Tag: SRI: Serotonin Reuptake Inhibitor

What is Brofaromine?

Published on by Andrew Marshall1 Comment

Introduction

Brofaromine (proposed brand name Consonar) is a reversible inhibitor of monoamine oxidase A (RIMA) discovered by Ciba-Geigy. The compound was primarily researched in the treatment of depression and anxiety but its development was dropped before it was brought to market.

Brofaromine also acts as a serotonin reuptake inhibitor, and its dual pharmacologic effects offered promise in the treatment of a wide spectrum of depressed patients while producing less severe anticholinergic side effects in comparison with older standard drugs like certain of the tricyclic antidepressants.

Pharmacology

Brofaromine is a reversible inhibitor of monoamine oxidase A (RIMA, a type of monoamine oxidase inhibitor (MAOI)) and acts on epinephrine (adrenaline), norepinephrine (noradrenaline), serotonin, and dopamine. Unlike standard MAOIs, possible side effects do not include cardiovascular complications (hypertension) with encephalopathy, liver toxicity or hyperthermia.

Refer to Moclobemide.

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What is a Serotonin Releasing Agent?

Published on by Andrew Marshall3 Comments

Introduction

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.

SSRAs have been used clinically as appetite suppressants, and they have also been proposed as novel antidepressants and anxiolytics with the potential for a faster onset of action and superior efficacy relative to the selective serotonin reuptake inhibitors (SSRIs).

A closely related type of drug is a serotonin reuptake inhibitor (SRI).

Examples and Use of SRAs

Amphetamines like MDMA, MDEA, MDA, and MBDB, among other relatives, are recreational drugs termed entactogens. They act as serotonin-norepinephrine-dopamine releasing agents (SNDRAs) and also agonise serotonin receptors such as those in the 5-HT2 subfamily. 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 additional action of potent agonism of the 5-HT2B receptor. The designer drug 4-methylaminorex, which is an SNDRA and 5-HT2B agonist, has 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 SNDRAs and non-selective serotonin receptor agonists that were originally thought to be monoamine oxidase inhibitors and were formerly used as antidepressants. They have since been discontinued and are now encountered solely as recreational drugs.

Indeloxazine is an SRA and norepinephrine reuptake inhibitor that was formerly used as an antidepressant, nootropic, and neuroprotective.

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)
  • 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)

This page is based on the copyrighted Wikipedia article < https://en.wikipedia.org/wiki/Serotonin_releasing_agent >; it is used under the Creative Commons Attribution-ShareAlike 3.0 Unported License (CC-BY-SA). You may redistribute it, verbatim or modified, providing that you comply with the terms of the CC-BY-SA.

What is a Serotonin Reuptake Inhibitor?

Published on by Andrew Marshall6 Comments

Introduction

A serotonin reuptake inhibitor (SRI) is a type of drug which acts as a reuptake inhibitor of the neurotransmitter serotonin (5-hydroxytryptamine, or 5-HT) by blocking the action of the serotonin transporter (SERT). This in turn leads to increased extracellular concentrations of serotonin and, therefore, an increase in serotonergic neurotransmission.

Outline

A SRI is a type of monoamine reuptake inhibitor (MRI); other types of MRIs include dopamine reuptake inhibitors and norepinephrine reuptake inhibitors.

SRIs are not synonymous with selective serotonin reuptake inhibitors (SSRIs), as the latter term is usually used to describe the class of antidepressants of the same name, and because SRIs, unlike SSRIs, can either be selective or non-selective in their action. For example, cocaine, which non-selectively inhibits the reuptake of serotonin, norepinephrine, and dopamine, is a SRI but not an SSRI.

SRIs are used predominantly as antidepressants (e.g., SSRIs, SNRIs, and TCAs), though they are also commonly used in the treatment of other psychological conditions such as anxiety disorders and eating disorders. Less often, SRIs are also used to treat a variety of other medical conditions including neuropathic pain and fibromyalgia (e.g. duloxetine, milnacipran), and premature ejaculation (e.g. dapoxetine) as well as for dieting (e.g. sibutramine). Additionally, some clinically used drugs such as chlorpheniramine, dextromethorphan, and methadone possess SRI properties secondarily to their primary mechanism of action(s) and this contributes to their side effect and drug interaction profiles.

A closely related type of drug is a serotonin releasing agent (SRA), an example of which is fenfluramine.

This page is based on the copyrighted Wikipedia article < https://en.wikipedia.org/wiki/Serotonin_reuptake_inhibitor >; it is used under the Creative Commons Attribution-ShareAlike 3.0 Unported License (CC-BY-SA). You may redistribute it, verbatim or modified, providing that you comply with the terms of the CC-BY-SA.