5-Bromotryptamine
chemical compound
5-Bromotryptamine (5-Br-T; developmental code name PAL-518) is a serotonin receptor modulator and monoamine releasing agent of the tryptamine family. It is the 5-bromo derivative of tryptamine.
The drug acts as a potent full agonist of the serotonin 5-HT2A receptor, with an EC50Tooltip half-maximal effective concentration of 5.14 nM and an EmaxTooltip maximal efficacy of 108%. It is also a potent full agonist of the serotonin 5-HT2B receptor. In addition to its serotonin receptor agonism, 5-bromotryptamine is a serotonin–dopamine releasing agent (SDRA), with EC50 values for induction of monoamine release of 75 nM for serotonin, 478 nM for dopamine, and >10,000 nM for norepinephrine in rat brain synaptosomes.
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. However, given intravenously at sufficiently high doses, tryptamine is still known to be able to produce weak and short-lived psychoactive effects in humans.
The chemical synthesis of 5-bromotryptamine has been described.
5-Bromotryptamine was first described in the scientific literature by 1965.
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