Velusetrag (TD-5108) hydrochloride 是一种具有口服活性，有效和选择性的血清素 5-HT₄ 受体 (5-HT₄R) 激动剂，pK_i 为 7.7。Velusetrag hydrochloride 对 5-HT_2A 和 5-HT_2B 受体没有亲和力 (K_i>10 μM)。Velusetrag hydrochloride 可用于胃肠道疾病和帕金森病的研究。

Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin 5-HT 4 receptor (5-HT 4 R), with a pK i of 7.7. Velusetrag hydrochloride exhibits no affinity (K i >10 μM) for 5-HT 2A and 5-HT 2B receptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinsons disease.

Solid

5-HT4 Receptor 7.7 (pKi)

Velusetrag (10 pM-100 μM) concentration-dependently increases the cAMP in HEK-293 cells stably transfected with the h5-HT4(c) receptor, with a pEC50 of 8.3.
Velusetrag (100 pM-1 μM) produces concentration-dependent contraction of the guinea pig colonic longitudinal muscle/myenteric plexus (LMMP), with a pEC50 of 7.9.
TD-5108 (0.001-10 μM) produces a concentration-dependent relaxation of the carbachol (3 μM)-precontracted rat esophagus, with a pEC50 of 7.9. has not independently confirmed the accuracy of these methods. They are for reference only.

Velusetrag (3 mg/kg; a single i.p.) significantly improves the facilitation of contextual fear extinction in PD mice.
Velusetrag (3 mg/kg; a single i.p.) increase hippocampal cAMP levels in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated mice.
Velusetrag (0.003-3 mg/kg; a single s.c.) increases colonic transit in a dose-dependent manner and reduces the time taken for excretion of the dye in guinea pigs.
Velusetrag (0.003-1 mg/kg; a single i.v.) dose-dependently increases inter-crystal distance, consistent with relaxation of the oesophagus in rats. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Smith JAM, et, al. The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):125-37.
[2]. Beattie DT, et, al. The in vivo gastrointestinal activity of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):139-47.

In Vitro: DMSO : 220 mg/mL (406.58 mM; Need ultrasonic)H₂O : 10 mg/mL (18.48 mM; ultrasonic and warming and heat to 60°C)配制储备液