Site-directed mutagenesis of the human adenosine A2A receptor. Critical involvement of Glu13 in agonist recognition.

A glutamic acid residue in the first transmembrane domain of the human adenosine A2A receptor was mutated to glutamine. Radioligand binding studies on COS-7 cell membranes expressing either the wild-type or the mutant receptor revealed that the affinity of the prototypic agonist CGS21680 (2-[4-[(2-carboxyethyl)phenyl]ethylamino]-5'-N… CONTINUE READING