6β-Naltrexol
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| Elimination half-life | 12–18 hours[1] |
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| ECHA InfoCard | 100.230.713 |
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| Formula | C20H25NO4 |
| Molar mass | 343.423 g·mol−1 |
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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.[2][3] Relative to naltrexone, 6β-naltrexol has about half the affinity for the μ-opioid receptor,[1] but is present at approximately 10–30-fold higher concentrations at steady state due to extensive first-pass metabolism of the parent drug.[4] 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.[2]
See also
References
- ^ a b Dean R, Bilsky EJ, Negus SS (12 March 2009). Opiate Receptors and Antagonists: From Bench to Clinic. Springer Science & Business Media. pp. 269–. ISBN 978-1-59745-197-0.
- ^ a b Smith HS (21 February 2013). Opioid Therapy in the 21st Century. Oxford University Press. pp. 69–. ISBN 978-0-19-984497-5.
- ^ Cote CJ, Lerman J, Anderson BJ (2013). A Practice of Anesthesia for Infants and Children: Expert Consult - Online and Print. Elsevier Health Sciences. pp. 148–. ISBN 1-4377-2792-1.
- ^ Davis MP, Glare PA, Hardy J (28 May 2009). Opioids in Cancer Pain. Oxford University Press. pp. 41–. ISBN 978-0-19-923664-0.
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