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Drug metabolism letters · 2014

Inhibition and structural changes of liver alkaline phosphatase by tramadol.

СтатьяНазвание и аннотация: Перевод в очереди
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Minai-Tehrani Dariush, Eslami Mahya, Khazaei Nafsa, Katebian Elmira, Azizi Leila, Yazdi Fatemeh, Hosseini Akram Sadat, Taheri Mohammadreza

Аннотация

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 effect 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 the alteration in the content of secondary structures and also conformational changes in enzyme occurred when the drug bound to enzyme-substrate complex.

Предметные рубрики MeSH

ИП Урсолов Владлен Сергеевич

ИНН 500118482352 · ОГРНИП 314500117700049

Реквизиты и контакты