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The identification of biotransformation products of the new antihypertensive drug urapidil in mouse, rat, dog and man has been performed by means of high-performance liquid chromatographic and mass spectrometric techniques. In urine, three metabolites were found in addition to the unchanged drug. The para-hydroxylated product (1) (6-(3-[4-(o-methoxy-p-hydroxyphenyl)piperazinyl]-propylamino)-1, 3-dimethyl-uracil), the O-demethylated compound (2) (6-(3-[4-(o-hydroxyphenyl)piperazinyl]-propylamino)-1, 3-dimethyluracil) and the uracil-N-dealkylated compound (3) (6-(3-[4-(o-methoxyphenyl)piperazinyl]-propylamino)-1-methyluracil). In urine of dog, the metabolite with the N-oxide structure (5) was also identified, but only in trace amounts (6-(3-[4-(o-methoxyphenyl)piperazinyl-N-oxide]-propylamino)-1, 3-dimethyluracil).
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K Zech
August 1986,
Xenobiotica; the fate of foreign compounds in biological systems,
E Sturm, and
K Zech
February 1984,
Die Pharmazie,
E Sturm, and
K Zech
September 1982,
Il Farmaco; edizione pratica,
E Sturm, and
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January 1978,
Arzneimittel-Forschung,
E Sturm, and
K Zech
January 1983,
Drug metabolism and disposition: the biological fate of chemicals,
E Sturm, and
K Zech
January 1982,
Biomedical mass spectrometry,
E Sturm, and
K Zech
September 1977,
Il Farmaco; edizione scientifica,
E Sturm, and
K Zech
January 1976,
Drug metabolism and disposition: the biological fate of chemicals,
E Sturm, and
K Zech
October 1991,
Arzneimittel-Forschung,
E Sturm, and
K Zech
October 1979,
Xenobiotica; the fate of foreign compounds in biological systems,
