Guanfacine is an a2-adrenergic receptor (a2-AR) agonist with Ki values of 93, 1,380, and 3,890 nM for a2A-, a2B-, and a2C-ARs, respectively, in a radioligand binding assay.{40326} It has EC50 values of 52, 288, and 602 nM for a2A-, a2B-, and a2C-ARs, respectively, for stimulated [35S]GTP?S binding....