ASP7663 is a selective activator of transient receptor potential ankyrin 1 (TRPA1), known to play a role for chemical sensing in the pain pathway. ASP7663 activated human, rat, and mouse TRPA1 receptors with EC50 values of 510, 540, and 500 nM, respectively, and little or no affinity at more than 60 other related receptors, channels and enzymes. ASP7663 enhanced colonic motility and exerted analgesic effects against abdominal pain in mouse models.