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Identification of Psychoplastogenic N,N‑Dimethylaminoisotryptamine (isoDMT) Analogues through Structure–Activity Relationship Studies
- Dunlap, Lee E;
- Azinfar, Arya;
- Ly, Calvin;
- Cameron, Lindsay P;
- Viswanathan, Jayashri;
- Tombari, Robert J;
- Myers-Turnbull, Douglas;
- Taylor, Jack C;
- Grodzki, Ana Cristina;
- Lein, Pamela J;
- Kokel, David;
- Olson, David E
Published Web Location
https://doi.org/10.1021/acs.jmedchem.9b01404Abstract
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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