Abstract
Radioligand-binding studies were performed to ascertain the actions of noribogaine, a suspected metabolite of ibogaine, on opioid receptors. Consistent with previous results, ibogaine showed highest affinity for kappa opioid receptors (Ki = 3.77 +/- 0.81 microM), less affinity for mu receptors (Ki = 11.04 +/- 0.66 microM) and no affinity for delta receptors (Ki > 100 microM). Noribogaine showed a higher affinity than ibogaine for all of the opioid receptors: kappa Ki = 0.96 +/- 0.08 microM, mu Ki = 2.66 +/- 0.62 microM and delta Ki = 24.72 +/- 2.26 microM. These data suggest that noribogaine is active in vivo and that it may contribute to ibogaine's pharmacological effects.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Analgesics / metabolism
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Animals
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Benzeneacetamides*
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Cattle
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Cerebral Cortex / drug effects
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Cerebral Cortex / metabolism
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Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
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Enkephalin, D-Penicillamine (2,5)-
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Enkephalins / metabolism
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Ibogaine / analogs & derivatives*
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Ibogaine / metabolism*
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In Vitro Techniques
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Kinetics
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Naloxone / pharmacology
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Pyrrolidines / metabolism
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Radioligand Assay
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Receptors, Opioid / drug effects
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Receptors, Opioid / metabolism*
Substances
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Analgesics
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Benzeneacetamides
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Enkephalins
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Pyrrolidines
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Receptors, Opioid
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Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
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Naloxone
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Ibogaine
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noribogaine
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Enkephalin, D-Penicillamine (2,5)-
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U 69593