pd156707

**PD156707** is an orally active, nonpeptide, and highly selective antagonist of the endothelin-A receptor, sometimes referred to as ETA receptor antagonist[2][3][5][10][13][14]. It was developed as a research compound to block the actions of endothelin-1 on the endothelin-A receptor, thereby inhibiting vasoconstrictive and pathological vascular remodeling responses[2][3][5][10][13]. In preclinical studies, PD156707 has demonstrated potent inhibition of endothelin-1-induced increases in renal vascular resistance, significant oral bioavailability, and favorable pharmacokinetic properties[2][3][9]. The compound’s selectivity for the endothelin-A receptor (ETA) over endothelin-B (ETB) is demonstrated by its very low nanomolar affinity for ETA (Ki ~ 0.17 nM) and much weaker affinity for ETB (Ki > 130 nM)[8]. Its primary indications in preclinical studies have included models of congestive heart failure, pulmonary hypertension, and cerebral ischemia, but not approved for clinical use[9][16].

Other names

sodium 2-benzo[1,3]dioxol-5-yl-4-(4-methoxy-phenyl)-4-oxo-3-(3,4,5-trimethoxy-benzyl)-but-2-enoate