The 5-hydroxytryptamine2A receptor antagonist sarpogrelate hydrochloride inhibits acute platelet aggregation in injured endothelium.
In this study, the effect of sarpogrelate hydrochloride, a 5-hydroxytryptamine2A receptor antagonist, on platelet aggregation at the site of injured carotid artery endothelium was examined. The rat common carotid artery was clamped for 30 min to induce endothelial injury. Sarpogrelate hydrochloride was administered before and after the injury, and the effects were compared with those in rats receiving sham operation only and those receiving clipping injury but no sarpogrelate hydrochloride. The animals were killed 24 h after the procedure. The common carotid artery was examined by scanning electron microscopy and stained immunochemically for factor VIII. Sarpogrelate hydrochloride treatment was associated with reduced aggregation of platelets on electron microscopy and lower expression of factor VIII at the injured intima. Sarpogrelate hydrochloride has an inhibitory effect on platelet aggregation at the intima in the acute stage after injury, suggesting that this drug may be used to prevent early ischaemic complications after surgical or endovascular arterial intervention.
Houkin
K
K
Department of Neurosurgery, Sapporo Medical University School of Medicine, Sapporo, Japan. houkin@sapmed.ac.jp
Nakayama
N
N
Nonaka
T
T
Koyanagi
I
I
D000818:Animals; D017536:Carotid Artery, Common / Q000648:ultrastructure; D004334:Drug Administration Schedule; D004727:Endothelium / Q000293:injuries* / Q000648:ultrastructure; D005169:Factor VIII / Q000378:metabolism; D007150:Immunohistochemistry; D007274:Injections, Intraperitoneal; D008297:Male; D010975:Platelet Aggregation Inhibitors / Q000008:administration & dosage / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011985:Receptors, Serotonin / Q000378:metabolism*; D012701:Serotonin / Q000378:metabolism; D012702:Serotonin Antagonists / Q000008:administration & dosage / Q000494:pharmacology*; D013386:Succinates / Q000008:administration & dosage / Q000494:pharmacology*; D017539:Tunica Intima / Q000648:ultrastructure
D010975:Platelet Aggregation Inhibitors; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D013386:Succinates; C064294:sarpogrelate; D012701:Serotonin; D005169:Factor VIII