Development of a Peripherally Restricted 5-HT_2B Partial Agonist for Treatment of Pulmonary Arterial Hypertension.

ABSTRACT: Ligands for the serotonin 2B receptor (5-HT_2B) have shown potential to treat pulmonary arterial hypertension in preclinical models but cannot be used in humans because of predicted off-target neurological effects. The aim of this study was to develop novel systemically restricted compounds targeting 5-HT_2B. Here, we show that mice treated with VU6047534 had decreased RVSP compared with control treatment in both the prevention and intervention studies using Sugen-hypoxia. VU6047534 is a novel 5-HT_2B partial agonist that is peripherally restricted and able to both prevent and treat Sugen-hypoxia-induced pulmonary arterial hypertension. We have synthesized and characterized a structurally novel series of 5-HT_2B ligands with high potency and selectiv

SUBMITTER: Valentine MS 

PROVIDER: S-EPMC10714182 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature