Trace amine
| Trace amine | |
|---|---|
| Drug class | |
Phenethylamine skeleton
|
|
| Class identifiers | |
| Mechanism of action | Receptor agonist |
| Biological target | Trace amine-associated receptor 1 |
| Chemical class | Endogenous amines with trace occurrence |
| External links | |
| MeSH | C434723 |
Trace amines are an endogenous group of trace amine associated receptor 1 (TAAR1) agonists[1] – and hence, monoaminergic neuromodulators[2][3][4] – that are structurally and metabolically related to classical monoamine neurotransmitters.[5] Compared to the classical monoamines, they are present in trace concentrations.[5] They are distributed heterogeneously throughout the mammalian brain and peripheral nervous tissues and exhibit high rates of metabolism.[5][6] Although they can be synthesized within parent monoamine neurotransmitter systems,[7] there is evidence that suggests that some of them may comprise their own independent neurotransmitter systems.[2]
Trace amines play significant roles in regulating the quantity of monoamine neurotransmitters in the synaptic cleft of monoamine neurons with co-localized TAAR1.[6] They have well-characterized presynaptic amphetamine-like effects on these monoamine neurons via TAAR1 activation;[3][4] specifically, by activating TAAR1 in neurons they promote the release[note 1] and prevent reuptake of monoamine neurotransmitters from the synaptic cleft as well as inhibit postsynaptic neuronal firing.[6][8] Phenethylamine and amphetamine possess analogous pharmacodynamics in human dopamine neurons, as both compounds induce efflux from vesicular monoamine transporter 2 (VMAT2)[7][9] and activate TAAR1 with comparable efficacy.[6] Like dopamine, noradrenaline, and serotonin, the trace amines have been implicated in a vast array of human disorders of affect and cognition, such as ADHD,[3][4][10] depression[3][4] and schizophrenia,[2][3][4] among others.[3][4][10]
A thorough review of trace amine-associated receptors that discusses the historical evolution of this research particularly well is that of Grandy.[11]
List of trace amines
The human trace amines include:
- Phenethylamines (related to catecholamines):
- Thyronamine compounds:
- Tryptamine[4][6]
While not trace amines themselves, the classical monoamines dopamine, norepinephrine, serotonin, and histamine are all partial TAAR1 agonists in humans.[6] N-Methyltryptamine and N,N-dimethyltryptamine are endogenous amines in humans, however their human TAAR1 binding has not yet been documented.[2]
See also
Notes
- ↑ Certain trace amines (e.g., phenethylamine) functionally inhibit the vesicular monoamine transporter VMAT2, while others do not (e.g., octopamine). The trace amines that do not inhibit VMAT2 function in monoamine neurons do not release neurotransmitters as effectively as those which do.
References
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