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Zalsupindole
Chemical compound From Wikipedia, the free encyclopedia
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Zalsupindole, also known by its code names DLX-001 and AAZ-A-154 and as (R)-5-methoxy-N,N-dimethyl-α-methylisotryptamine ((R)-5-MeO-α-Me-isoDMT), is non-hallucinogenic serotonin receptor agonist and psychoplastogen of the isotryptamine family related to psychedelic tryptamines such as dimethyltryptamine (DMT).[1][2][4][5][6] It is under development for the treatment of major depressive disorder and other central nervous system disorders.[2][4] The drug is taken orally.[1][2][3]
It acts as a partial agonist of the serotonin 5-HT2A receptor and also interacts with other serotonin receptors.[1] The drug activates the serotonin 5-HT2A receptor with sufficiently high efficacy to promote neuroplasticity but not with adequate efficacy to cause psychedelic effects.[1] It does not produce psychedelic-like effects in animals or humans but does produce antidepressant-like effects in animals.[1][3]
Zalsupindole was first described in the scientific literature by 2021.[7] It was developed by David E. Olson and colleagues at the University of California, Davis and Delix Therapeutics.[2][4] As of December 2024, it is in phase 1 clinical trials and a phase 2 trial is being planned.[2]
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Use and effects
A phase 1 dose-ranging clinical trial found that zalsupindole is non-hallucinogenic in humans across a dose range of 2 to 360 mg orally.[1][3] Nonetheless, it produced changes in brain function as measured by quantitative electroencephalography (qEEG).[3]
Side effects
Side effects of zalsupindole include dose-dependent nausea, headache, and dizziness.[3]
Pharmacology
Summarize
Perspective
Pharmacodynamics
Zalsupindole is a non-selective serotonin receptor modulator including of the serotonin 5-HT2A receptor.[1][8] It acts as a low-potency, low-efficacy partial agonist of the serotonin 5-HT2A receptor, with an EC50 of 8,200 nM and an Emax of 17%.[1] The drug is also a moderate-efficacy partial agonist of the serotonin 5-HT2C receptor, with an EC50 of 3,300 nM and an Emax of 70%.[1] Other activities have also been reported.[1] It is selective for the serotonin 5-HT2 receptors over a number of other receptors, including dopamine receptors, adrenergic receptors, and the κ-opioid receptor, among others.[1][8] The drug is a silent antagonist of the serotonin 5-HT2B receptor, with an IC50 of 27,600 nM.[1][6]
Zalsupindole is orally bioavailable and centrally penetrant in animals.[6] It is a psychoplastogen via activation of the serotonin 5-HT2A receptor and rapidly and persistently increases neuroplasticity in preclinical research.[1][9][5][6] Animal studies have found that it produces antidepressant-like effects without causing psychedelic-like effects such as the head-twitch response.[1][7][10][5][6][11] It does not produce hyperlocomotion at therapeutically relevant doses.[1] In accordance with its serotonin 5-HT2B receptor antagonism, zalsupindole showed no cardiovascular safety signals in animals.[6]
Pharmacokinetics
The pharmacokinetics of zalsupindole have been studied.[1][3]
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Chemistry
Zalsupindole, also known as (R)-5-methoxy-N,N-dimethyl-α-methylisotryptamine, is a substituted isotryptamine derivative.[12][13] It is a combined derivative of 5-methoxy-N,N-dimethylisotryptamine (5-MeO-isoDMT) and α-methylisotryptamine (isoAMT).[12][13] Another related compound is 6-methoxy-N,N-dimethylisotryptamine (6-MeO-isoDMT).[12] Zalsupindole is a close isotryptamine analogue of α,N,N,O-tetramethylserotonin (α,N,N,O-TMS or 5-MeO-α,N,N-TMT).[13]
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History
Zalsupindole was first described in the scientific literature by David E. Olson and colleagues in 2021.[7] It was developed by Olson's lab at the University of California, Davis and at his company Delix Therapeutics.[2][4] The drug was initially described under the name AAZ-A-154 and then by the name DLX-001 before receiving the name zalsupindole.[2][4][1]
Society and culture
Names
Zalsupindole is the generic name of the drug and its INN.[14] It is also known by its developmental code names DLX-001 and AAZ-A-154.[2][4]
Research
Zalsupindole, as well as related drugs such as tabernanthalog (TBG; DLX-007), DLX-159, DLX-2270, and JRT, are licensed by Delix Therapeutics and are being developed for treatment of neuropsychiatric disorders such as depression and schizophrenia.[9][2][4] As of December 2024, zalsupindole is in phase 1 clinical trials for major depressive disorder and other central nervous system disorders.[2][4] A phase 2 trial is being planned.[2]
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See also
References
External links
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