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209394-27-4

中文名稱 化合物 T32535
英文名稱 LADOSTIGIL
CAS 209394-27-4
分子式 C16H20N2O2
分子量 272.34
MOL 文件 209394-27-4.mol
209394-27-4 結(jié)構(gòu)式 209394-27-4 結(jié)構(gòu)式

基本信息

英文別名
LADOSTIGIL
Ladostigil (TV-3,326)
LHXOCOHMBFOVJS-OAHLLOKOSA-N
Carbamic acid, N-ethyl-N-methyl-, (3R)-2,3-dihydro-3-(2-propyn-1-ylamino)-1H-inden-5-yl ester

常見問題列表

生物活性
Ladostigil (TV-3326) 是膽堿酯酶 (cholinesterase) 和腦選擇性單胺氧化酶 (MAO) 的雙重抑制劑,抑制 MAO-B 和 AChE 的 IC50 值分別為 37.1 和 31.8 μM。Ladostigil 能夠增加膽堿能的傳遞,防止 ROS 的形成或其作用,可用于抑郁癥和阿爾茨海默氏病的研究。
靶點(diǎn)

MAO-B

37.1 μM (IC 50 )

AChE

31.8 μM (IC 50 )

體外研究

Ladostigil (1-10 μM) exerts neuroprotective activities, including a prevention of the fall of the mitochondrial membrane potential (ψ), attenuation of apoptotic cascades and an inhibition of ROS production induced by OS insults.
Ladostigil (1-10 μM) has a significant neuroprotective activity, including inhibition of caspase-3 activation, induction of Bcl-2 and reduction of Bad and Bax gene and protein expression in human neuroblastoma SK-N-SH cells.

體內(nèi)研究

Ladostigil (17 mg/kg; p.o. daily for 6 weeks) abolishes their hyperanxiety and depressive-like behaviour in the elevated plus maze (EPM) and forced swim tests (FST) tests in adulthood from puberty to prenatally-stressed rats.
Ladostigil (50 μmol/kg; single p.o.) restores the loss of episodic memory in the object recognition test in rats.

Animal Model: Pathogen-free (SPF) Sprague-Dawley rats
Dosage: 17 mg/kg
Administration: P.o. (added to the drinking water) daily for 6 weeks
Result: Inhibited brain MAO-A and B by more than 60%.
Reduced hyperanxiety of male and female prenatally stressed (PS) rats in the EPM and depressive-like behaviour in the FST.
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