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Merck
CN

5.32383

Donecopride Fumarate

别名:

Donecopride Fumarate, 5-HT4R Agonist, AChE Inhibitor, MR31147, Serotonin receptor 5-HT4R agonist

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关于此项目

经验公式(希尔记法):
C22H33ClN2O2 · xC2H2O4 · yH2O
化学文摘社编号:
分子量:
392.96
UNSPSC Code:
12352200
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assay

≥95% (HPLC)

form

powder

potency

10.4 nM Ki

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

off-white

solubility

DMSO: 50 mg/mL

storage temp.

−20°C

Quality Level

Biochem/physiol Actions

Cell permeable: yes
Primary Target
5-HT4R
Secondary Target
AChE

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell permeable, brain penetrating piperidin-4-yl-propanone compound that that acts as a highly potent, selective and partial agonist of serotonin subtype 4 receptor ((h)5-HT4R; Ki = 10.4 nM and 48% efficacy compared to 5-HT control). Also acts as a potent, mixed type, competitive inhibitor of acetylcholinesterase (IC50 = 16 nM for human AChE) and offers selectivity over butyrylcholinesterase (IC50 = 3.5 µM). With respect to 5-HT2BR, it behaves like an inverse agonist (Ki = 1.6 nM). Promotes sAPPα secretion in COS-7 cells transiently expressing 5-HT4R (EC50 = 11.3 nM) and is shown to have a precognitive effect in murine model where it significantly improves discrimination index (6.3 vs -.0.22 in control mice; 0.3 mg/kg).
A cell permeable, highly potent, selective, and partial agonist of serotonin subtype 4 receptor (Ki= 10.4 nM). Also acts as a potent, mixed type, competitive inhibitor of AChE (IC₅₀ = 16 nM).

Other Notes

Lecoutey, C., et al. 2014. Proc. Natl. Acad. Sci. USA111, E3825.

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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Culture media provides a habitat with suitable nutrients, energy sources, and certain environmental conditions for the growth of microorganisms. The components of the culture media range from simple sugars to peptones, salts, antibiotics, and complex indicators.

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