronchoconstriction were also determined. All of the i.v. administered pyrazolopyridine derivatives showed an inhibition of the increase in Rrs induced by aerosolized methacholine. Among these derivatives, KC-404 exerted the most potent bronchodilating effect. KC-404 also inhibited the histamine-induced increase in Rrs. These effects of KC-404 were more potent than those of aminophylline. On the other hand, the dose of KC-404 tested caused an increase in heart rate, although the degree was moderate as compared with aminophylline. From the results obtained in this study, it is considered that the pyrazolopyridine derivatives, particularly KC-404, may be promising bronchodilators for the treatment of bronchial asthma.
Authors:
S Mue; T Ishihara; W Hida; K Sekizawa; G Tamura; K Yamauchi; H Ohtsu; T Takishima
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Archives internationales de pharmacodynamie et de thérapie     Volume:  283     ISSN:  0003-9780     ISO Abbreviation:  Arch Int Pharmacodyn Ther     Publication Date:  1986 Sep 
Date Detail:
Created Date:  1987-01-28     Completed Date:  1987-01-28     Revised Date:  2012-01-12    
Medline Journal Info:
Nlm Unique ID:  0405353     Medline TA:  Arch Int Pharmacodyn Ther     Country:  BELGIUM    
Other Details:
Languages:  eng     Pagination:  153-62     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Airway Resistance / drug effects
Aminophylline / pharmacology
Anesthesia
Animals
Bronchodilator Agents*
Female
Heart Rate / drug effects
Histamine / pharmacology
Macaca
Male
Methacholine Compounds / pharmacology
Pyridines / pharmacology*
Chemical
Reg. No./Substance:
0/Bronchodilator Agents; 0/Methacholine Compounds; 0/Pyridines; 317-34-0/Aminophylline; 50847-11-5/ibudilast; 51-45-6/Histamine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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