| Identification | Back Directory | [Name]
1,2-Dihydro-N-[(3-endo)-8-[(2R)-2-hydroxy-3-[methyl(methylsulfonyl)amino]propyl]-8-azabicyclo[3.2.1]oct-3-yl]-1-(1-methylethyl)-2-oxo-3-quinolinecarboxamide | [CAS]
866933-46-2 | [Synonyms]
TD 5108
Velusetrag
HXLOHDZQBKCUCR-WOZUAGRISA-N
1,2-Dihydro-N-[(3-endo)-8-[(2R)-2-hydroxy-3-[methyl(methylsulfonyl)amino]propyl]-8-azabicyclo[3.2.1]oct-3-yl]-1-(1-methylethyl)-2-oxo-3-quinolinecarboxamide
3-QuinolinecarboxaMide, 1,2-dihydro-N-[(3-endo)-8-[(2R)-2-hydroxy-3-[Methyl(Methylsulfonyl)aMino]propyl]-8-azabicyclo[3.2.1]oct-3-yl]-1-(1-Methylethyl)-2-oxo- | [Molecular Formula]
C25H36N4O5S | [MDL Number]
MFCD16621124 | [MOL File]
866933-46-2.mol | [Molecular Weight]
504.64 |
| Chemical Properties | Back Directory | [density ]
1.34 | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (198.16 mM; Need ultrasonic) | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag 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.) increases 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]
Store at -20°C | [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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