tcsc0018166 5-HT4 antagonist 1

5-HT4 antagonist 1 is a 5-HT₄ receptor antagonist with a pK_i of 9.6.

IC50 & Target: pKI: 9.6 (5-HT₄ receptor)^[1]

In Vitro: 5-HT4 antagonist 1 (compound 6b) is a 5-HT₄ receptor antagonist with a pK_i of 9.6.

In Vivo: 5-HT4 antagonist 1 (compound 6b) demonstrates good exposure and prolongs t_1/2 in other species, including the mouse (t_1/2 7 h), rat (t_1/2 12 h) and mini-pig (t_1/2 21 h). In Phase I clinical trial, it is found that 5-HT4 antagonist 1 has good oral bioavailability with a steady state plasma t_1/2 of >100 h^[1].