- Source: Serotonin releasing agent
A serotonin releasing agent (SRA) is a type of drug that induces the release of serotonin into the neuronal synaptic cleft. A selective serotonin releasing agent (SSRA) is an SRA with less significant or no efficacy in producing neurotransmitter efflux at other types of monoamine neurons, including dopamine and norepinephrine neurons.
A closely related type of drug is a serotonin reuptake inhibitor (SRI), for instance fluoxetine. However, SRAs achieve much greater increases in serotonin levels than SRIs and have far more robust of subjective effects.
SRAs, for instance fenfluramine, have been used clinically as appetite suppressants. In addition, SSRAs have been proposed as novel antidepressants and anxiolytics, with the potential for a faster onset of action and superior effectiveness relative to the selective serotonin reuptake inhibitors (SSRIs).
Examples and use of SRAs
Fenfluramine, chlorphentermine, and aminorex, which are also amphetamines and relatives, were formerly used as appetite suppressants but were discontinued due to concerns of cardiac valvulopathy. This side effect has been attributed to their serotonin release and/or the additional action of potent agonism of the 5-HT2B receptor in the case of fenfluramine. Indeloxazine is said to be an SRA and norepinephrine reuptake inhibitor (NRI) that was formerly used as an antidepressant, nootropic, and neuroprotective.
Amphetamines like MDMA, MDEA, MDA, and MBDB, among other relatives (see MDxx), are recreational drugs termed entactogens. They act as serotonin–norepinephrine–dopamine releasing agents (SNDRAs) and also agonize serotonin receptors such as those in the 5-HT2 subfamily.
Some tryptamines, such as DMT, bufotenin, and psilocin, are SRAs as well as non-selective serotonin receptor agonists. Psilocin is a partial releaser of serotonin, with an EmaxTooltip maximal efficacy of 54%. These drugs are serotonergic psychedelics, which is a consequence of their ability to activate the 5-HT2A receptor. Other tryptamines, including tryptamine itself, αET, and αMT, are SNDRAs and non-selective serotonin receptor agonists. αET and αMT were originally thought to be monoamine oxidase inhibitors (MAOIs) and were formerly used as antidepressants, but are now encountered solely as recreational drugs. αET and αMT are described as being entactogen-like.
List of SSRAs
= Pharmaceutical drugs
=Chlorphentermine (Apsedon, Desopimon, Lucofen)
Cloforex (Oberex) (prodrug of chlorphentermine)
Dexfenfluramine (Redux) (enantiomer of fenfluramine)
Etolorex (prodrug of chlorphentermine; never marketed)
Fenfluramine (Pondimin, Fen-Phen)
Flucetorex (related to chlorphentermine; never marketed)
Indeloxazine (Elen, Noin) (non-selective; discontinued)
Levofenfluramine (enantiomer of fenfluramine)
Carbamazepine (Equetro, Epitol, and many other variations)
= Research chemicals
=Amiflamine (FLA-336)
Viqualine (PK-5078)
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)
5-Methoxy-2-aminoindane (MEAI, 5-MeO-AI)
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)
6-(2-aminopropil)benzofurans (6-APB)
5-(2-aminopropyl)benzofuran (5-APB)
See also
Monoamine releasing agent
References
Further reading
External links
Media related to Serotonin releasing agents at Wikimedia Commons
Kata Kunci Pencarian:
- Serotonin releasing agent
- Serotonin–dopamine releasing agent
- Serotonin
- Serotonin–norepinephrine–dopamine releasing agent
- Serotonin–norepinephrine releasing agent
- Norepinephrine releasing agent
- Monoamine releasing agent
- Dopamine releasing agent
- N-Ethyltryptamine
- Serotonin reuptake inhibitor