| S-methyl N,N-diethylthiolcarbamate sulfone, an in vitro and in vivo inhibitor of rat liver mitochondrial low Km aldehyde dehydrogenase. | |
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MedLine Citation:
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PMID: 8185656 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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S-Methyl N,N-diethylthiolcarbamate sulfone (DETC-Me sulfone) was investigated for its rat liver mitochondrial low Km aldehyde dehydrogenase (ALDH2) inhibitory properties. DETC-Me sulfone inhibited ALDH2 in vitro (IC50 = 3.8 microM) and in vivo (ID50 = 170 mumol/kg; 31 mg/kg). Maximum inhibition (60%) of ALDH2 was observed 8 hr after DETC-Me sulfone administration. In addition, incubation of S-methyl N,N-diethylthiolcarbamate (DETC-Me) or S-methyl N,N-diethylthiolcarbamate sulfoxide (DETC-Me sulfoxide) with rat liver microsomes and an NADPH-generating system failed to produce DETC-Me sulfone. Furthermore, DETC-Me sulfone could not be detected in plasma from rats treated with either DETC-Me sulfoxide or DETC-Me sulfone. In conclusion, DETC-Me sulfone inhibited ALDH2 in vitro and in vivo. However, there was no evidence suggesting that DETC-Me sulfoxide was metabolized to DETC-Me sulfone. |
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Authors:
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S N Nagendra; A Madan; M D Faiman |
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Publication Detail:
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Type: Journal Article; Research Support, U.S. Gov't, P.H.S. |
Journal Detail:
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Title: Biochemical pharmacology Volume: 47 ISSN: 0006-2952 ISO Abbreviation: Biochem. Pharmacol. Publication Date: 1994 Apr |
Date Detail:
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Created Date: 1994-06-14 Completed Date: 1994-06-14 Revised Date: 2007-11-14 |
Medline Journal Info:
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Nlm Unique ID: 0101032 Medline TA: Biochem Pharmacol Country: ENGLAND |
Other Details:
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Languages: eng Pagination: 1465-7 Citation Subset: IM |
Affiliation:
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Department of Pharmacology and Toxicology, University of Kansas Lawrence 60045. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Aldehyde Dehydrogenase
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antagonists & inhibitors* Animals Disulfiram / metabolism Ditiocarb / analogs & derivatives*, chemical synthesis, metabolism, pharmacology Male Mitochondria, Liver / drug effects*, enzymology Oxidation-Reduction Rats Thiocarbamates / metabolism |
| Grant Support | |
ID/Acronym/Agency:
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AA 03577/AA/NIAAA NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/S-methyl-N,N-diethylthiolcarbamate sulfone; 0/Thiocarbamates; 140703-15-7/S-methyl N,N-diethylthiolcarbamate sulfoxide; 147-84-2/Ditiocarb; 37174-63-3/S-methyl diethylthiocarbamate; 97-77-8/Disulfiram; EC 1.2.1.3/Aldehyde Dehydrogenase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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