Serotonin–dopamine releasing agent explained

A serotonin–dopamine releasing agent (SDRA) is a type of drug which induces the release of serotonin and dopamine in the body and/or brain.

A closely related type of drug is a serotonin–dopamine reuptake inhibitor (SDRI).

Examples of SDRAs

A number of tryptamine derivatives have been found to act as SDRAs.^[1] One such agent is 5-chloro-αMT (PAL-542), which has been reported as having about 64-fold selectivity for dopamine release over norepinephrine release and about 3-fold selectivity for serotonin release over dopamine release, making it a highly selective and well-balanced SDRA.^[2] Another agent is 5-fluoro-αET (PAL-545), which has about 35-fold selectivity for dopamine release over norepinephrine release and about 4-fold selectivity for serotonin release over dopamine release. Though selective for inducing the release of serotonin and dopamine over norepinephrine, these agents are not selective monoamine releasers; they have all also been found to be potent agonists of the 5-HT_2A receptor, and may act as agonists of other serotonin receptors as well.

UWA-101 is an SDRI that, based on its chemical structure, may also have a great efficacy as a releasing agent of serotonin and dopamine.^[3]

See also

• Monoamine releasing agent
• Serotonin releasing agent
• Dopamine releasing agent
• Serotonin–norepinephrine–dopamine releasing agent

Notes and References

1. Blough BE, Landavazo A, Partilla JS, etal . Alpha-ethyltryptamines as dual dopamine-serotonin releasers . Bioorganic & Medicinal Chemistry Letters . 24 . 19 . 4754–8 . October 2014 . 25193229 . 10.1016/j.bmcl.2014.07.062 . 4211607.
2. Banks ML, Bauer CT, Blough BE, etal . Abuse-related effects of dual dopamine/serotonin releasers with varying potency to release norepinephrine in male rats and rhesus monkeys . . 22 . 3 . 274–84 . June 2014 . 24796848 . 10.1037/a0036595 . 4067459.
3. Johnston TH, Millar Z, Huot P, etal . A novel MDMA analogue, UWA-101, that lacks psychoactivity and cytotoxicity, enhances L-DOPA benefit in parkinsonian primates . FASEB Journal . 26 . 5 . 2154–63 . May 2012 . 22345403 . 10.1096/fj.11-195016 . free . 37589231 .