5-Fluorotryptamine
5-Fluorotryptamine is a serotonin receptor agonist and monoamine releasing agent of the tryptamine family.
Pharmacology
5-FT is known to have affinity for the serotonin 5-HT1A and 5-HT2A receptors, with Ki values of 18nM and 6.0–3,908nM, respectively. It is a full agonist of the serotonin 5-HT2A receptor, with an of 2.64 to 58nM and an of 110%. The drug is also an agonist of the serotonin 5-HT1A receptor, with an of 129nM. 5-HT shows high affinity for the serotonin 5-HT2B and 5-HT2C receptors as well. In addition to its serotonin receptor agonism, 5-FT is a serotonin–dopamine releasing agent, with values for induction of monoamine release of 10.1nM for serotonin, 82.3nM for dopamine, and 464nM for norepinephrine. The drug is also a weak monoamine oxidase inhibitor, with values of 13,200nM for monoamine oxidase A and 52,500nM for monoamine oxidase B.Despite its serotonin 5-HT2A receptor agonism, 5-FT failed to induce the head-twitch response, a behavioral proxy of psychedelic effects, in rodents, suggesting that it may not have hallucinogenic effects in humans.
Tryptamines without substitutions at the amine or alpha carbon, such as tryptamine, serotonin, and 5-methoxytryptamine, are known to be very rapidly metabolized and thereby inactivated by monoamine oxidase A in vivo and to have very short elimination half-lives. However, given intravenously at sufficiently high doses, tryptamine is still known to be able to produce weak and short-lived psychoactive effects in humans.