BAY73-1449是一种选择性前列环素受体(prostacyclinreceptor,IP)的拮抗剂,在人HEL细胞和大鼠DRG的cAMP分析中具有很高的效价(IC50值小于0.1nM)。BAY73-1449可用于降血压的研究。
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BAY 73-1449 is a selective antagonist of prostacyclin receptor (IP), with high potency (IC50 of less than 0.1 nM) in cAMP assays in Human HEL cells and rat DRG. BAY 73-1449 can be used in the research of lowering blood pressure[1].
BAY 73-1449 (0.1-1 mg/kg; i.v.) does not significantly reduce mesenteric inflow, but significantly reduces splenic shunt vessel outflow in rats[1].BAY 73-1449 (1-5 mg/kg, s.c. once daily for 7 d) has no effects on the degree of porto-systemic shunting in rats[1].BAY 73-1449 (1 mg/kg, s.c. once daily for 7 d), has no effects on portal pressures in rats[1]. Animal Model: Male Wistar rats (250-350 g) are ligated portal vein[1]
[1]. Bexis S, et, al. Vascular actions of the prostacyclin receptor antagonist BAY 73-1449 in the portal hypertensive rat. Eur J Pharmacol. 2008 Aug 20;590(1-3):322-6.
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