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Luvesilocin
Chemical compound From Wikipedia, the free encyclopedia
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Luvesilocin (INN),[2] also known by its developmental code names RE104 and FT-104, as well as by its chemical name 4-glutaryloxy-N,N-diisopropyltryptamine (4-HO-DiPT O-glutarate or 4-GO-DiPT), is an investigational drug product being developed by the pharmaceutical company Reunion Neuroscience.[3] Luvesilocin a prodrug ester of a synthetic psychedelic 4-hydroxytryptamine, 4-HO-DiPT.[4] It is one of a number of related psychedelic derivatives being developed as pharmaceuticals to treat mood disorders.
Luvesilocin is in human clinical trials as a possible treatment for postpartum depression and treatment-resistant depression.[5][6][7][8] As of 2024, luvesilocin entered a Phase II clinical trial for post-partum depression.[9]
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Pharmacology
Luvesilocin is a prodrug that is converted into the psychedelic tryptamine 4-HO-DiPT upon administration.[4][10] 4-OH-DiPT is chemically related to the neurotransmitter serotonin and acts as a non-selective agonist of the serotonin receptors. 4-OH-DiPT acts as an agonist on the serotonin 2A receptor (Ki 120 nM).[4] Activation of one serotonin receptor, the serotonin 5-HT2A receptor, is specifically responsible for the hallucinogenic effects and preclinical behavioral changes induced by 4-OH-DiPT and other serotonergic psychedelics.
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Research
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Synthesis, pharmacology and preclinical studies with luvesilocin have been published.[4] 4-OH-DiPT, the active metabolite of luvesilocin, produces measurable head-twitch response in rodents, indicative of its psychedelic properties.[11] Discriminative stimulus tests in rats showed 4-OH-DiPT fully substituted for DOM with a 5-fold lower potency than DOM and 2-fold lower potency than psilocin.[12] Findings suggest that 4-OH-DiPT activates BLA interneurons via the 5-HT2A receptor to enhance GABAergic inhibition of BLA principal neurons in the basolateral amygdala, which provides a potential mechanism for suppressing learned fear (fear extinction).[13]
Luvesilocin is being developed as a subcutaneous injection. Luvesilocin has been investigated in a randomized, placebo-controlled, single escalating dose Phase 1 study in healthy volunteers to assess the safety of luvesilocin, as well as to characterize the pharmacodynamics, including the duration and intensity of the psychedelic experience.[14] The mean duration of the psychedelic experience after administration of RE104 30 mg in humans was found to be 3.7 hours.[1]
Luvesilocin is currently under investigation to treat postpartum depression (PPD).[1][15][16]
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References
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