ChemicalBook CAS DataBase List 866933-51-9

866933-51-9

Name	Velusetrag hydrochloride
CAS	866933-51-9
Molecular Formula	C25H37ClN4O5S
MDL Number	MFCD34469340
Molecular Weight	541.1
MOL File	866933-51-9.mol

Chemical Properties

storage temp.	4°C, away from moisture
solubility	DMSO : 220 mg/mL (406.58 mM; Need ultrasonic)
form	Solid
color	White to off-white

Hazard Information

Uses

Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag hydrochloride exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease[1][2][3][4][5].

in vivo

Velusetrag (3 mg/kg; a single i.p.) significantly improves the facilitation of contextual fear extinction in PD mice^[3].
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^[3].
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^[2].
Velusetrag (0.003-1 mg/kg; a single i.v.) dose-dependently increases inter-crystal distance, consistent with relaxation of the oesophagus in rats^[2].

Animal Model:	Male C57BL/6 mice (7-8 weeks old) were injected with MPTP^[3]
Dosage:	3 mg/kg
Administration:	A single i.p.
Result:	Improved facilitation of contextual fear extinction. Did not improve the impaired rotarod performance in PD mice.

IC 50

5-HT₄ Receptor: 7.7 (pKi)

storage

4°C, away from moisture

References

[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. DOI:10.1007/s00210-008-0282-y
[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. DOI:10.1007/s00210-008-0281-z
[3] Ishii T, et, al. Serotonin 5-HT 4 Receptor Agonists Improve Facilitation of Contextual Fear Extinction in an MPTP-Induced Mouse Model of Parkinson's Disease. Int J Mol Sci. 2019 Oct 26;20(21):5340. DOI:10.3390/ijms20215340
[4] Kuo B, et al. Velusetrag accelerates gastric emptying in subjects with gastroparesis: a multicentre, double-blind, randomised, placebo-controlled, phase 2 study. Aliment Pharmacol Ther. 2021;53(10):1090-1097. DOI:10.1111/apt.16344
[5] Goldberg M, et al. Clinical trial: the efficacy and tolerability of velusetrag, a selective 5-HT4 agonist with high intrinsic activity, in chronic idiopathic constipation - a 4-week, randomized, double-blind, placebo-controlled, dose-response study. Aliment Pharmacol Ther. 2010;32(9):1102-1112. DOI:10.1111/j.1365-2036.2010.04456.x

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