High affinity ibogaine binding to a mu opioid agonist site.
Life sciences January 1, 1995 E E Codd 29 citations
Ibogaine, a naturally occurring alkaloid, may reduce drug-seeking behavior and opioid withdrawal symptoms. Previous research found weak binding to opioid receptors, but this study examined ibogaine's interaction with the mu opioid receptor in mouse forebrain using a radiolabeled tracer. Analysis revealed ibogaine binds to two different affinity states of the receptor, with a high-affinity binding constant (Ki) of about 130 nM and a lower one of 4 µM. Adding sodium chloride, which shifts receptors to a low-affinity state, reduced ibogaine's binding, indicating it acts as an agonist at the mu opioid receptor. This suggests ibogaine's effects on pain, withdrawal, and drug seeking may be mediated through mu opioid receptor activation.