1476760-57-2Relevant academic research and scientific papers
BENZAMIDE DERIVATIVE
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Paragraph 0914; 0915, (2015/03/16)
The present invention relates to benzamide derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.
Pharmacokinetic studies of mabuterol, a new selective β2-stimulant. II: Urinary metabolites of mabuterol in rats and their pharmacological effects
Horiba,Murai,Nomura,Yuge,Sanai,Osada
, p. 1668 - 1679 (2007/10/02)
A selective β2-stimulating bronchodilator, dl-1-(4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-tert.-butylamino-ethano l hydrochloride (mabuterol), is mainly metabolized by the oxidative deamination pathway. Unchanged mabuterol and the following 6 types of metabolites, M-1 (hydroxylation of tert.-butyl group), M-2 (glycol), M-3 (mandelic acid), M-4 (aldehyde), M-5 (benzoic acid) and M-6 (hippuric acid) were identified by thin-layer chromatography and mass spectroscopy. Pharmacologically, only M-1 had effects on the airway resistance, blood pressure and heart rate, and the isolated organs. But its selective β2-stimulating effect was 2-10 times lower than that of mabuterol. M-1 antagonized the positive inotropic action induced by isoprenaline (isoproterenol). Other metabolites showed no appreciable activity.
