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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
10
pubmed:dateCreated
1994-1-25
pubmed:abstractText
The metabolism of mosapride citrate ((+-)-4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2-morpho li nyl] methyl]benzamide citrate, AS-4370, CAS 112885-42-4) was investigated in rats, dogs and monkeys after a single oral administration. Four metabolites, M-1 to M-4, were isolated from rat urine. Two of them were identified as des-p-fluorobenzyl (M-1) and 5'-oxo-des-p-fluorobenzyl mosapride (M-2) and the other two were considered to be as 3-hydroxy des-p-fluorobenzyl (M-3) and 3-hydroxy 5'-oxo-des-p-fluorobenzyl mosapride (M-4) by mass spectrometry and/or nuclear magnetic resonance spectrometry. Metabolites in biological specimens such as plasma and urine after oral administration of [14C]mosapride in rats, dogs and monkeys were analyzed by thin layer chromatography (TLC). Unchanged mosapride, M-1, M-2 and some other metabolites were observed in the plasma of male rats. On the other hand, female rat plasma contained mosapride as the major radioactive component with a small amount of M-1 and little other metabolite(s). In rat urine, irrespective of sex, M-1, M-2, M-3, M-4 and a few other metabolites were observed but the unchanged drug was hardly detected. These facts suggested that the metabolic rate of mosapride was different between sexes in rats. In male rat bile, mosapride, M-1 and polar metabolite(s) were observed. In dogs, mosapride and M-1 were observed as major radioactive components in plasma, and M-1 was seen also as the major metabolite in urine but unchanged drug was hardly detected. Similar results were obtained in monkeys.(ABSTRACT TRUNCATED AT 250 WORDS)
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0004-4172
pubmed:author
pubmed:issnType
Print
pubmed:volume
43
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1095-102
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed-meshheading:8267676-Administration, Oral, pubmed-meshheading:8267676-Animals, pubmed-meshheading:8267676-Benzamides, pubmed-meshheading:8267676-Biotransformation, pubmed-meshheading:8267676-Chromatography, Thin Layer, pubmed-meshheading:8267676-Dogs, pubmed-meshheading:8267676-Female, pubmed-meshheading:8267676-Fetus, pubmed-meshheading:8267676-Gastrointestinal Agents, pubmed-meshheading:8267676-Macaca fascicularis, pubmed-meshheading:8267676-Magnetic Resonance Spectroscopy, pubmed-meshheading:8267676-Male, pubmed-meshheading:8267676-Mass Spectrometry, pubmed-meshheading:8267676-Maternal-Fetal Exchange, pubmed-meshheading:8267676-Milk, pubmed-meshheading:8267676-Morpholines, pubmed-meshheading:8267676-Pregnancy, pubmed-meshheading:8267676-Rats, pubmed-meshheading:8267676-Rats, Wistar, pubmed-meshheading:8267676-Sex Characteristics, pubmed-meshheading:8267676-Species Specificity
pubmed:year
1993
pubmed:articleTitle
Metabolism of [carbonyl-14C]mosapride citrate after a single oral administration in rats, dogs and monkeys.
pubmed:affiliation
Developmental Research Laboratories, Dainippon Pharmaceutical Co., Ltd., Osaka, Japan.
pubmed:publicationType
Journal Article, Comparative Study