Sabeluzole

Names

[ Name ]:
Sabeluzole

[Synonym ]:
(+/-)-4-(2-benzothiazolylmethylamino)-α-[(4-fluorophenoxy)methyl]-1-pipiridineethanol
sabeluzole
reminyl
galantamine
1-[4-(Benzothiazol-2-yl-methyl-amino)-piperidin-1-yl]-3-(4-fluoro-phenoxy)-propan-2-ol

Biological Activity

[Description]:

Sabeluzole (R 58735), a benzothiazol derivative, has antiischemic, antiepileptic, and cognitive-enhancing properties. Sabeluzole protects rat hippocampal neurons against NMDA- and glutamate-induced neurotoxicity via preventing tau expression. Sabeluzole enhances memory in rats, and prevents the amnesic effect of Chlordiazepoxide. Sabeluzole can be used fro research of Alzheimer's disease[1][2].

[Related Catalog]:

Research Areas >> Neurological Disease

[In Vitro]

Sabeluzole（50 nM、100 nM；细胞损伤前 20 分钟）在小脑颗粒细胞原代培养物中对谷氨酸 (50 μM) 介导的兴奋性毒性具有保护作用[1]。 Sabeluzole（50 nM；7 天）抑制谷氨酸诱导的 tau 蛋白水平增加[1]。 Sabeluzole（50 nM; 4 d）在人神经母细胞瘤细胞系 SH-SY5Y 中表现出神经保护作用[1]。

[In Vivo]

Sabeluzole（5 mg/kg，25 mg/kg；sc；两次给药，间隔 72 小时）在 20 mg/kg Chlordiazepoxide 诱导的习惯性遗忘症雄性大鼠中表现出阳性和记忆增强特性[2]。 Animal Model: Adult albino male rats (270-330 g) induced by Chlordiazepoxide[2] Dosage: 5 mg/kg, 25 mg/kg Administration: SC; 0.5 ml/kg; twice dose with 72 h interval; 1 h before 20 mg/kg Chlordiazepoxide Result: Showed the positive effects on several learning and memory tasks in rats. Did not influence locomotor and rearing activity of animals during the acquisition session.

[References]

[1]. Uberti D, et al. Priming of cultured neurons with sabeluzole results in long-lasting inhibition of neurotoxin-induced tau expression and cell death. Synapse. 1997 Jun;26(2):95-103.

[2]. Hlinák Z,et al. Sabeluzole improves social recognition and antagonizes chlordiazepoxide's effect on habituation in the rat. Psychopharmacology (Berl). 1991;104(4):505-9.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₆FN₃O₂S

[ Molecular Weight ]:
415.52

[ Exact Mass ]:
415.17300

[ PSA ]:
77.07000

[ LogP ]:
3.71380

Related Compounds

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