A2A-D2

2023-03-18:

A2A-D2 Heteromer #

• Activating-inhibiting Adenylyl Cyclase makes for a real fun time. Net effect? I think it’s actually positive, which is interesting to think about how the receptors may have different weights even with the same G-protein.
• I think it’s Gαq-coupled. Justl like D21 is…

• Activation of the A2A is necessary for them to downregulate, thus antagonism from Istradefylline, etc. prevents this.
  • Modulation of A2a receptor antagonist on D2 receptor internalization and ERK phosphorylation
• Found in indirect Medium Spiny Neurons, in which apparently adenosine is a NAM.
• [Adenosine A 2A-Dopamine D 2 Receptor-Receptor Heteromerization]
  • A2A agonist decreases the affinity of D2 for agonists.
• [Adenosine A2A and dopamine D2 heteromeric receptor complexes and their function]
  • Present in the absence of A2A/D2 agonists, implying that they’re constitutive.
  • could either be A2A-D2 heterodimers and/or higher-order A2A-D2 hetero-oligomers.
    • Heterodimer, or heterotetramer (A2A and D2 both exist as monomers (though D2 technically can oligomerize)). But really it’s been disputed I think on how they oligomerize specifically
• A2A-D2 Heteromers on Striatal Astrocytes: Biochemical and Biophysical Evidence
• Adenosine Receptor Heteromers and their Integrative Role in Striatal Function
  • You thought we were done? There are also mGluR5-A2A-D2 heteromers. And others I’m sure.