CJ-033466

CJ-033466 is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4. It induces cAMP accumulation in HEK293 cells expressing human 5-HT4D receptors and relaxation of rat tunica muscularis mucosae strips (EC50s = 0. and 1. nM, respectively). CJ-033466 selectively binds to 5-HT4D over 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, and 5-HT2B receptors (Kis = 1. >4,820, >5,070, 2,150, 1,400, and 2,900 nM, respectively) and 5-HT3, 5-HT7, and dopamine D2 receptors (Kis = 4,590, >3,890, and 2,150 nM, respectively), as well as a panel of greater than 50 additional receptors at 1,000 nM. CJ-033466 (0. mg/kg) increases gastric antral motility in conscious dogs in the fasted or postprandial states. It reverses clonidine-induced decreases in gastric emptying in a dog model of gastroparesis. CJ-033466 also induces superoxide production in a light-dependent manner and is phototoxic to NIH3T3 fibroblasts (IC50s = 11. and 203. µg/ml in the presence and absence of light, respectively).. Solulibility: DMSO: Sparingly soluble: 1-10 mg/mL: Ethanol: Slightly soluble: 0.1-1 mg/mL.