6β-Naltrexol
Clinical data | |
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Other names | 6beta-Naltrexol; 6β-Hydroxynaltrexone; AIKO-150; 17-(Cyclopropylmethyl)-4,5α-epoxymorphinan-3,6α,14-triol |
Drug class | Opioid antagonist |
Pharmacokinetic data | |
Elimination half-life | 12–18 hours[1] |
Identifiers | |
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JSmol) | |
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6β-Naltrexol, or 6β-hydroxynaltrexone (developmental code name AIKO-150), is a
6β-Naltrexol binds to the
6β-Naltrexol is said to have very limited capacity to cross the blood–brain barrier.[8] However, 6β-naltrexol is still able to cross into the brain and produce central opioid receptor antagonism at sufficient levels.[5] In animal studies, 6β-naltrexol showed about 10-fold separation in potency between peripheral and central opioid antagonism, whereas naltrexone showed no separation.[5] Because it is a MOR neutral antagonist and hence does not reduce basal MOR signaling, 6β-naltrexol shows much lower potential for producing opioid withdrawal symptoms than naltrexone at doses achieving similar central opioid blockade in animal studies.[5][7] Due to the very high levels of 6β-naltrexol that occur during naltrexone therapy, 6β-naltrexol may contribute to the central opioid receptor antagonism of naltrexone.[9]
See also
References
- ^ ISBN 978-1-59745-197-0.
- ^ ISBN 978-0-19-984497-5.
- ^ ISBN 978-1-4377-2792-0.
- ISBN 978-0-19-923664-0.
- ^ ISSN 0065-7743.
- ^ PMID 22123184.
- ^ PMID 15680308.
- PMID 27189967.
- S2CID 195697174.