(4E)-SUN9221是一种有效的α1-adrenergicreceptor和5-HT2receptor拮抗剂，具有抗高血压和抗血小板聚集的功效。
CAS：222318-55-0
分子式：C25H31FN4O3
分子量：454.54
纯度：98%
存储：Store at -20°C

Background:

(4E)-SUN9221 is a potent antagonist of α1-adrenergic receptor and 5-HT2 receptor, with antihypertensive and anti-platelet aggregation activities.

(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].

(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].

[1]. Mizuno A, et al. Synthesis and pharmacological evaluation of pyrroloazepine derivatives as potent antihypertensive agents with antiplatelet aggregation activity. Chem Pharm Bull (Tokyo). 1999 Feb;47(2):246-56.