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Effects of l ‐serine borate on antagonism of leukotriene C 4 ‐induced contractions of guinea‐pig trachea
Author(s) -
Charette L.,
Jones T.R.
Publication year - 1987
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1987.tb08997.x
Subject(s) - antagonist , ibmx , nifedipine , aminophylline , antagonism , chemistry , guinea pig , receptor antagonist , endocrinology , medicine , yohimbine , pharmacology , receptor , biology , calcium , biochemistry , forskolin
1 The antagonist activity of three leukotriene D 4 (LTD 4 ) receptor antagonists and a number of bronchodilators was determined against LTC 4 ‐induced contractions of guinea‐pig isolated tracheal chains in the absence and presence of the γ‐glutamyltranspeptidase inhibitor, l ‐serine borate (SB). 2 The LTD 4 receptor antagonists FPL‐55712, L‐649,923 and L‐648,051 effectively antagonized LTC 4 responses in the absence of SB but were ineffective in the presence of 15 and/or 45 m m SB. 3 Salbutamol > isobutylmethylxanthine (IBMX) > dibutyryl cyclic AMP > aminophylline > nifedipine antagonized contractions to LTC 4 in the absence of SB. In contrast, in the presence of SB the antagonist activity of all of these agents except nifedipine was significantly reduced. The antagonist activity of the Ca 2+ entry blocker, nifedipine, was similar in the absence and presence of SB. 4 Salbutamol and IBMX were potent functional antagonists of LTE 4 ‐induced contractions both in the absence and presence of SB. 5 These results are consistent with the hypothesis that there are contractile LTC 4 receptor mechanisms in guinea‐pig trachea which are unmasked by SB and are not blocked by LTD 4 receptor antagonists and which are less effectively down modulated by cyclic AMP‐dependent bronchodilators.