Key result
Sarpogrelate, a 5-HT2A receptor antagonist, significantly inhibited thrombus formation by 75.8% and reduced the arterial occlusion ratio from 100% to 40% in diabetic rats.
Why the study?
Does sarpogrelate reduce thrombus formation and endothelial injury in diabetic rat models and human umbilical vein endothelial cells?
Does sarpogrelate reduce thrombus formation and endothelial injury in diabetic rat models and human umbilical vein endothelial cells?
Absolute Event Rate: 40% vs 100%
p-value: p=<0.01
Sarpogrelate, a 5-HT2A receptor antagonist, reduces thrombosis and endothelial injury in diabetic models, suggesting therapeutic potential for diabetic vascular complications.
May support 5-HT2A blockade in diabetic thrombosis models; leaves open human translation.
To clarify the involvement of 5-hydroxytryptamine (5-HT) in promotion of thrombogenesis in diabetes, we examined the inhibitory effect of sarpogrelate, a 5-HT(2A) receptor antagonist, on thrombus formation in diabetic rats. In streptozotocin-induced diabetic rats, polyethylene tube-induced thrombus formation was enhanced compared with that in normal rats. The thrombogenesis was inhibited by sarpogrelate; cilostazol, a PDE3 inhibitor; and aspirin, a COX inhibitor, by 75.8%, 42.3%, and 34.3%, respectively. The inhibition by sarpogrelate was more pronounced in diabetic rats than normal ones. High glucose and 5-HT increased the expression of vascular cell adhesion molecule-1 (VCAM-1) in human umbilical vein endothelial cells (HUVECs) and combination of both high glucose and 5-HT further potentiated the effect. Sarpogrelate but not aspirin inhibited the increase in VCAM-1 expression induced by high glucose and 5-HT. These findings suggest that 5-HT mediates the enhanced thrombogenesis in diabetes and suggests that a 5-HT(2A) receptor antagonist may have novel therapeutic potential for the treatment of diabetic complications.
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Yamada et al. (2012) studied Diabetes mellitus (experimental thrombosis). Sarpogrelate vs. Vehicle was evaluated on Arterial occlusion ratio (p=<0.01). Sarpogrelate, a 5-HT2A receptor antagonist, significantly inhibited thrombus formation by 75.8% and reduced the arterial occlusion ratio from 100% to 40% in diabetic rats.
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