LU302872

LU302872 is a **glycerinic acid derivative** and **dual endothelin receptor antagonist** that exhibits high and balanced affinity for both ETA and ETB receptors with Ki values of 2.2 and 5.8 nmol/L respectively. It demonstrates high oral bioavailability and effectiveness in multiple species for both ETA and ETB-mediated responses. The compound has shown efficacy in inhibiting big ET-1-induced blood pressure increases in rats and bronchospasm in guinea pigs. In human prostate tissue studies, LU302872 dose-dependently inhibited ET-1-induced contractions and was identified as a suitable candidate for testing in **benign prostate hyperplasia (BPH)**. However, research also indicated that nonselective endothelin receptor antagonism with related compounds can be detrimental after myocardial infarction, particularly when started early post-MI.