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Drug Metabolism Letters
ISSN (Print): 1872-3128
ISSN (Online): 1874-0758
Epub Full Text Article
DOI: 10.2174/1872312808666140506093756      Price:  $95









Inhibition and Structural Changes of Liver Alkaline Phosphatase by Tramadol

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Author(s): Dariush Minai-Tehrani
Abstract:
Tramadol is a potent analgesic drug which interacts with mu-opioid and has low effect on other opioid receptors. Unlike other opioids, it has no clinically significant effects on respiratory or cardiovascular parameters. Alakaline phosphatase is a hydrolase enzyme that prefers alkaline condition and removes phosphate group from different substrates. In this study, the interaction between tramadol and calf liver alkaline phosphatase was investigated. The results showed that tramadol can bind to alakaline phosphatase and inhibit the enzyme in an un-competitive manner. Ki and IC50 values of tramadol were determined as about 91 and 92 μM, respectively. After enzyme purification, structural changes on alakaline phosphatase-drug interaction were studied by circular dichroism and fluorescence measurement. These data revealed that the alteration in the content of secondary structures and also conformational changes in enzyme occurred when the drug bound to enzyme-substrate complex
Keywords:
Conformational changes, drug, enzyme, inhibition
Affiliation:
Bioresearch Lab, Faculty of Biological sciences, Shahid Beheshti University, Iran