Ibogainalog

Pharmacodynamics

Ibogainalog acts as a non-selective serotonin receptor modulator, including as an agonist of the serotonin 5-HT_1B, 5-HT_1F, 5-HT_2A, and 5-HT₆ receptors, as an agonist or antagonist of the serotonin 5-HT_2B and 5-HT_2C receptors, and as an inverse agonist of the serotonin 5-HT₇ receptor.^[3][4][5][6] Unlike noribogaine, IBG shows no activation of the opioid receptors or κ-opioid receptor agonism.^[3] In addition to its actions at serotonin receptors, IBG weakly inhibits certain nicotinic acetylcholine receptors.^[7] The drug also acts as a relatively weak serotonin reuptake inhibitor.^[5]

The drug produces the head-twitch response in animals and hence shows psychedelic-like effects.^[1][3] However, it has reduced and relatively weak hallucinogen-like effects compared to 5-MeO-DMT.^[1][5][3] Conversely, tabernanthalog (TBG), a simplified analogue of tabernanthine and positional isomer of IBG, appears to be completely non-hallucinogenic.^[1][3] IBG shows comparable psychoplastogenic activity to ibogaine.^[1] In contrast to ibogaine, IBG and TBG appear to have much less or no potential for cardiotoxicity secondary to hERG inhibition.^[1][3] However, TBG showed a better overall safety profile than IBG and was selected for development instead of IBG.^[1][3] IBG shows analgesic effects against neuropathic pain and visceral pain in animals that appear to be mediated by serotonin 5-HT_2A receptor activation.^[4]

In early animal studies, ibogainalog was described as having enhanced tryptamine-like, tremorogenic, and sedative effects compared to ibogaine.^[8][9] It was also said to have chlorpromazine-like effects.^[8][9]

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