| Bioactivity | Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2B receptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility[1][2]. |
| Invitro | Relenopride hydrochloride do not show any significant off-target binding to any other receptors, enzymes, orserotonin-receptor subtypes at 1 μM, except for binding to the 5-HT2A receptor and the 5-HT2B receptor. Relenopride hydrochloride shows antagonist activity at the 5-HT2B receptor with an IC50 of 2.1 μM and no significant activity at the 5-HT2A receptor up to 10 μM. Relenopride hydrochloride shows no activity against serotonin-receptor subtypes 5-HT1B, 5-HT1D, or 5-HT2A at 1 nM to 10 μM, or for serotonin-receptor subtype 5-HT7 at 10 nM to 30 μM[1]. |
| Name | Relenopride hydrochloride |
| CAS | 1221416-42-7 |
| Formula | C24H31Cl2FN4O4 |
| Molar Mass | 529.43 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) |
| Reference | [1]. Shin A, et al. A randomized trial of 5-hydroxytryptamine4-receptor agonist, YKP10811, on colonic transit and bowel function in functional constipation. Clin Gastroenterol Hepatol. 2015;13(4):701-8.e1. [2]. Yin J, et al. Prokinetic effects of a new 5-HT4 agonist, YKP10811, on gastric motility in dogs. J Gastroenterol Hepatol. 2017;32(3):625-630. [3]. Gilet M, et al. Influence of a new 5-HT4 receptor partial agonist, YKP10811, on visceral hypersensitivity in rats triggered by stress and inflammation. Neurogastroenterol Motil. 2014;26(12):1761-1770. |
Relenopride hydrochloride
CAS: 1221416-42-7 F: C24H31Cl2FN4O4 W: 529.43
Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydroc
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