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PRX-08066 is a selective antagonist of 5-hydroxytryptamine receptor 2B (5-HT2BR) with Ki value of 3.4nM [1].

PRX-08066 is found to causes selective vasodilation of pulmonary arteries and is developed to treat for pulmonary arterial hypertension (PAH). In the in vitro studies, PRX-08066 shows effects on the vascular muscularization induced by 5-HT. It inhibits 5-HT induced mitogen-activated protein kinase activation with IC50 value of 12nM. In addition, it significantly reduces thymidine incorporation in CHO cells expressing human 5-HT2BR with IC50 value of 3nM. In both mice and rat models, PRX-08066 reverses the hypoxia-dependent increase in right ventricular systolic pressure. Besides that, PRX-08066 is also found to have anti-proliferative and anti-fibrotic effects. It inhibits the secretion of 5-HT, the phosphorylation of ERK1/2 and synthesis of profibrotic growth factor. Moreover, PRX-08066 inhibits the proliferation of the small intestinal neuroendocrine tumor cell line KRJ-I with IC50 value of 4.6nM [1, 2].

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