261766-73-8

261766-73-8 structure

Name	5-HT4 antagonist 1
Synonyms	inhibit,5-HT4 antagonist 1,5-hydroxytryptamine Rector,Serotonin Rector,5-HT Rector,5 HT4 antagonist 1,5-HT-4 antagonist 1,Inhibitor,5HT4 antagonist 1 1,4-Benzodioxin-5-cboxamide, 2,3-dihydro-N-[[1-[3-[(4-methyl-1-piperazinyl)sulfonyl]propyl]-4-piperidinyl]methyl]

Description	5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Research Areas >> Neurological Disease
Target	pKI: 9.6 (5-HT4 receptor)[1]
In Vitro	5-HT4 antagonist 1 (compound 6b) is a 5-HT4 receptor antagonist with a pKi of 9.6.
In Vivo	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].
References	[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.