Ladostigil hydrochloride  (Synonyms: TV-3326 hydrochloride)

Ladostigil (TV-3326) hydrochloride is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC₅₀s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hydrochloride exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease^[1][2]. Ladostigil (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Ladostigil (1-10 µM) hydrochloride 具有神经保护活性，包括防止线粒体膜电位 (ψ) 下降，衰减凋亡级联和抑制 OS 损伤诱导的 ROS 产生^[2]。
Ladostigil (1-10 µM) hydrochloride 具有显著的神经保护活性，包括抑制 caspase-3 激活，诱导 Bcl-2，降低人成神经细胞瘤 SK-N-SH 细胞中 Bad 和 Bax 基因和蛋白的表达^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Ladostigil (17 mg/kg; p.o. daily for 6 weeks) hydrochloride 在从青春期到产前压力大鼠的成年期的高架十字迷宫 (EPM) 和强迫游泳测试 (FST) 测试中，消除了他们的高度焦虑和抑郁样行为^[4]。
Ladostigil (50 μmol/kg; single p.o.) hydrochloride 在大鼠物体识别测试中恢复丧失的情景记忆^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

308.80

C₁₆H₂₁ClN₂O₂

209394-18-3

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

• [1]. Denya I, et, al. Design, synthesis and evaluation of indole derivatives as multifunctional agents against Alzheimer's disease. Medchemcomm. 2018 Jan 16; 9(2):357-370.  [Content Brief]

  [2]. Weinreb O, et, al. Ladostigil: a novel multimodal neuroprotective drug with cholinesterase and brain-selective monoamine oxidase inhibitory activities for Alzheimer's disease treatment. Curr Drug Targets. 2012 Apr; 13(4): 483-94.  [Content Brief]

  [3]. Weinstock M, et, al. Ladostigil, a novel multifunctional drug for the treatment of dementia co-morbid with depression. J Neural Transm Suppl. 2006; (70):443-6.  [Content Brief]

  [4]. Poltyrev T, et, al. Effect of chronic treatment with ladostigil (TV-3326) on anxiogenic and depressive-like behaviour and on activity of the hypothalamic-pituitary-adrenal axis in male and female prenatally stressed rats. Psychopharmacology (Berl). 2005 Aug;181(1): 118-25.  [Content Brief]