Serotonin-dopamine releasing agent

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 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.[1] 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-HT2A receptor, and may act as agonists of other serotonin receptors as well.[1]

UWA-101 is a reuptake inhibitor of serotonin and dopamine, but may also have efficacy as a releasing agent of these neurotransmitters.[3]

See also

References

  1. ↑ 1.0 1.1 1.2 Blough BE, Landavazo A, Partilla JS et al. (October 2014). "Alpha-ethyltryptamines as dual dopamine-serotonin releasers". Bioorganic & Medicinal Chemistry Letters 24 (19): 4754–8. doi:10.1016/j.bmcl.2014.07.062. PMID 25193229.
  2. ↑ Banks ML, Bauer CT, Blough BE et al. (June 2014). "Abuse-related effects of dual dopamine/serotonin releasers with varying potency to release norepinephrine in male rats and rhesus monkeys". Experimental and Clinical Psychopharmacology 22 (3): 274–84. doi:10.1037/a0036595. PMID 24796848.
  3. ↑ Johnston TH, Millar Z, Huot P et al. (May 2012). "A novel MDMA analogue, UWA-101, that lacks psychoactivity and cytotoxicity, enhances L-DOPA benefit in parkinsonian primates". FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology 26 (5): 2154–63. doi:10.1096/fj.11-195016. PMID 22345403.