Blockade of serotonin 2A receptor improves glomerular endothelial function in rats with streptozotocin-induced diabetic nephropathy

Abstract

Our results indicate that sarpogrelate improves endothelial function in rats with STZ-induced diabetes through a reduction of glomerular platelet activation and an increase in serum adiponectin concentrations and suggest that sarpogrelate is potentially useful for the treatment of diabetic nephropathy.

Evaluation of the effectiveness of sarpogrelate on the surrogate markers for macrovascular complications in patients with type 2 diabetes

“…Sarpogrelate has been shown to be effective in the prevention of diabetic neuropathy and diabetic nephropathy. It is also known to be effective in the recovery of insulin resistance and in the prevention of neurogenic bladder caused by autonomic nervous system complications in type 2 diabetes patients [15][16][17][18][19][20][21]. Additionally, studies have shown that sarpogrelate is effective in preventing peripheral circulatory disturbances.…”

Microvesicles and diabetic complications — novel mediators, potential biomarkers and therapeutic targets

“…[124] . A few studies have indicated that the levels of monocyte-derived MVs [14,55] , endothelial-derived MVs [74] , and platelet-derived MVs [70,125,126] are increased in patients with diabetic nephropathy. The increase in monocyte-derived MVs is most significant in patients with diabetic nephropathy among the T2DM patients with diabetic microangiopathy, ie, nephropathy, retinopathy, or neuropathy [14] .…”

“…The circulating platelet-derived MVs [70,125,126] , monocyte-derived MVs [14,55] , endothelial-derived MVs [74] , and MVs derived from renal mesangial cells [82] may act as mediators and influence endothelial function by simulating the release of cytokines and the expression of various adhesion molecules by endothelial cells, inducing the morphological changes that lead to angiogenesis induction in microvascular endothelial cells.…”

“…Treatment with sarpogrelate, a serotonin (5-HT) 2A receptor antagonist, can reduce the level of albuminuria in streptozotocin-induced diabetic rats [125] . An experiment showed that sarpogrelate improves ROS/NO imbalance and suppresses platelet aggregation in glomeruli, which may be associated with reduced circulating platelet-derived MVs [125] .…”

“…An experiment showed that sarpogrelate improves ROS/NO imbalance and suppresses platelet aggregation in glomeruli, which may be associated with reduced circulating platelet-derived MVs [125] . Administration of angiotensin II receptor blockers can decrease circulating monocyte-derived MVs, chemokines (monocyte chemoattractant protein 1 and RANTES), and soluble adhesion markers (soluble P-selectin and sVCAM-1) [55] .…”