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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
7
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pubmed:dateCreated |
1980-10-24
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pubmed:abstractText |
A variety of substituent groups has been attached to the exocyclic imine function of 2-imino-3-methylthiazolidine (1) in a search for metabolic precursors of this potent inhibitor of the enzyme indoleethylamine N-methyltransferase (INMT) which would exhibit superior pharmacodynamic properties in animals. It has been determined that chemically stable derivatives of 1 based on succinic, nicotinic, and N-acylated amino acids, although they lack in vitro efficacy, are potent inhibitors of INMT when administered orally or intravenously to rabbits. Metabolic studies carried out with 14C-labeled N,N'-bix(3-methyl-2-thiazolidinylidene)succinamide (3) have established that conversion of this compound to 1 occurs both in the whole rabbit and in the isolated rabbit liver. 1 itself has been shown to be metabolically inert in rabbits, being excreted primarily in the urine.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
23
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
773-80
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:7401104-Administration, Oral,
pubmed-meshheading:7401104-Animals,
pubmed-meshheading:7401104-Biotransformation,
pubmed-meshheading:7401104-Humans,
pubmed-meshheading:7401104-Imines,
pubmed-meshheading:7401104-Injections, Intravenous,
pubmed-meshheading:7401104-Liver,
pubmed-meshheading:7401104-Lung,
pubmed-meshheading:7401104-Male,
pubmed-meshheading:7401104-Methyltransferases,
pubmed-meshheading:7401104-Rabbits,
pubmed-meshheading:7401104-Thiazoles,
pubmed-meshheading:7401104-Tissue Distribution,
pubmed-meshheading:7401104-Tryptamines
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pubmed:year |
1980
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pubmed:articleTitle |
Inhibitors of indoleethylamine N-methyltransferase. Derivatives of 3-methyl-2-thiazolidinimine. In vitro, in vivo, and metabolic studies.
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pubmed:publicationType |
Journal Article,
In Vitro
|