产品描述:
BPTU is an allosteric antagonist of the purinergic P2Y1 receptor (Ki = 6 nM for the human receptor).{53133,53134} BPTU is selective for P2Y1 over P2Y2, P2Y6, P2Y11, P2Y12, and P2Y14 receptors (Kis = ≥3,500 nM).{53133} It inhibits platelet aggregation in human platelet-rich plasma (hPRP; IC50 = 2.1 µM). BPTU reduces thrombus weight by 68% in a rat model of iron chloride-induced arterial thrombosis and prolongs provoked cuticle and mesenteric bleeding time in rats when administered intravenously as a 10 mg/kg bolus dose followed by a 10 mg/kg per hour infusion. It also inhibits contractions induced by electrical field stimulation in isolated muscle strips from rat and mouse colon (EC50s = 0.5 and 0.1 µM, respectively) and antrum (EC50s = 9 and 0.3 µM, respectively).{53134}