Further information: Chemistry:Serotonin releasing agent and Chemistry: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 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.[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 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
References
- ↑ 1.0 1.1 1.2 "Alpha-ethyltryptamines as dual dopamine-serotonin releasers". Bioorganic & Medicinal Chemistry Letters 24 (19): 4754–8. October 2014. doi:10.1016/j.bmcl.2014.07.062. PMID 25193229.
- ↑ "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. June 2014. doi:10.1037/a0036595. PMID 24796848. PMC 4067459. http://content.apa.org/journals/pha/22/3/274.
- ↑ "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. doi:10.1096/fj.11-195016. PMID 22345403.
Monoamine releasing agents |
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| DRAs | |
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| NRAs | |
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| SRAs | |
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| Others |
- Monoamine activity enhancers: BPAP
- PPAP
- DAT modulators: Agonist-like: SoRI-9804
- SoRI-20040; Antagonist-like: SoRI-20041
- Adrenergic release blockers: Bethanidine
- Bretylium
- Guanadrel
- Guanazodine
- Guanethidine
- Guanoxan
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See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • Monoamine metabolism modulators • Monoamine neurotoxins |
Human trace amine-associated receptor ligands |
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| TAAR1 | | Agonists | | Endogenous† |
- Classical monoamine neurotransmitters
- Dopamine
- Histamine
- Norepinephrine
- Serotonin
- Trace amines
- 3-Iodothyronamine
- 3-Methoxytyramine
- N-Methylphenethylamine
- N-Methyltyramine
- m-Octopamine
- p-Octopamine
- Phenethylamine
- Phenylethanolamine
- Synephrine
- Tryptamine
- m-Tyramine
- p-Tyramine
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| Synthetic‡ |
- Amphetamine
- DOB
- DOET
- 4-Hydroxyamphetamine
- Isoprenaline
- MDA (tenamfetamine)
- MDMA (midomafetamine)
- 2-Methylphenethylamine
- 3-Methylphenethylamine
- 4-Methylphenethylamine
- β-Methylphenethylamine
- Methamphetamine
- 3-MMA
- Norfenfluramine
- Phentermine
- o-PIT
- Propylhexedrine
- RO5166017
- N,N-Dimethylphenethylamine
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| Neutral antagonists | |
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| Inverse agonists | |
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| TAAR2 | | Agonists‡ | |
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| Neutral antagonists | |
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| TAAR5 | | Agonists‡ |
- N,N-Dimethylethylamine
- Trimethylamine
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| Neutral antagonists | |
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| Inverse agonists‡ | |
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† References for all endogenous human TAAR1 ligands are provided at List of trace amines
‡ References for synthetic TAAR1 agonists can be found at TAAR1 or in the associated compound articles. For TAAR2 and TAAR5 agonists and inverse agonists, see TAAR for references.
See also: Receptor/signaling modulators |
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