Document Detail


Inhibition of leukotriene-induced contraction of guinea pig trachea by 5-lipoxygenase inhibitors.
MedLine Citation:
PMID:  3108959     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The effects of the 5-lipoxygenase inhibitors nordihydroguiaretic acid (NDGA), 5, 8, 11, 14-eicosatetraynoic acid (ETYA), 1-phenyl-3-pyrazolidone (phenidone) and BW-755c, on the contractile response to LTC4 or LTD4 were examined on the isolated guinea pig trachea. Responses to either LTC4 or LTD4 were obtained on indomethacin treated tissues, in the presence of either L-serine-borate complex or L-cysteine, respectively, to inhibit metabolic conversion of the leukotrienes. NDGA (30 microM) and ETYA (100 microM) produced a selective competitive antagonism of LTD4-induced contractions, while phenidone antagonized both LTC4- and LTD4-induced responses in a non-competitive manner. In contrast, BW-755c (30 microM) did not significantly antagonize LTC4 or LTD4 concentration-response curves. The results suggest that leukotriene antagonism may be produced by large concentrations of some 5-lipoxygenase inhibitors.
Authors:
S F Schwalm; A J Lewis; J M Hand
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Prostaglandins     Volume:  33     ISSN:  0090-6980     ISO Abbreviation:  Prostaglandins     Publication Date:  1987 Jan 
Date Detail:
Created Date:  1987-07-01     Completed Date:  1987-07-01     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0320271     Medline TA:  Prostaglandins     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  113-9     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
4,5-Dihydro-1-(3-(trifluoromethyl)phenyl)-1H-pyrazol-3-amine
5,8,11,14-Eicosatetraynoic Acid / pharmacology
Animals
Arachidonate 5-Lipoxygenase / antagonists & inhibitors*
Arachidonate Lipoxygenases / antagonists & inhibitors*
Guinea Pigs
Muscle Contraction / drug effects
Muscle, Smooth / drug effects,  physiology
Nordihydroguaiaretic Acid / pharmacology
Pyrazoles / pharmacology
SRS-A / antagonists & inhibitors,  physiology*
Trachea / drug effects,  physiology*
Chemical
Reg. No./Substance:
0/Pyrazoles; 0/SRS-A; 1191-85-1/5,8,11,14-Eicosatetraynoic Acid; 500-38-9/Nordihydroguaiaretic Acid; 66000-40-6/4,5-Dihydro-1-(3-(trifluoromethyl)phenyl)-1H-pyrazol-3-amine; 92-43-3/phenidone; EC 1.13.11.-/Arachidonate Lipoxygenases; EC 1.13.11.34/Arachidonate 5-Lipoxygenase

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


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