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5-HT4antagonist1是一个5-HT4受体拮抗剂,其pKi值为9.6。
5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6.
5-HT4 antagonist 1 (compound 6b) is a 5-HT4 receptor antagonist with a pKi of 9.6.
5-HT4 antagonist 1 (compound 6b) demonstrates good exposure and prolongs t1/2 in other species, including the mouse (t1/2 7 h), rat (t1/2 12 h) and mini-pig (t1/2 21 h). In Phase I clinical trial, it is found that 5-HT4 antagonist 1 has good oral bioavailability with a steady state plasma t1/2 of >100 h[1].
[1]. Clark RD, et al. Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1697-700.
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