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The aim of the present study was to examine the effects of sarpogrelate, a 5-HT2 antagonist, on 5-HT-induced endothelium-dependent relaxation in isolated porcine coronary artery preincubated with ketanserin (3 x 10(-6) M) and precontracted by U 46619 (5 x 10(-9) M) and compare its effects with other 5-HT2 antagonists such as ritanserin and cyproheptadine. The investigation showed that sarpogrelate (10(-7)-10(-5) M) had a weak antagonistic effect on 5-HT-induced relaxation and its effect was weaker than that of ritanserin (10(-9)-10(-7) M) and cyproheptadine (10(-8)-10(-6) M). The rank order of the antagonistic effects was: ritanserin &gt; cyproheptadine &gt; sarpogrelate. The study also showed that both sarpogrelate and ritanserin had no inhibitory effect on bradykinin-induced relaxation. In our previous study, we investigated the binding affinity of sarpogrelate, ritanserin and cyproheptadine to the 5-HT2A-receptor in rabbit cerebral cortex membranes and the pKi values found were 7.22, 8.98 and 7.54, respectively (M. Rashid et al., Jpn J Pharmacol 87, 189-194, 2001). Rank order of the calculated ratio of concentration of pA2 or pD'2 vs Ki was: sarpogrelate &gt; ritanserin &gt; cyproheptadine. Thus, these findings suggest that sarpogrelate has the lowest antagonistic effect on 5-HT-induced endothelium-dependent relaxation and the highest selectivity towards 5-HT2A receptor and might also be the safest drug with respect to its clinical implications in comparison with ritanserin and cyproheptadine.

Effects of Sarpogrelate, a Novel 5-HT2 Antagonist, on 5-HT-Induced Endothelium-Dependent Relaxations in Porcine Coronary Artery