Pharmacology of human trace amine‐associated receptors: Therapeutic opportunities and challenges☆

@article{Berry2017PharmacologyOH,
  title={Pharmacology of human trace amine‐associated receptors: Therapeutic opportunities and challenges☆},
  author={Mark D. Berry and R. R. Gainetdinov and Marius C. Hoener and Mohammed Shahid},
  journal={Pharmacology \& Therapeutics},
  year={2017},
  volume={180},
  pages={161–180}
}

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References

SHOWING 1-10 OF 217 REFERENCES

Further Insights Into the Pharmacology of the Human Trace Amine‐Associated Receptors: Discovery of Novel Ligands for TAAR1 by a Virtual Screening Approach

An homology model for the hTAAR1 was used and several agonists and one antagonist, with activities in the low micromolar range were found, which could represent the starting point for the development of more potent and selective TAAR1 ligands.

Insights into the Structure and Pharmacology of the Human Trace Amine‐Associated Receptor 1 (hTAAR1): Homology Modelling and Docking Studies

A homology model for the hTAAR1 receptor was derived and an opportunity to reasonably identify the h TAAR1 key residues involved in ligand recognition and thus define important starting points to design new agonists was provided.

Human and mouse trace amine-associated receptor 1 have distinct pharmacology towards endogenous monoamines and imidazoline receptor ligands.

The successful expression of human and mouse TAAR1 and the characterization of their responses to various natural and synthetic agonists raise new possibilities about the mechanism of some of the imidazoline-related agents.

A renaissance in trace amines inspired by a novel GPCR family.

The potential of trace amines and their receptors for treating neurological and psychiatric diseases.

  • M. D. Berry
  • Biology
    Reviews on recent clinical trials
  • 2007
The aim of the current article is to review the previous studies linking trace amines to human pathology in the context of the recently discovered trace amine receptors and evidence of the existence of Trace amine receptor polymorphisms and mutations associated with such disorders.

International Union of Pharmacology. LXXII. Recommendations for Trace Amine Receptor Nomenclature

This review proposes an official nomenclature designating TAAR1 as the trace amine 1 receptor following the convention of naming receptors after the endogenous agonist, abbreviated to TA1 where necessary.

Trace Amines and the Trace Amine-Associated Receptor 1: Pharmacology, Neurochemistry, and Clinical Implications

TAAR1 is uniquely positioned to exert direct control over DA and 5-HT neuronal firing and release, which has profound implications for understanding the pathophysiology of, and therefore designing more efficacious therapeutic interventions for, a range of neuropsychiatric disorders that involve aminergic dysregulation.

The Trace Amine 1 receptor knockout mouse: an animal model with relevance to schizophrenia

Trace amines have been implicated in a number of neuropsychiatric disorders including depression and schizophrenia. Although long known to modulate neurotransmission indirectly through the release of
...