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5-Fluorotryptamine

Pharmaceutical compound From Wikipedia, the free encyclopedia

5-Fluorotryptamine
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5-Fluorotryptamine (5-fluoro-T, 5-FT, or 5-F-T; code name PAL-284) is a serotonin receptor agonist and monoamine releasing agent of the tryptamine family.[1][2]

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Pharmacology

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5-FT is known to have affinity for the serotonin 5-HT1A and 5-HT2A receptors, with Ki values of 18 nM and 6.0–3,908 nM, respectively.[3][4][5] It is a full agonist of the serotonin 5-HT2A receptor, with an EC50Tooltip half-maximal effective concentration of 2.64 to 58 nM and an EmaxTooltip half-maximal effective concentration of 110%.[2][4] The drug is also an agonist of the serotonin 5-HT1A receptor, with an EC50 of 129 nM.[4] 5-HT shows high affinity for the serotonin 5-HT2B and 5-HT2C receptors as well (Ki = 5.7 nM and 3.72 nM, respectively).[5] In addition to its serotonin receptor agonism, 5-FT is a serotonin–dopamine releasing agent (SDRA), with EC50 values for induction of monoamine release of 10.1 nM for serotonin, 82.3 nM for dopamine, and 464 nM for norepinephrine.[2] The drug is also a weak monoamine oxidase inhibitor (MAOI), with IC50Tooltip half-maximal inhibitory concentration values of 13,200 nM for monoamine oxidase A (MAO-A) and 52,500 nM for monoamine oxidase B (MAO-B).[1][6]

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.[1][6]

Tryptamines without substitutions at the amine or alpha carbon, such as tryptamine, serotonin (5-hydroxytryptamine; 5-HT), and 5-methoxytryptamine (5-MeO-T), are known to be very rapidly metabolized and thereby inactivated by monoamine oxidase A (MAO-A) in vivo and to have very short elimination half-lives.[7][8][9][10][11][12][13] However, given intravenously at sufficiently high doses, tryptamine is still known to be able to produce weak and short-lived psychoactive effects in humans.[14][8][2][13]

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History

5-FT was first described in the scientific literature by 1983.[15]

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References

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