Inhibition of Renal Alkaline Phosphatase by Cimetidine
Autor: | Saeed Minoui, Raheleh Osmani, Sana Alavi, Shiva Ahmadi, Dariush Minai-Tehrani, Somayeh Khodai, Zahra Sobhani-Damavadifar, Somayeh Aminnaseri |
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Rok vydání: | 2011 |
Předmět: |
medicine.medical_specialty
Clinical Biochemistry Pharmaceutical Science Kidney Inhibitory Concentration 50 Mice chemistry.chemical_compound Internal medicine medicine Animals Pharmacology (medical) Cimetidine chemistry.chemical_classification Mice Inbred BALB C Dose-Response Relationship Drug Biochemistry (medical) Antagonist Kidney metabolism Alkaline Phosphatase Endocrinology Enzyme Histamine H2 Antagonists chemistry Alkaline phosphatase Gastric acid Uncompetitive inhibitor Histamine medicine.drug |
Zdroj: | Drug Metabolism Letters. 5:197-201 |
ISSN: | 1872-3128 |
DOI: | 10.2174/187231211796904982 |
Popis: | Alkaline phosphatase (ALP) belongs to hydrolase group of enzymes. It is responsible for removing phosphate groups from many types of molecules, including nucleotides and proteins. Cimetidine (trade name Tagamet) is an antagonist of histamine H2-receptor that inhibits the production of gastric acid. Cimetidine is used for the treatment of gastrointestinal diseases. In this study the inhibitory effect of cimetidine on mouse renal ALP activity was investigated. Our results showed that cimetidine can inhibit ALP by uncompetitive inhibition. In the absence of inhibitor the V(max) and K(m) of the enzyme were found to be 13.7 mmol/mg prot.min and 0.25 mM, respectively. Both the Vmax and Km of the enzyme decreased with increasing cimetidine concentrations (0- 1.2 mM). The Ki and IC(50) of cimetidine were determined to be about 0.5 mM and 0.52 mM, respectively. |
Databáze: | OpenAIRE |
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