Serotonin releasing agent
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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
Contents |
Clinical and recreational use
Edit
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 SRAsEdit
- Pharmaceutical Drugs
- Amphetamines
- Chlorphentermine (Apsedon, Desopimon, Lucofen)
- Cloforex (Oberex)
- Clortermine (Voranil)
- Dexfenfluramine (Redux)
- Fenfluramine (Pondimin, Fen-Phen)
- Norfenfluramine (metabolite of fenfluramine)
- Oxazolines
- Aminorex (Menocil)
- Tryptamines
- Etryptamine (Monase)[1]
- Metryptamine (Indopan)[2][2][3]
- Others
- Street Drugs
- Amphetamines
- 4-Methylthioamphetamine (4-MTA)
- Methylenedioxyamphetamine (MDA)
- Methylenedioxyethylamphetamine (MDEA)
- Methylenedioxymethamphetamine (MDMA; "Ecstasy")[2]
- para-Methoxyamphetamine (PMA)
- para-Methoxyethylamphetamine (PMEA)
- para-Methoxymethamphetamine (PMMA)
- Cathinones
- Oxazolines
- 4-Methylaminorex (4-MAR)
- Piperazines
- meta-Chlorophenylpiperazine (mCPP)[2][8][9]
- Methoxyphenylpiperazine (MeOPP)[2]
- para-Fluorophenylpiperazine (pFPP; Fluoperazine)
- Trifluoromethylphenylpiperazine (TFMPP)
- Tryptamines
- 5-Methoxyalphaethyltryptamine (5-MeO-AET)
- 5-Methoxyalphamethyltryptamine (5-MeO-AMT)[2]
- Research Chemicals
- Aminoindanes
- 5-Iodoaminoindane (5-IAI)
- Ethyltrifluoromethylaminoindane (ETAI)
- Indanylaminopropane (IAP)
- Indanylmethylaminopropane (IMP)
- Methoxymethylaminoindane (MMAI)
- Methylenedioxyaminoindane (MDAI)
- Methylenedioxymethylaminoindane (MDMAI)
- Trifluoromethylaminoindane (TAI)
- Aminotetralins
- 8-Hydroxydipropylaminotetralin (8-OH-DPAT)[10]
- 6-Chloroaminotetralin (6-CAT)
- Methylenedioxyaminotetralin (MDAT)
- Amphetamines
- 3-Methylamphetamine (3-MA)
- 4-Methylamphetamine (4-MA)
- 4-Methylmethamphetamine (4-MMA)
- 5-(2-Aminopropyl)-2,3-dihydrobenzofuran (5-APDB)
- 6-(2-Aminopropyl)-2,3-dihydrobenzofuran (6-APDB)
- Amiflamine
- Benzodioxylbutanamine (BDB)[2]
- Ethylenedioxymethamphetamine (EDMA)
- Etolorex
- Methoxymethylamphetamine (MMA)
- Methoxymethylenedioxyamphetamine (MMDA)
- Methoxymethylenedioxymethylamphetamine (MMDMA)
- Methylbenzodioxolbutanamine (MBDB)[2]
- Methylenedioxyhydroxyamphetamine (MDOH)
- Methylenedioxyhydroxymethamphetamine (MDHMA)
- para-Bromoamphetamine (PBA)
- para-Chloroamphetamine (PCA)
- para-Iodoamphetamine (PIA)
- Tryptamines
- 5-Carboxamidotryptamine (5-CT)[10]
- 5-Methoxytryptamine (5-MT)[10]
- Others
- Naphthylaminopropane (NAP; PAL-287)
- Trace Amines
See alsoEdit
- Releasing agent
- Selective serotonin releasing agent
- Serotonin reuptake inhibitor
- Dopamine releasing agent
- Norepinephrine releasing agent
ReferencesEdit
- ↑ Krebs KM, Geyer MA (1993). Behavioral characterization of alpha-ethyltryptamine, a tryptamine derivative with MDMA-like properties in rats. Psychopharmacology 113 (2): 284–7.
- ↑ 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.
- ↑ Marsden CA (November 1979). Evidence for the release of hippocampal 5-hydroxytryptamine by alpha-methyltryptamine [proceedings]. British Journal of Pharmacology 67 (3): 438P–439P.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
Further readingEdit
- Nichols DE, Marona-Lewicka D, Huang X, Johnson MP (1993). Novel serotonergic agents. Drug Design and Discovery 9 (3-4): 299–312.
