209394-27-4

中文名称化合物 T32535

英文名称 LADOSTIGIL

CAS 209394-27-4

分子式 C16H20N2O2

分子量 272.34

MOL 文件 209394-27-4.mol

209394-27-4 结构式

基本信息常见问题列表

基本信息

英文别名

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

常见问题列表

生物活性

Ladostigil (TV-3326) 是胆碱酯酶 (cholinesterase) 和脑选择性单胺氧化酶 (MAO) 的双重抑制剂，抑制 MAO-B 和 AChE 的 IC50 值分别为 37.1 和 31.8 μM。Ladostigil 能够增加胆碱能的传递，防止 ROS 的形成或其作用，可用于抑郁症和阿尔茨海默氏病的研究。

靶点

MAO-B

37.1 μM (IC ₅₀ )

AChE

31.8 μM (IC ₅₀ )

体外研究

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.

体内研究

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.