The binding affinity for native (K_i=0.067 nM) and cloned human (K_i=0.070 nM) and rhesus (K_i=0.079 nM) receptors was similar for ubrogepant, with relatively lower affinities for CGRP receptors of other species (ranging from K_i=9.6 to 47 nM). Ubrogepant potently blocked human α-CGRP–stimulated cAMP response (IC₅₀ of 0.08) and exhibited highly selective antagonist activity in relation to the CGRP receptor compared with other members of the human calcitonin receptor family. Ubrogepant produced concentration-dependent inhibition of CIDV in the rhesus forearm. Population pharmacokinetic/pharmacodynamic modeling of CIDV suggested that ubrogepant has a mean EC₅₀ of 3.2 nM, which may be correlated with an EC₉₀ of approximately 29 nM.