Serotonin releasing agent
A serotonin releasing agent (SRA) is a type of drug which induces the release of serotonin into the neuronal synaptic cleft, with less significant or no efficacy in producing neurotransmitter efflux at other types of monoamine neurons.
List of serotonin releasing agents
- Pharmaceutical Drugs
- Chlorphentermine (Apsedon, Desopimon, Lucofen)
- Cloforex (Oberex; prodrug to chlorphentermine)
- Dexfenfluramine (Redux) (enantiomer of fenfluramine)
- Etolorex (prodrug to chlorphentermine; never marketed)
- Fenfluramine (Pondimin, Fen-Phen)
- Levofenfluramine (enantiomer of fenfluramine)
- Research Chemicals
- 2-Methyl-3,4-methylenedioxyamphetamine (2-Methyl-MDA)
- 3-Methoxy-4-methylamphetamine (MMA)
- 3-Methyl-4,5-methylenedioxyamphetamine (5-Methyl-MDA)
- 3,4-Ethylenedioxy-N-methylamphetamine (EDMA)
- 4-Methoxyamphetamine (PMA)
- 4-Methoxy-N-ethylamphetamine (PMEA)
- 4-Methoxy-N-methylamphetamine (PMMA)
- 4-Methylthioamphetamine (4-MTA)
- 5-(2-Aminopropyl)-2,3-dihydrobenzofuran (5-APDB)
- 5-Indanyl-2-aminopropane (IAP)
- 5-Methoxy-6-methylaminoindane (MMAI)
- 5-Trifluoromethyl-2-aminoindane (TAI)
- 5,6-Methylenedioxy-2-aminoindane (MDAI)
- 5,6-Methylenedioxy-N-methyl-2-aminoindane (MDMAI)
- 6-Chloro-2-aminotetralin (6-CAT)
- 6-Tetralinyl-2-aminopropane (TAP)
- 6,7-Methylenedioxy-2-aminotetralin (MDAT)
- 6,7-Methylenedioxy-N-methyl-2-aminotetralin (MDMAT)
- N-Ethyl-5-trifluoromethyl-2-aminoindane (ETAI)
- N-Methyl-5-indanyl-2-aminopropane (IMP)
Examples and use
MDMA, MDEA, MDA, and MBDB, among other relatives (see MDxx), are recreational drugs termed entactogens. They act as releasing agents of not only serotonin, but of dopamine and norepinephrine as well, and also agonize serotonin receptors such as 5-HT2A.
Fenfluramine, chlorphentermine, and aminorex were used as appetite suppressants but they were discontinued due to concerns of cardiac valvulopathy. This side effect has been attributed not only to their action as SRAs but due to potent agonism of the 5-HT2B receptor as well. The designer drugs MDMA and 4-methylaminorex which are also SRAs and 5-HT2B agonists have been reported to cause this effect as well.
Many tryptamines, such as DMT, DET, DPT, DiPT, psilocin, and bufotenin are SRAs as well as non-selective serotonin receptor agonists. These drugs are serotonergic psychedelics, which is a consequence of their ability to activate the 5-HT2A receptor.
αET and αMT, also tryptamines, are serotonin, norepinephrine, and dopamine releasing agents and non-selective serotonin receptor agonists which were formerly used as antidepressants. They have since been discontinued and are now encountered solely as recreational drugs.
Tramadol, in addition to its opioid and norepinephrine reuptake-inhibiting effects, is an SRA and is used as an analgesic. Indeloxazine is an SRA and norepinephrine reuptake inhibitor used as a nootropic and neuroprotective.
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