6β-Naltrexol
6β-Naltrexol, or 6α-hydroxynaltrexone, is a major active metabolite of naltrexone formed by hepatic 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.
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6β-Naltrexol
6β-Naltrexol, or 6α-hydroxynaltrexone, is a major active metabolite of naltrexone formed by hepatic 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.
has abstract
6β-Naltrexol, or 6α-hydroxynal ...... , but was not further pursued.
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CAS number
49625-89-0
FDA UNII code
J0W963M37T
PubChem
Wikipage page ID
44,743,902
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990,026,744
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ATC prefix
None
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CAS number
ChemSpiderID
elimination half-life
IUPAC name
PubChem
SMILES
c1ccO
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StdInChIKey
JLVNEHKORQFVQJ-PYIJOLGTSA-N
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UNII
J0W963M37T
@en
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hypernym
comment
6β-Naltrexol, or 6α-hydroxynal ...... , but was not further pursued.
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label
6β-Naltrexol
@en