(4E)-SUN9221

(4E)-SUN9221 is a potent antagonist of α1-adrenergic receptor and 5-HT2 receptor, with antihypertensive and anti-platelet aggregation activities. In Vitro: (4E)-SUN9221 potently inhibits collagen-, ADP- and epinephrine-induced platelet aggregation, with IC₅₀s of 10 nM, 35 nM, 14 nM, respectively, in human platelet-rich plasma (PRP). (4E)-SUN9221 displays potent α1-adrenergic antagonist activity (pA2 =8.89±0.21) and 5-HT2 antagonist activity (pA2 =8.74±0.22)^[1]. In Vivo: (4E)-SUN9221 (1, 3, 10 mg/kg, p.o.) reduces the blood pressure in a dose-dependent manner in conscious spontaneously hypertensive rats (SHR). (4E)-SUN9221 (3 mg/kg) exhibits antihypertensive activity in SHR^[1].