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THE PHARMACOLOGY OF ISAMOXOLE [2‐METHYL‐ N ‐BUTYL‐ N (4‐METHYLOXAZOL‐2‐YL) PROPANAMIDE] LRCL 3950, A NEW ANTI‐ALLERGIC COMPOUND
Author(s) -
DAWSON W.,
SWEATMAN W.J.F.
Publication year - 1980
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.1476-5381.1980.tb10951.x
Subject(s) - guinea pig , histamine , bronchoconstriction , pharmacology , in vivo , bradykinin , in vitro , chemistry , anaphylaxis , compound 48/80 , ileum , medicine , allergy , immunology , biology , biochemistry , endocrinology , degranulation , asthma , receptor , microbiology and biotechnology
1 Isamoxole [2‐methyl‐ N ‐butyl‐ N (4‐methyloxazol‐2‐yl) propanamide] is an effective orally active anti‐allergic compound in animals. 2 Isamoxole inhibits the immunological release of mediators, notably slow‐reacting substance of anaphylaxis (SRS‐A) from sensitized human and guinea‐pig chopped lung in vitro.3 In vivo , allergic responses were inhibited in guinea‐pigs and rats by doses as low as 25 mg/kg given orally 180 and 30 min before challenge. The effect of Isamoxole was still present 4 h after a single dose of 100 mg/kg orally in the guinea‐pig and 3 h in the rat. 4 Isamoxole is a moderately potent, selective inhibitor of SRS‐A activity on the guinea‐pig ileum in vitro , at concentrations that do not antagonize histamine, 5‐hydroxytryptamine, or bradykinin. 5 Isamoxole causes human bronchial muscle to relax and antagonizes the bronchoconstriction induced by SRS‐A.