584555-10-2

SB 714786 is a potent and selective 5-hydroxytryptamine 1D (5-HT1D) receptor antagonist. It was developed from the previously reported series of dual 5-HT1 selective 5-hydroxytryptamine reuptake inhibitors (5HT1-SSRIs). SB 714786 is the first reported highly potent and selective 5-HT1D receptor antagonist, providing an extremely useful pharmacological tool for further understanding the role of 5-HT1 receptor subtypes. It has no or very low intrinsic activity against all three receptors. SB 714786 has pKi values of 6.5, 6.7, 9.1 and 6.5 for 5-HT1A, 5-HT1B, 5-HT1D and SerT receptors, respectively, showing high selectivity for 5-HT1D receptors. These properties make SB 714786 a potential tool compound for studying the function of 5-HT1D receptors and the treatment of related diseases.

[1] Discovery of the First Potent, Selective 5-Hydroxytryptamine1D Receptor Antagonist