產(chǎn)品目錄

規(guī)格	1 mg 5 mg
CAS	N/A
別名	N/A
化學(xué)名	N/A
分子式	C22H33ClN2O2.C4H4O4 [XH2O]
分子量	509
溶解度	DMSO: 50 mg/ml
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Donecopride is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4E (Ki = 8.5 nM) and an inhibitor of acetylcholinesterase (AChE; IC50 = 16 nM).1 It is selective for AChE over butyrylcholinesterase (BChE; IC50 = 3,530 nM) but does bind to 5-HT2B and sigma-2 (σ2) receptors (Ki = 1.6 nM for both) in a panel of 42 neurotransmitter receptors and transporters. Donecopride induces release of soluble amyloid precursor protein-α (sAPP-α) in COS-7 cells transiently expressing 5-HT4 with an EC50 value of 11.3 nM. Oral administration of donecopride (1 mg/kg) reduces brain soluble and insoluble amyloid-β (1-42) levels and increases the time spent exploring the novel object in the novel object recognition (NOR) test in the 5XFAD transgenic mouse model of Alzheimer's disease. Donecopride (3 mg/kg, p.o.) prevents a reduction in spontaneous alternation behavior induced by intracerebroventricular administration of soluble Aβ42 (sAβ42) in the Y-maze in mice.2

1.Lecoutey, C., Hedou, D., Freret, T., et al.Design of donecopride, a dual serotonin subtype 4 receptor agonist/acetylcholinesterase inhibitor with potential interest for Alzheimer's disease treatmentProc. Natl. Acad. Sci. USA111(36)E3825-E3830(2014) 2.Rochais, C., Lecoutey, C., Hamidouche, K., et al.Donecopride, a Swiss army knife with potential against Alzheimer's diseaseBr. J. Pharmacol.177(9)1988-2005(2020)

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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