FT-104
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RE104, formerly known as FT-104, and as 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 Field Trip Health was a Canadian Ketamine-assisted psychotherapy company, founded in April 2019. In May 2022, the company split into two separate, independent entities: Field Trip Health and Wellness and Reunion Neuroscience. Field Trip Health ...
. RE104 a
prodrug A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be ...
ester In chemistry, an ester is a compound derived from an acid (either organic or inorganic) in which the hydrogen atom (H) of at least one acidic hydroxyl group () of that acid is replaced by an organyl group (R). These compounds contain a distin ...
of a synthetic
psychedelic Psychedelics are a subclass of hallucinogenic drugs whose primary effect is to trigger non-ordinary mental states (known as psychedelic experiences or "trips") and a perceived "expansion of consciousness". Also referred to as classic halluci ...
4-hydroxytryptamine, 4-HO-DiPT. It is one of a number of related psychedelic derivatives being developed as pharmaceuticals to treat mood disorders. RE104 is in human
clinical trial Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...
s as a possible treatment for
postpartum depression Postpartum depression (PPD), also called perinatal depression, is a mood disorder which may be experienced by pregnant or postpartum women. Symptoms include extreme sadness, low energy, anxiety, crying episodes, irritability, and extreme cha ...
and
treatment-resistant depression Treatment-resistant depression (TRD) is often defined as major depressive disorder in which an affected person does not respond adequately to at least two different antidepressant medications at an adequate dose and for an adequate duration. Inad ...
. As of 2024, RE104 entered a Phase II clinical trial for post-partum depression.


Pharmacology

RE104 is a
prodrug A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be ...
that is converted into the
psychedelic Psychedelics are a subclass of hallucinogenic drugs whose primary effect is to trigger non-ordinary mental states (known as psychedelic experiences or "trips") and a perceived "expansion of consciousness". Also referred to as classic halluci ...
tryptamine Tryptamine is an indolamine metabolite of the essential amino acid tryptophan. The chemical structure is defined by an indole—a fused benzene and pyrrole ring, and a 2-aminoethyl group at the second carbon (third aromatic atom, with the firs ...
4-HO-DiPT upon administration. 4-OH-DiPT s chemically related to the
neurotransmitter A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a Chemical synapse, synapse. The cell receiving the signal, or target cell, may be another neuron, but could also be a gland or muscle cell. Neurotra ...
serotonin Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, ...
and acts as a non-selective
agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...
of the
serotonin receptor 5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in multiple tissues including the central and peripheral nervous systems. They mediate both ex ...
s. 4-OH-DiPT acts as an
agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...
on the
serotonin 2A receptor The 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and functions as a G protein-coupled receptor (GPCR). It is a cell surface receptor that activates multiple intracellular signalling cascades ...
(Ki 120 nM). 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 4-HO-DiPT, also known as 4-hydroxy-''N'',''N''-diisopropyltryptamine or as iprocin, is a synthetic compound, synthetic psychedelic drug of the substituted tryptamine, tryptamine family. It is a higher homologous series, homologue of psilocin and ...
and other
serotonergic psychedelic Psychedelics are a subclass of hallucinogenic drugs whose primary effect is to trigger non-ordinary mental states (known as psychedelic experiences or "trips") and a perceived "expansion of consciousness". Also referred to as classic halluci ...
s.


Research

Synthesis, pharmacology and preclinical studies with RE104 have been published. 4-OH-DiPT, the active metabolite of RE104, produces measurable
head-twitch response The head-twitch response (HTR), also sometimes known as wet dog shakes (WDS) in rats, is a rapid side-to-side head movement that occurs in mice and rats in association with serotonin 5-HT2A receptor activation. Serotonergic psychedelics like lys ...
in rodents, indicative of its psychedelic properties. 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. 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). RE104 is being developed as a subcutaneous injection. RE104 has been investigated in a randomized, placebo-controlled, single escalating dose Phase 1 study in healthy volunteers to assess the safety of RE104, as well as to characterize the pharmacodynamics, including the duration and intensity of the psychedelic experience. The mean duration of the psychedelic experience after administration of RE104 30 mg in humans was found to be 3.7hours. RE104 is currently under investigation to treat
postpartum depression Postpartum depression (PPD), also called perinatal depression, is a mood disorder which may be experienced by pregnant or postpartum women. Symptoms include extreme sadness, low energy, anxiety, crying episodes, irritability, and extreme cha ...
(PPD).


See also

*
List of investigational hallucinogens and entactogens This is a list of investigational hallucinogens and entactogens, or hallucinogens and entactogens that are currently under formal development for clinical use but are not yet approved. ''Chemical/generic names are listed first, with developmenta ...
*
RE-109 ''O''-Glutarylpsilocin (developmental code name RE109), also known as 4-glutaryloxy-''N'',''N''-dimethyltryptamine (4-HO-DMT ''O''-glutarate) is a serotonergic psychedelic of the tryptamine family. It acts as a prodrug of psilocin (4-HO-DMT) simil ...
(4-GO-DMT) * 4-AcO-DiPT *
4-PrO-DMT 4-Propionoxy-''N,N''-dimethyltryptamine (4-PrO-DMT, or O-Propionylpsilocin) is a synthetic psychedelic drug from the tryptamine family with psychedelic effects, and is believed to act as a prodrug for psilocin. It produces a head-twitch response ...
*
EB-002 EB-002, also formerly known as EB-373, is a synthetic prodrug of the non-selective serotonin receptor agonist and serotonergic psychedelic psilocin which is under development for the treatment of neuropsychiatric disorders like depression and a ...
*
MSP-1014 MSP-1014 is a serotonergic psychedelic which is under development for the treatment of major depressive disorder, other depressive disorders, and anxiety disorders.Araujo JA, Higgins GA, de Lannoy IA, Dean I, Atkinson J, Lanthier J, Slassi M. (2 ...
*
THC hemisuccinate THC hemisuccinate (Δ9-THC-O-hemisuccinate, Dronabinol hemisuccinate) is a synthetic derivative of tetrahydrocannabinol, developed in the 1990s. It is a water-soluble prodrug ester which is converted into THC inside the body, and was developed t ...


References

{{Tryptamines 4-Acyloxytryptamines Designer drugs N,N-Dialkyltryptamines Diisopropylamino compounds Esters Experimental hallucinogens Prodrugs Psychedelic tryptamines Secondary amino acids Serotonin receptor agonists