BUR1 is a BMP upregulator (EC50: 98 nM) and activates BMPRII signalling. BUR1 induces BMP2 and PTGS2 expression. BUR1 reversed pulmonary arterial pressure in Monocrotaline induced rats.
BUR1 (0.2 μM, 15 min-24 h) increases expression of Inhibitor of DNA binding 1 (Id1) and phosphorylation of Smad1/5 in PAECs[1].
BUR1 (4.5 mg/day, i.g., 3 weeks) reverses MCT-induced pulmonary arterial pressure and right ventricular systolic pressure in rats[1].
References:
[1]. Xing Y, et al. A novel piperidine identified by stem cell-based screening attenuates pulmonary arterial pertension by regulating BMP2 and PTGS2 levels. Eur Respir J. 2018 Apr 4;51(4):1702229.