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Published on: March 27, 2018
Functional interaction between trace amine-associated receptor 1 and dopamine D2 receptor.
Stefano Espinoza1, Ali Salahpour, Bernard Masri
1Department of Neuroscience and Brain Technologies, Italian Institute of Technology, Genoa, Italy.
Molecular Pharmacology
|June 15, 2011
Summary
Trace amine-associated receptor 1 (TAAR1) and dopamine D2 receptor (D2R) physically interact, modulating dopamine system functions. This interaction is crucial for TAAR1
Area of Science:
- Neuroscience
- Pharmacology
- Molecular Biology
Background:
- Dopamine receptors modulate functions and behaviors.
- Trace amine-associated receptor 1 (TAAR1) influences the dopaminergic system.
- TAAR1 is a Gα(s) protein-coupled receptor activated by trace amines like β-phenylethylamine (β-PEA).
Purpose of the Study:
- Investigate the biochemical mechanism of TAAR1 and dopamine D2 receptor (D2R) interaction.
- Determine the role of this interaction in D2R signaling and behaviors.
Main Methods:
- Bioluminescence resonance energy transfer (BRET) biosensor for cAMP.
- Coexpression of TAAR1 and D2R in human embryonic kidney 293 cells.
- Assessment of haloperidol-induced striatal c-Fos expression and catalepsy in TAAR1 knockout mice.
Main Results:
- D2R antagonists enhanced TAAR1-mediated cAMP increase.
- TAAR1 and D2R form heterodimers, disrupted by haloperidol.
- Absence of TAAR1 reduced haloperidol-induced effects in mice.
Conclusions:
- TAAR1 and D2R exhibit functional and physical interactions.
- These interactions are critical for TAAR1's in vivo modulation of the dopaminergic system.
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