Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 63, Issue 3, Pages 1142-1155Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.9b01404
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Funding
- NIAAA NIH HHS [R01 AA022583] Funding Source: Medline
- NICHD NIH HHS [U54 HD079125] Funding Source: Medline
- NIEHS NIH HHS [P30 ES023513] Funding Source: Medline
- NIGMS NIH HHS [R01 GM128997, T32 GM113770] Funding Source: Medline
- NIMH NIH HHS [T32 MH112507] Funding Source: Medline
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Ketamine, N,N-dimethyltryptamine (DMT), and other psychoplastogens possess enormous potential as neurotherapeutics due to their ability to potently promote neuronal growth. Here, we report the first-ever structure activity relationship study with the explicit goal of identifying novel psychoplastogens. We have discovered several key features of the psychoplastogenic pharmacophore and used this information to develop N,N-dimethylaminoisotryptamine (isoDMT) psychoplastogens that are easier to synthesize, have improved physicochemical properties, and possess reduced hallucinogenic potential as compared to their DMT counterparts.
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