159081-22-8

YM-31636 free base is an orally active, potent and selective 5-HT3 receptor agonist with a Ki value of 0.2 nM. YM-31636 free base induces contraction of isolated guinea pig distal colon. YM-31636 free base induces tachycardia with the relative intrinsic activity of approximately 0.23 in isolated guinea pig right atrium. YM-31636 free base is promising for research of constipation[1][2].

5-HT₃ Receptor: 0.2 nM (Ki); 5-HT_1F Receptor: >10000 nM (Ki); 5-HT_2A Receptor: >10000 nM (Ki)

[1] Ito H, et al. Pharmacological profile of YM-31636, a novel 5-HT3 receptor agonist, in vitro. Eur J Pharmacol. 2000 Dec 8;409(2):195-201. DOI:10.1016/s0014-2999(00)00851-7
[2] Kiso T, et al. A novel 5-HT3 receptor agonist, YM-31636, increases gastrointestinal motility without increasing abdominal pain. Eur J Pharmacol. 2001 Nov 9;431(1):35-41. DOI:10.1016/s0014-2999(01)01425-x