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[Inhibition of microsomal enzyme activity of the liver by various H2 receptor antagonists].
Z Gastroenterol. 1987 Feb; 25(2):112-8.ZG

Abstract

The inhibition of 7-ethoxycoumarin deethylase activity by four different H2-receptor antagonists was studied using rat liver microsomes. The compounds tested represent two classes of H2-antagonists, i. e. structures with (cimetidine and oxmetidine) and without (ranitidine and SKF 93479) an imidazole ring. The microsomes were prepared from untreated and phenobarbital-treated animals. It was found that all four compounds, even those without an imidazole ring, inhibited deethylase activity. The compounds inhibited in the following order: SKF 93479 (90%) greater than cimetidine (58%) = oxmetidine (58%) greater than ranitidine (23%). In microsomes from phenobarbital-induced animals, the inhibitory activity of oxmetidine was increased 5-fold. Only the inhibitory potency of cimetidine was increased by preincubation of the H2-antagonist with the microsomes prior to the addition of the substrate.

Authors

Jensen JC
No affiliation info available
Gugler R
No affiliation info available

MeSH

7-Alkoxycoumarin O-DealkylaseAnimalsCimetidineCulture TechniquesHistamine H2 AntagonistsImidazolesMaleMicrosomes, LiverOxygenasesPyrimidinonesRanitidineRatsRats, Inbred StrainsStructure-Activity Relationship

Pub Type(s)

Comparative Study
English Abstract
Journal Article
Research Support, Non-U.S. Gov't

Language

ger

PubMed ID

2882636

Citation

Jensen, J C., and R Gugler. "[Inhibition of Microsomal Enzyme Activity of the Liver By Various H2 Receptor Antagonists]." Zeitschrift Fur Gastroenterologie, vol. 25, no. 2, 1987, pp. 112-8.
Jensen JC, Gugler R. [Inhibition of microsomal enzyme activity of the liver by various H2 receptor antagonists]. Z Gastroenterol. 1987;25(2):112-8.
Jensen, J. C., & Gugler, R. (1987). [Inhibition of microsomal enzyme activity of the liver by various H2 receptor antagonists]. Zeitschrift Fur Gastroenterologie, 25(2), 112-8.
Jensen JC, Gugler R. [Inhibition of Microsomal Enzyme Activity of the Liver By Various H2 Receptor Antagonists]. Z Gastroenterol. 1987;25(2):112-8. PubMed PMID: 2882636.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - [Inhibition of microsomal enzyme activity of the liver by various H2 receptor antagonists]. AU - Jensen,J C, AU - Gugler,R, PY - 1987/2/1/pubmed PY - 1987/2/1/medline PY - 1987/2/1/entrez SP - 112 EP - 8 JF - Zeitschrift fur Gastroenterologie JO - Z Gastroenterol VL - 25 IS - 2 N2 - The inhibition of 7-ethoxycoumarin deethylase activity by four different H2-receptor antagonists was studied using rat liver microsomes. The compounds tested represent two classes of H2-antagonists, i. e. structures with (cimetidine and oxmetidine) and without (ranitidine and SKF 93479) an imidazole ring. The microsomes were prepared from untreated and phenobarbital-treated animals. It was found that all four compounds, even those without an imidazole ring, inhibited deethylase activity. The compounds inhibited in the following order: SKF 93479 (90%) greater than cimetidine (58%) = oxmetidine (58%) greater than ranitidine (23%). In microsomes from phenobarbital-induced animals, the inhibitory activity of oxmetidine was increased 5-fold. Only the inhibitory potency of cimetidine was increased by preincubation of the H2-antagonist with the microsomes prior to the addition of the substrate. SN - 0044-2771 UR - https://www.unboundmedicine.com/medline/citation/2882636/[Inhibition_of_microsomal_enzyme_activity_of_the_liver_by_various_H2_receptor_antagonists]_ DB - PRIME DP - Unbound Medicine ER -