DA-6886 is a 5-Hydroxytryptamine receptor 4 (5-HT4) agonist. DA-6886 induces relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels reveals that it inhibits hERG channel current with an pIC50 value of 4.3, indicating that the compound is 1000-fold more selective for the 5-HT4 receptor over hERG channels. DA-6886 can be used in the study of constipated irritable bowel syndrome[1][2].
IC 50
5-HT4 Receptor: 4.3 (pIC50)
References
[1] Lee D Y, et al. Pharmacokinetics of DA-6886, a new 5-HT4 receptor agonist, in rats[J]. Pharmaceutics, 2022, 14(4): 702. DOI:10.3390/pharmaceutics14040702 [2] Lee M J, et al. Pharmacological profile of DA-6886, a novel 5-HT4 receptor agonist to accelerate colonic motor activity in mice[J]. European Journal of Pharmacology, 2014, 735: 115-122. DOI:10.1016/j.ejphar.2014.03.061
