Noribogaine stimulates naloxone‐sensitive [35S]GTPγS binding
作者:
John Pablo,
Deborah Mash,
期刊:
NeuroReport
(OVID Available online 1998)
卷期:
Volume 9,
issue 1
页码: 109-114
ISSN:0959-4965
年代: 1998
出版商: OVID
关键词: Agonist;Ibogaine;12-OH Ibogamine;Metabolite;μ-opioid receptor
数据来源: OVID
摘要:
NORIBOGAINE is formedin vivoby theO-demethylation of the indole alkaloid ibogaine. We report here that noribogaine acts as a full agonist at the μ-opioid receptor. Noribogaine-stimulated guanylyl 5′γ-[35S]thio]triphosphate ([35S]GTPγS) was studied in rat thalamic membranes to measure activation of guanine nucleotide binding proteins (G-proteins) in the presence of excess GDP. Noribogaine caused a 170% increase above basal [35S]GTPγS binding at sub-micromolar effective concentrations (EC50) in a naloxone-sensitive manner, confirming that this effect was an opioid receptor-mediated process. The level of intrinsic activity for noribogaine in these assays was comparable to the full agonists DAMGO and morphine. In contrast, ibogaine had no significant effect on [35S]GTPγS binding over a similar concentration range. The efficacy of noribogaine as a full μ-opioid agonist may explain ibogaine's ability to block the acute signs of opiate withdrawal and its suppressive effects on morphine self-administration.
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