Releasing agent: Difference between revisions

Releasing agents act to varying extents on the monoamine neurotransmitters. Some will induce the release of all three monoamines; an example of this is [[MDMA]]. Others are more selective as [[methamphetamine]] is a potent releasing agent of dopamine and noradrenaline, but is a weak releaser of serotonin. A majority of releasing agents are non-selective, but there are currently a limited amount of agents that release serotonin (SRAs) or norephinephrine (NRAs) selectively; no selective dopamine releasing agents are currently known. Many tryptamines, such as [[DMT]], [[DiPT]], and [[psilocin]], are selective serotonin releasing agents in addition to their other pharmacological effects.<ref>Blough BE, Landavazo A, Decker AM, Partilla JS, Baumann MH, Rothman RB (October 2014). "Interaction of psychoactive tryptamines with biogenic amine transporters and serotonin receptor subtypes". Psychopharmacology 231 (21): 4135–44. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/24800892</ref>

Many releasing agents, notably many of those derived from [[amphetamine]], have been found to be neurotoxic to [[serotonin]] and/or [[dopamine]] neurons via damage to axons and dendrites, enzymes, mitochondria, DNA, plasmalemmal and vesicular transporters, and the cell membrane, ultimately causing cell death as a result.  

The neurotoxicity of some of these drugs is believed to be caused by oxidative stress induced by the generation of reactive oxygen species or free radicals, highly reactive particles that rip apart proteins and induce chain reactions of destruction. The free radicals are thought to be generated as byproducts when either the base compound or one or more of its metabolites are broken down by the enzymes monoamine oxidase (MAO-B) and/or cyclooxygenase (COX). It is thought hyperthermia and concurrent serotonin-dopamine release may also play a major role in augmenting damage.