BQ-3020

BQ-3020 is a selective endothelin receptor (ET_B receptor) agonist that displaces [¹²⁵I] ET-1 binding to ET_B receptors, with an IC₅₀ value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research¹². In Vitro: BQ-3020 (0.01–300 nM, 7 min), produced concentration-dependent relaxationso on PhE-precontracted urothelium-denuded strips^[1].
BQ-3020 (0.01–200 nM, 20 min) causes potent dose-dependent vasoconstriction with EC₅₀ values of 0.57nM in rabbit pulmonary arteries by inhibiting ETB receptors^[2].
. In Vivo: BQ-3020 (3 mg/kg for i.h., single dose) attenuates cancer pain by approximately 50% up to 3 h post-injection compared to PBS-vehicle and contralateral injection in cancer pain mouse model^[3].