PRX-08066

PRX-08066 Maleic acid is a selective 5-HT2BR antagonist. It has high selectivity over the closely related 5-HT2A and 5-HT2C receptors and other receptor targets.

This selective 5-hydroxytryptamine (serotonin) receptor antagonist (FW = 517.96 g/mol; CAS = 866206-55-5), also named 5-((4-(6-chlorothieno[2,3- d]pyrimidin-4-ylamino)piperidin-1-yl)methyl)-2-fluorobenzonitrile, targets 5-HT2B (IC50 of 3.4 nM), showing high selectivity over the closely related 5-HT2A, 5-HT2C and other receptors and preventing the severity of pulmonary arterial hypertension in the monocrotaline (MCT)-induced rat pulmonary artery hypertension model. PRX-08066 significantly attenuates the elevation in pulmonary artery pressure and right ventricular hypertrophy, thereby improving cardiac function. Targeting the 5-5-HT2B receptor also appears be an effective antiproliferative and antifibrotic strategy for small intestinal neuroendocrine tumors (SI-NETs), because it inhibits tumor microenvironment fibroblasts as well as NET cells.