Discovery of a number of potent and selective P2X7Rs antagonists has been instrumental in studying the receptor in human and rodent. Some of these ligands including AZD9056193 and CE-224535194 were developed for the treatment of inflammation but failed to exhibit benefits in patients.194 Other existing and understudy ligands of the P2X7 receptors include A438079, A740003, A804598, A839977, AZ1060612, AZ11645373, GSK1482160, and GW791343.9,195