4-Fluoro-5-methoxy-DMT explained

4-Fluoro-5-Methoxy-N,N-dimethyltryptamine (4-F-5-MeO-DMT) was first described by David E. Nichols team in 2000. It is a potent 5-HT_1A agonist. Substitution with the 4-fluorine markedly increased 5-HT_1A selectivity over 5-HT_2A/2C receptors with potency greater than that of the 5-HT_1A agonist 8-OH-DPAT.^[1]

The analog compound with the N,N-dialkyl substituents constrained into a pyrrolidine ring, is a slightly stronger agonist for the 5-HT_1A receptor and retains the selectivity over the 5-HT_2A/2C receptors.^[2]

See also

• 4-HO-5-MeO-DMT
• 5-Fluoro-AMT
• 6-Fluoro-DMT
• 7F-5-MeO-MET

Notes and References

1. Blair JB, Kurrasch-Orbaugh D, Marona-Lewicka D, Cumbay MG, Watts VJ, Barker EL, Nichols DE . Effect of ring fluorination on the pharmacology of hallucinogenic tryptamines . Journal of Medicinal Chemistry . 43 . 24 . 4701–10 . November 2000 . 11101361 . 10.1021/jm000339w .
2. Laban U, Kurrasch-Orbaugh D, Marona-Lewicka D, Nichols DE . A novel fluorinated tryptamine with highly potent serotonin 5-HT1A receptor agonist properties . Bioorganic & Medicinal Chemistry Letters . 11 . 6 . 793–5 . March 2001 . 11277522 . 10.1016/S0960-894X(01)00062-2 .