SB-203186 is a highly selective antagonist of the 5-HT4 receptor. It demonstrates a potent competitive antagonistic effect, as evidenced by its pKB value of 8.3 in the isolated right atrium model of piglets. The compound effectively shifts the serotonin-induced tachycardia curve to the right in a dose-dependent manner without inhibiting the maximum response. While SB-203186 shows significant antagonistic activity in pig and human atria, it does not exhibit substantial effects in rat atria, making it valuable for investigating conditions such as arrhythmias and abnormal myocardial contraction.
SB-203186 is a highly selective antagonist of the 5-HT4 receptor. It demonstrates a potent competitive antagonistic effect, as evidenced by its pKB value of 8.3 in the isolated right atrium model of piglets. The compound effectively shifts the serotonin-induced tachycardia curve to the right in a dose-dependent manner without inhibiting the maximum response. While SB-203186 shows significant antagonistic activity in pig and human atria, it does not exhibit substantial effects in rat atria, making it valuable for investigating conditions such as arrhythmias and abnormal myocardial contraction.
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