Nexopamil racemate is the racemate of Nexopamil. Nexopamil is a combined Ca2+/5-HT2 antagonist on platelet aggregation in vitro and on thrombus formation in vivo.

Serotonin-induced platelet aggregation in dog platelet-rich plasma (PRP) in vitro was most potently inhibited by ketanserin (IC50 0.55 x 10(-8) M), followed by nexopamil (IC50) 0.81 x 10(-7) M) and gallopamil (IC50 1.76 x 10(-6) M). Because serotonin is an important pathophysiologic mediator in unstable angina, 5-HT2 receptor antagonism should be of considerable benefit by preventing platelet activation and aggregation.?The combination with calcium-antagonistic activity leads to an increase in coronary blood flow (CBF) and a decrease in cardiac oxygen demand.

Nexopamil (0.05 mg/kg) completely abolished CFRs during the first 30 min after application without significantly altering hemodynamics.?The same effect was noted with 0.02 mg/kg ketanserin (5-HT2/alpha 1 antagonist).?The Ca2+ antagonist gallopamil reduced CFRs only in the highest hemodynamically tolerable dose by 40%.

116759-35-4

C24H40N2O3

404.59

Nexopamil racemate

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years