SB 714786 is a potent and selective antagonist of the 5-hydroxytryptamine 1D (5-HT1D) receptor. Engineered from a series of dual 5-HT1 receptor selective reuptake inhibitors, it represents the first highly potent compound targeting specifically the 5-HT1D subtype. With pKi values of 6.5, 6.7, 9.1, and 6.5 for 5-HT1A, 5-HT1B, 5-HT1D, and SerT receptors, respectively, SB 714786 exhibits remarkable selectivity for the 5-HT1D receptor while showing minimal intrinsic activity against other receptor subtypes. This specificity makes it a valuable pharmacological tool for investigating the role of 5-HT1D receptors in various biological contexts and potential therapeutic applications.
SB 714786 is a potent and selective antagonist of the 5-hydroxytryptamine 1D (5-HT1D) receptor. Engineered from a series of dual 5-HT1 receptor selective reuptake inhibitors, it represents the first highly potent compound targeting specifically the 5-HT1D subtype. With pKi values of 6.5, 6.7, 9.1, and 6.5 for 5-HT1A, 5-HT1B, 5-HT1D, and SerT receptors, respectively, SB 714786 exhibits remarkable selectivity for the 5-HT1D receptor while showing minimal intrinsic activity against other receptor subtypes. This specificity makes it a valuable pharmacological tool for investigating the role of 5-HT1D receptors in various biological contexts and potential therapeutic applications.
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