Figure 9
From: Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation
Proposed mechanism of positive allosteric modulation of A 2a R function by AEA061. The orthosteric agonist (adenosine) and the positive allosteric modulator, AEA061, bind to topographically distinct sites at the A2AR. Unlike adenosine, AEA061 on its own has no effect on A2AR response. However, it can enhance affinity and efficacy of adenosine and hence the receptor response. 1. Orthosteric (adenosine) agonism; 2. Allosteric (AEA061) affinity (potency) enhancement; 3. allosteric (AEA061) efficacy signaling (capacity) enhancement.