Amphetamine, 3,4-methylenedioxymethamphetamine, lysergic acid diethylamide, and metabolites of the catecholamine neurotransmitters are agonists of a rat trace amine receptor.

@article{Bunzow2001Amphetamine3L,
  title={Amphetamine, 3,4-methylenedioxymethamphetamine, lysergic acid diethylamide, and metabolites of the catecholamine neurotransmitters are agonists of a rat trace amine receptor.},
  author={James R. Bunzow and Mark S. Sonders and Seksiri Arttamangkul and LAURA M. Harrison and G Zhang and Denise I. Quigley and Tristan Darland and Katherine L. Suchland and S Pasumamula and James L. Kennedy and Susan B. Olson and R. Ellen Magenis and Susan G. Amara and D K Grandy},
  journal={Molecular pharmacology},
  year={2001},
  volume={60 6},
  pages={
          1181-8
        }
}
The trace amine para-tyramine is structurally and functionally related to the amphetamines and the biogenic amine neurotransmitters. It is currently thought that the biological activities elicited by trace amines such as p-tyramine and the psychostimulant amphetamines are manifestations of their ability to inhibit the clearance of extracellular transmitter and/or stimulate the efflux of transmitter from intracellular stores. Here we report the discovery and pharmacological characterization of a… 

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References

SHOWING 1-10 OF 43 REFERENCES
Trace amines: Identification of a family of mammalian G protein-coupled receptors
TLDR
Using a degenerate PCR approach, 15 G protein-coupled receptors (GPCR) from human and rodent tissues are identified and it is demonstrated that two of these receptors bind and/or are activated by trace amines.
Self-administration of the endogenous trace amines beta-phenylethylamine, N-methyl phenylethylamine and phenylethanolamine in dogs.
TLDR
Data indicate that the endogenous trace amines beta-phenylethylamine, phenylethanolamine and the N-methyl homolog of beta-PNL can function as reinforcers and are compatible with hypotheses that they may play a physiological role in the reinforcement process or in neuropsychiatric disorders.
The release of 3H-noradrenaline by p- and m-tyramines and -octopamines, and the effect of deuterium substitution in alpha-position.
TLDR
The introduction of a beta-OH-group enhances the ability of indirectly acting sympathomimetic amines to mobilize vesicular noradrenaline; the introduction of deuterium in alpha-position enhances this mobilizing effect exclusively when MAO is intact.
Some aspects of basic psychopharmacology: The trace amines
  • A. Boulton
  • Psychology
    Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 1982
Neurotoxic Amphetamine Analogues: Effects in Monkeys and Implications for Humans a
TLDR
Although findings in animals are compelling, observations in humans are less clear, and it remains to be determined whether amphetamine analogues damage central monoaminergic neurons in humans and, if they do, whether functional consequences ensue.
2‐Phenylethylamine: A Modulator of Catecholamine Transmission in the Mammalian Central Nervous System?
TLDR
The neurochemical, neuropharmacological, and neurophysiological findings that lead to propose that PE is a neuromodulator of catecholamine neurotransmission in the CNS are reviewed.
The Forgotten Serine
TLDR
Both Ser-203 and Ser-204 appear to interact with the meta-OH of catecholamines, perhaps through a bifurcated H bond, and the removal of the OH at position 203 led to a significant loss of affinity of antagonists with nitrogen in their heterocyclic ring structure.
Biosynthesis and metabolism of endogenous tyramine and its normal presence in sympathetic nerves.
TLDR
The results suggest that tyramine exists at least partly in sympathetic nerves in many tissues and is present endogenously in rat tissues, including brain, heart, kidney and salivary gland.
Amphetamine: effects on catecholamine systems and behavior.
TLDR
The effects of AMPH in humans have close parallels in animals and at low doses, AMPH increases stereotypic locomotor activity and species-specific stereotypies at higher doses and interferes with intake.
...
1
2
3
4
5
...