Casopitant (GW679769) is a potent, selective, orally active, and brain penetrant neurokinin 1 (NK1) receptor antagonist with pKi of 9.48.
Casopitant (GW679769) inhibit SP-induced release of cytosolic Ca2+ in h-NK1-CHO cells using FLIPR with pA2 value of 9.7.
Casopitant (GW679769) possesses subnanomolar affinity and high selectivity for the NK1 receptors without sign of pharmacological species difference between human and gerbil NK1 receptors.
Casopitant (GW679769) possesses an anxiolytic-like property, confirming the preclinical profile of NK1 receptor antagonists on emotional behavior.
