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Re: Esmethadone helps treatment-resistant depression SLS

Posted by Hugh on January 11, 2022, at 20:41:21

In reply to Re: Esmethadone helps treatment-resistant depression Hugh, posted by SLS on January 11, 2022, at 11:03:19

Ketamine, memantine (NAMENDA XR), and REL-1017 [esmethadone] share the same core mechanism of action, inhibiting the NMDA receptor directly as channel blockers. Ketamine and its metabolites are also thought to have other activities in the brain that may be responsible for some of its effects.

Ketamine enters the NMDA receptor channel when it is activated, blocking its unwanted function and showing significant activity in reducing symptoms of depression within a few hours after administration. However, it remains "trapped" in the channel to a high degree after closure. This prolonged blocking activity is believed to be a causative factor in ketamine's unfavorable side effects including hallucinations, delusion and delirium, which are found even at therapeutic doses

REL-1017 acts very similarly by blocking the NMDA receptor at a channel level when the receptor is activated and potentially showing similar rapid therapeutic effect. However, several studies have demonstrated that differences in the degree of trapping exist among use-dependent NMDA receptor antagonists and that these differences are correlated with efficacy and safety. For example, the NMDA receptor antagonist memantine is currently FDA approved to treat Alzheimer's disease, but it hasn't shown efficacy in treating depression or neuropathic pain in studies to-date.

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