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Zalsupindole
Chemical compound From Wikipedia, the free encyclopedia
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Zalsupindole,[1] also known by its developmental code names DLX-001 and AAZ-A-154 and as (R)-5-methoxy-N,N-dimethyl-α-methylisotryptamine, is a novel isotryptamine derivative which acts as a serotonin 5-HT2A receptor agonist discovered and synthesized by the lab of Professor David E. Olson at the University of California, Davis.[2][3][4][5] It is being developed for the treatment of major depressive disorder and other central nervous system disorders.[2][3]
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Pharmacology
Animal studies suggest that it produces antidepressant effects without the psychedelic action typical of drugs from this class.[6][7][4][5] In tests, zalsupindole had antidepressant-like effects in mice without causing the head-twitch response linked to hallucinogenic effects.[8][4][5] Due to the rapidly-induced and enduring neuroplasticity, zalsupindole is a member of the class of compounds known as non-hallucinogenic psychoplastogens.[9][4][5] A Phase 1 dose-ranging clinical trial confirmed that zalsupindole is non-hallucinogenic in humans across a dose range of 2 to 360 mg.[10]
The drug was selective for the serotonin 5-HT2 receptors over several other receptors, including dopamine receptors, adrenergic receptors, and the κ-opioid receptor.[11] It is an antagonist of the serotonin 5-HT2B receptor and showed no cardiovascular safety signals in animals.[5] Zalsupindole is orally bioavailable and centrally penetrant in animals.[5]
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Chemistry
Zalsupindole is a member of the isotryptamine group of compounds.[12][13] It is a combined derivative of isoDMT, 5-MeO-isoDMT, and isoAMT.[12][13] Another related compound is 6-MeO-isoDMT.[12] Zalsupindole is a close isotryptamine analogue of α,N,N,O-tetramethylserotonin (α,N,N,O-TMS).[13]
Research
Zalsupindole, as well as related compounds, are licensed by Delix Therapeutics and are being developed as potential medicines for neuropsychiatric disorders.[9][2][3] As of December 2023, zalsupindole is in Phase 1 clinical trials for major depressive disorder and other central disorders.[2][3]
See also
References
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