Serotonin releasing agent

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Serotonin

A serotonin releasing agent (SRA) is a type of drug which induces the release of serotonin from the pre-synaptic neuron into the synapse. This in turn leads to increased extracellular concentrations of serotonin and therefore an increase in serotonergic neurotransmission.

Main article: Releasing agent

Clinical and recreational use

MDMA, MDEA, MDA, and MBDB, among other relatives (see MDxx), are recreational drugs termed empathogen-entactogens and are often used at all-night dance parties known as raves. They act as releasing agents of not only serotonin, but of dopamine and norepinephrine as well.

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.

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.

αET and αMT are serotonin, norepinephrine, and dopamine releasing agents which were formerly used as antidepressants in Russia. They are now encountered solely as recreational drugs similarly to the MDxx series.

List of SRAs

Pharmaceutical drugs
Street drugs
Research chemicals
Trace amines

See also

References

  1. ↑ Krebs KM, Geyer MA (1993). "Behavioral characterization of alpha-ethyltryptamine, a tryptamine derivative with MDMA-like properties in rats". Psychopharmacology 113 (2): 284–7. doi:10.1007/BF02245712. PMID 7855195. 
  2. ↑ 2.0 2.1 2.2 2.3 2.4 2.5 2.6 2.7 2.8 Nagai F, Nonaka R, Satoh Hisashi Kamimura K (March 2007). "The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain". European Journal of Pharmacology 559 (2–3): 132–7. doi:10.1016/j.ejphar.2006.11.075. PMID 17223101. 
  3. ↑ Marsden CA (November 1979). "Evidence for the release of hippocampal 5-hydroxytryptamine by alpha-methyltryptamine proceedings". British Journal of Pharmacology 67 (3): 438P–439P. PMC 2043998. PMID 497560. 
  4. ↑ Yamaguchi T, Ohyama M, Suzuki M, et al. (September 1998). "Neurochemical and behavioral characterization of potential antidepressant properties of indeloxazine hydrochloride". Neuropharmacology 37 (9): 1169–76. doi:10.1016/S0028-3908(98)00009-4. PMID 9833647. 
  5. ↑ Driessen B, Reimann W (January 1992). "Interaction of the central analgesic, tramadol, with the uptake and release of 5-hydroxytryptamine in the rat brain in vitro". British Journal of Pharmacology 105 (1): 147–51. doi:10.1111/j.1476-5381.1992.tb14226.x. PMC 1908625. PMID 1596676. 
  6. ↑ Bamigbade TA, Davidson C, Langford RM, Stamford JA (September 1997). "Actions of tramadol, its enantiomers and principal metabolite, O-desmethyltramadol, on serotonin (5-HT) efflux and uptake in the rat dorsal raphe nucleus". British Journal of Anaesthesia 79 (3): 352–6. doi:10.1093/bja/79.3.352. PMID 9389855. 
  7. ↑ Reimann W, Schneider F (May 1998). "Induction of 5-hydroxytryptamine release by tramadol, fenfluramine and reserpine". European Journal of Pharmacology 349 (2–3): 199–203. doi:10.1016/S0014-2999(98)00195-2. PMID 9671098. 
  8. ↑ Eriksson E, Engberg G, Bing O, Nissbrandt H (March 1999). "Effects of mCPP on the extracellular concentrations of serotonin and dopamine in rat brain". Neuropsychopharmacology 20 (3): 287–96. doi:10.1016/S0893-133X(98)00070-0. PMID 10063489. 
  9. ↑ Baumann MH, Ayestas MA, Dersch CM, Rothman RB (May 2001). "1-(m-chlorophenyl)piperazine (mCPP) dissociates in vivo serotonin release from long-term serotonin depletion in rat brain". Neuropsychopharmacology 24 (5): 492–501. doi:10.1016/S0893-133X(00)00221-9. PMID 11282249. 
  10. ↑ 10.0 10.1 10.2 10.3 Wölfel R, Graefe KH (February 1992). "Evidence for various tryptamines and related compounds acting as substrates of the platelet 5-hydroxytryptamine transporter". Naunyn-Schmiedeberg's Archives of Pharmacology 345 (2): 129–36. doi:10.1007/BF00165727. PMID 1570019. 

Further reading

Monoamine releasing agents
Substituted amines
Indanylamines
  • 2-Aminoindane (2-AI)
  • ETAI
  • IAI
  • Indanylaminopropane (IAP)
  • Indanylmethylaminopropane (IMP)
  • MDAI
  • MDMAI
  • MMAI
  • TAI
Indolylamines
Phenylalkylamines
Amine containing
Unclassified/unsorted
Phenylalkylamines
Cyclized phenyl-
alkylamines
  • Aminoindanes: 5-IAI
  • AMMI
  • ETAI
  • MDAI
  • MDMAI
  • MMAI
  • TAI
    Aminotetralins: 6-CAT
  • MDAT
  • MDMAT
Tryptamines
Others
Naphthylisopropylamine
Anxiolytics (N05B)
GABAA
PAMs
non-N05B
α2δ VDCC Blockers
5-HT1A Agonists
H1 Antagonists
CRH1 Antagonists
NK2 Antagonists
MCH1 antagonists
mGluR2/3 Agonists
mGluR5 NAMs
TSPO agonists
σ1 agonists
Antidepressants
Others

M: PSO/PSI

mepr

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc (eval/thrp), drug (N5A/5B/5C/6A/6B/6D)

Antiobesity agents/Anorectics (A08)
Central
Drinabant§ • Ibipinabant§ • Otenabant§ • Rimonabant‡ • Rosonabant§ • Surinabant§ • Taranabant§
Others
5-HTP • Galactomannan (Guar gum) • Glucomannan • L-DOPA • L-Phenylalanine • L-Tryptophan • L-Tyrosine • Lorcaserin • Lu AA-33810 • Metformin • Naltrexone • Naloxone • Oxyntomodulin • P57 • Peptide YY • Topiramate • Yohimbine (Yohimbe) • Zonisamide
Peripheral

M: NUT

cof, enz, met

noco, nuvi, sysi/epon, met

drug (A8/11/12)

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