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6β-Naltrexol : ウィキペディア英語版 | 6β-Naltrexol
6β-Naltrexol, or 6α-hydroxynaltrexone, is a major active metabolite of naltrexone formed by hepatic dihydrodiol dehydrogenase which acts as a potent, peripherally-selective opioid neutral antagonist. Relative to naltrexone, 6β-naltrexol has about half the affinity for the μ-opioid receptor,〔 but is present at approximately 10–30-fold higher concentrations at steady state due to extensive first-pass metabolism of the parent drug. 6β-Naltrexol was itself investigated as an opioid antagonist, specifically for the treatment of opioid-induced constipation, and was found to be effective and well-tolerated, but was not further pursued.〔 ==See also==
* 6β-Naltrexol-d4
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