Relenopride (YKP10811) hydrochloride 是一种特异性和选择性的 5-HT₄ 受体激动剂 (K_i=4.96 nM)。与5-HT₄相比，Relenopride hydrochloride 对 5-HT_2A (K_i=600 nM)和5-HT_2B (K_i=31 nM) 受体的亲和力分别低 120 倍和 6 倍。Relenopride hydrochloride 增加胃肠运动。

Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT 4 receptor agonist (K i =4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT 2A (K i =600 nM) and 5-HT 2B receptors (K i =31 nM) than for 5-HT 4 . Relenopride hydrochloride increases gastrointestinal (GI) motility.

Solid

5-HT4 Receptor 4.96 nM (Ki) 5-HT2A Receptor

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

[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.

In Vitro: DMSO : 110 mg/mL (207.77 mM; Need ultrasonic)H₂O : 50 mg/mL (94.44 mM; Need ultrasonic)配制储备液