- Marona-Lewicka D, Nichols DE (December 1997). The Effect of Selective Serotonin Releasing Agents in the Chronic Mild Stress Model of Depression in Rats. Stress (Amsterdam, Netherlands) 2 (2): 91–100.
- Scorza C, Silveira R, Nichols DE, Reyes-Parada M (July 1999). Effects of 5-HT-releasing agents on the extracellullar hippocampal 5-HT of rats. Implications for the development of novel antidepressants with a short onset of action. Neuropharmacology 38 (7): 1055–61.
- Rothman RB, Baumann MH (April 2002). Serotonin releasing agents. Neurochemical, therapeutic and adverse effects. Pharmacology, Biochemistry, and Behavior 71 (4): 825–36.
| Antidepressants (ATC N06A) edit | ||
|---|---|---|
| Monoamine oxidase inhibitors (MAOI) | Harmaline, Iproclozide, Iproniazid, Isocarboxazid, Nialamide, Phenelzine, Selegiline, Toloxatone, Tranylcypromine | |
| Reversible inhibitor of monoamine oxidase A (RIMA) | Brofaromine, Moclobemide | |
| Dopamine reuptake inhibitor (DARI) | Amineptine, Phenmetrazine, Vanoxerine, Modafinil | |
| Norepinephrine-dopamine reuptake inhibitors | Bupropion | |
| Norepinephrine reuptake inhibitor (NRI) or (NARI) | Atomoxetine, Maprotiline, Reboxetine, Viloxazine | |
| Serotonin-norepinephrine reuptake inhibitor (SNRI) | Duloxetine, Milnacipran, Venlafaxine | |
| Selective serotonin reuptake inhibitor (SSRI) | Alaproclate, Etoperidone, Citalopram, Escitalopram, Fluoxetine, Fluvoxamine, Paroxetine, Sertraline, Zimelidine | |
| Selective serotonin reuptake enhancer (SSRE) | Tianeptine | |
| Tricyclic antidepressants (TCA) | Amitriptyline, Amoxapine, Butriptyline, Clomipramine, Desipramine, Dibenzepin, Dothiepin, Doxepin, Imipramine, Iprindole, Lofepramine, Melitracen, Nortriptyline, Opipramol, Protriptyline, Trimipramine | |
| Tetracyclic antidepressants | Maprotiline, Mianserin, Nefazodone, Trazodone | |
| Noradrenergic and specific serotonergic antidepressant (NaSSA) Mirtazapine | ||
Psycholeptics: anxiolytics (N05B)
| |
|---|---|
| Benzodiazepine | Diazepam - Chlordiazepoxide - Medazepam - Oxazepam - Potassium clorazepate - Lorazepam - Adinazolam - Bromazepam - Clobazam - Ketazolam - Prazepam - Alprazolam - Halazepam - Pinazepam - Camazepam - Nordazepam - Fludiazepam - Ethyl loflazepate - Etizolam - Clotiazepam - Cloxazolam - Tofisopam |
| Diphenylmethane | Hydroxyzine - Captodiame |
| Carbamates | Meprobamate - Emylcamate - Mebutamate |
| Dibenzo-bicyclo-octadiene | Benzoctamine |
| Azaspirodecanedione (serotonin receptor agonist) | Buspirone - Gepirone - Tandospirone |
| Other | Mephenoxalone - Gedocarnil - Etifoxine |
Analgesics (N02A, N02B) | |
|---|---|
| Opioids |
Buprenorphine, Butorphanol, Codeine, Dextropropoxyphene, Diamorphine, Dihydrocodeine, Fentanyl, Hydrocodone, Hydromorphone, Ketobemidone, Levorphanol, Methadone, Morphine, Nicomorphine, Opium, Oxycodone, Oxymorphone, Pethidine, Tramadol, Tapentadol |
| Salicylic acid and derivatives |
Aspirin (Acetylsalicylic Acid), Diflunisal, Ethenzamide, Salicin, Salicylamide · See also: NSAIDs |
| Pyrazolones | |
| Cannabinoids | |
| Anilides | |
| Others |
Ziconotide, Ibuprofen, Ketoprofen, Mefenamic Acid, Naproxen, Diclofenac, Flurbiprofen, Diflunisal, Indomethacin, Ketorolac, Meloxicam, Piroxicam |
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