Tags

Type your tag names separated by a space and hit enter

S-methyl N,N-diethylthiolcarbamate sulfone, an in vitro and in vivo inhibitor of rat liver mitochondrial low Km aldehyde dehydrogenase.
Biochem Pharmacol. 1994 Apr 20; 47(8):1465-7.BP

Abstract

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.

Links

Publisher Full Text

Authors+Show Affiliations

Nagendra SN
Department of Pharmacology and Toxicology, University of Kansas Lawrence 60045.
Madan A
No affiliation info available
Faiman MD
No affiliation info available

MeSH

Aldehyde DehydrogenaseAnimalsDisulfiramDitiocarbMaleMitochondria, LiverOxidation-ReductionRatsThiocarbamates

Pub Type(s)

Journal Article
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

8185656

Citation

Nagendra, S N., et al. "S-methyl N,N-diethylthiolcarbamate Sulfone, an in Vitro and in Vivo Inhibitor of Rat Liver Mitochondrial Low Km Aldehyde Dehydrogenase." Biochemical Pharmacology, vol. 47, no. 8, 1994, pp. 1465-7.
Nagendra SN, Madan A, Faiman MD. S-methyl N,N-diethylthiolcarbamate sulfone, an in vitro and in vivo inhibitor of rat liver mitochondrial low Km aldehyde dehydrogenase. Biochem Pharmacol. 1994;47(8):1465-7.
Nagendra, S. N., Madan, A., & Faiman, M. D. (1994). S-methyl N,N-diethylthiolcarbamate sulfone, an in vitro and in vivo inhibitor of rat liver mitochondrial low Km aldehyde dehydrogenase. Biochemical Pharmacology, 47(8), 1465-7.
Nagendra SN, Madan A, Faiman MD. S-methyl N,N-diethylthiolcarbamate Sulfone, an in Vitro and in Vivo Inhibitor of Rat Liver Mitochondrial Low Km Aldehyde Dehydrogenase. Biochem Pharmacol. 1994 Apr 20;47(8):1465-7. PubMed PMID: 8185656.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - S-methyl N,N-diethylthiolcarbamate sulfone, an in vitro and in vivo inhibitor of rat liver mitochondrial low Km aldehyde dehydrogenase. AU - Nagendra,S N, AU - Madan,A, AU - Faiman,M D, PY - 1994/4/20/pubmed PY - 1994/4/20/medline PY - 1994/4/20/entrez SP - 1465 EP - 7 JF - Biochemical pharmacology JO - Biochem Pharmacol VL - 47 IS - 8 N2 - 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. SN - 0006-2952 UR - https://www.unboundmedicine.com/medline/citation/8185656/S_methyl_NN_diethylthiolcarbamate_sulfone_an_in_vitro_and_in_vivo_inhibitor_of_rat_liver_mitochondrial_low_Km_aldehyde_dehydrogenase_ L2 - https://linkinghub.elsevier.com/retrieve/pii/0006-2952(94)90350-6 DB - PRIME DP - Unbound Medicine ER -