Homodimerization of adenosine A₁ receptors in brain cortex explains the biphasic effects of caffeine.

@article{Gracia2013HomodimerizationOA,
  title={Homodimerization of adenosine A₁ receptors in brain cortex explains the biphasic effects of caffeine.},
  author={Eduard Gracia and E. {\'A}lvarez Moreno and Antoni Cort{\'e}s and Carme Llu{\'i}s and Josefa Mallol and Peter J. McCormick and Enric I. Canela and Vicent Casad{\'o}},
  journal={Neuropharmacology},
  year={2013},
  volume={71},
  pages={56-69}
}
Using bioluminescence resonance energy transfer and proximity ligation assays, we obtained the first direct evidence that adenosine A₁ receptors (A₁Rs) form homomers not only in cell cultures but also in brain cortex. By radioligand binding experiments in the absence or in the presence of the A₁Rs allosteric modulator, adenosine deaminase, and by using the two-state dimer receptor model to fit binding data, we demonstrated that the protomer-protomer interactions in the A₁R homomers account for… CONTINUE READING