Radioligand-binding study of noribogaine, a likely metabolite of ibogaine.
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.
Pearl
S M
SM
Department of Pharmacology and Neuroscience, Albany Medical College, NY 12208, USA.
Herrick-Davis
K
K
Teitler
M
M
Glick
S D
SD
D000700:Analgesics / Q000378:metabolism; D000818:Animals; D044482:Benzeneacetamides; D002417:Cattle; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D020881:Enkephalin, D-Penicillamine (2,5)-; D004745:Enkephalins / Q000378:metabolism; D007050:Ibogaine / Q000031:analogs & derivatives* / Q000378:metabolism*; D066298:In Vitro Techniques; D007700:Kinetics; D009270:Naloxone / Q000494:pharmacology; D011759:Pyrrolidines / Q000378:metabolism; D011869:Radioligand Assay; D011957:Receptors, Opioid / Q000187:drug effects / Q000378:metabolism*
D000700:Analgesics; D044482:Benzeneacetamides; D004745:Enkephalins; D011759:Pyrrolidines; D011957:Receptors, Opioid; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D009270:Naloxone; D007050:Ibogaine; C094385:noribogaine; D020881:Enkephalin, D-Penicillamine (2,5)-; C045444:U 69593