Studies on the anti-allergic action of N-(3',4'-dimethoxycinnamoyl) anthranilic acid (N-5').
The effects of the anti-allergic compound (N-(3',4'-dimethoxycinnamoyl) anthranilic acid (N-5' or Tranilast) have been investigated upon antigen-induced contractions of respiratory smooth muscle in vitro and bronchoconstriction in vivo. N-5' (3.1 X 10(-5) M) in vitro had no significant effect upon antigen-induced contractions of the guinea pig trachea. However, when tested at concentrations of 9.2 and 3.1 X 10(-5) M, but not 0.9 X 10(-5), N-5' significantly inhibited antigen-induced contractions of the human parenchyma. In vivo N-5' (5 and 10 mg/kg p.o.) failed to inhibit antigen-induced dyspnea in hyperreactive rats. N-5' (20 mg/kg p.o.) also failed to inhibit the immediate bronchoconstriction following ascaris challenge of conscious squirrel monkeys but significantly attenuated the reduction in dynamic compliance during the pulmonary late phase response observed between 4 and 10 h after antigen challenge. It is suggested that N-5' does not act as a "cromoglycate-like" compound but may have novel mechanisms of action in human bronchial asthma.
D000403:Airway Resistance / Q000187:drug effects; D000818:Animals; D001986:Bronchial Spasm / Q000188:drug therapy / Q000503:physiopathology; D004305:Dose-Response Relationship, Drug; D004417:Dyspnea / Q000188:drug therapy / Q000209:etiology; D006168:Guinea Pigs; D006801:Humans; D007114:Immunization; D066298:In Vitro Techniques; D008168:Lung / Q000187:drug effects / Q000276:immunology / Q000503:physiopathology; D008170:Lung Compliance / Q000187:drug effects; D008297:Male; D051381:Rats; D012130:Respiratory Hypersensitivity / Q000188:drug therapy* / Q000503:physiopathology; D012453:Saimiri; D014132:Trachea / Q000187:drug effects / Q000276:immunology / Q000503:physiopathology; D062367:ortho-Aminobenzoates / Q000494:pharmacology / Q000627:therapeutic use*
D062367:ortho-Aminobenzoates; C012293:tranilast