Clemastine fumarate

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Chemical Structure| 14976-57-9 同义名 : HS-592 fumarate; Meclastine fumarate; Clemastine (fumarate)
CAS号 : 14976-57-9
货号 : A157173
分子式 : C25H30ClNO5
纯度 : 98%
分子量 : 459.96
MDL号 : MFCD00137486
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 15 mg/mL(32.61 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • H1 receptor

    Histamine H1 receptor, IC50:3 nM
描述 Clemastine Fumarate is a first-generation histamine receptor H1 (HRH1) antagonist. As a safe and efficient anti-allergic agent, clemastine could impressively alleviate stress-related depressive-like phenotype in mice[3]. Clemastine fumarate can stimulate differentiation of oligodendrocyte precursor cells in vitro, in animal models, and in human cells[4]. Clemastine fumarate (CLE) can protect against myocardial ischemia-reperfusion injury (MIRI) through regulation of toll like receptor 4 (TLR4)[5]. Clemastine, failed to prevent migraine or headache after pituitary adenylate cyclase activating peptide-38 infusion, thus making a role for histamine release or mast cell degranulation in pituitary adenylate cyclase activating peptide-38-induced migraine less likely[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01154361 Angioedema Phase 2 Completed - Germany ... 展开 >> Klinikum rechts der Isar Hals-Nasen-Ohrenklinik der TUM Munich, Bavaria, Germany, 81675 收起 <<
NCT00481676 - Completed - -
NCT01125761 Dermatitis Phase 3 Withdrawn - Brazil ... 展开 >> LAL Clinica Pesquisa e Desenvolvimento Ltda Valinhos, São Paulo, Brazil, 13276-245 LAL Clínica Pesquisa e Desenvolvimento Ltda Valinhos, São Paulo, Brazil, 13276-245 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.87mL

2.17mL

1.09mL

21.74mL

4.35mL

2.17mL
参考文献

[1]Abbasi MM, Valizadeh H, et al.Inhibitory effect of clemastine on P-glycoprotein expression and function: an in vitro and in situ study. Iran J Basic Med Sci. 2016 Apr;19(4):423-9.

[2]Li Z, He Y, et al. Clemastine rescues behavioral changes and enhances remyelination in the cuprizone mouse model of demyelination. Neurosci Bull. 2015 Oct;31(5):617-25.

[3]Su WJ, Zhang T, Jiang CL, Wang W. Clemastine Alleviates Depressive-Like Behavior Through Reversing the Imbalance of Microglia-Related Pro-inflammatory State in Mouse Hippocampus. Front Cell Neurosci. 2018 Nov 13;12:412

[4]Green AJ, Gelfand JM, Cree BA, Bevan C, Boscardin WJ, Mei F, Inman J, Arnow S, Devereux M, Abounasr A, Nobuta H, Zhu A, Friessen M, Gerona R, von Büdingen HC, Henry RG, Hauser SL, Chan JR. Clemastine fumarate as a remyelinating therapy for multiple sclerosis (ReBUILD): a randomised, controlled, double-blind, crossover trial. Lancet. 2017 Dec 2;390(10111):2481-2489

[5]Yuan X, Juan Z, Zhang R, Sun X, Yan R, Yue F, Huang Y, Yu J, Xia X. Clemastine Fumarate Protects Against Myocardial Ischemia Reperfusion Injury by Activating the TLR4/PI3K/Akt Signaling Pathway. Front Pharmacol. 2020 Feb 10;11:28

[6]Vollesen LH, Guo S, Andersen MR, Ashina M. Effect of the H1-antihistamine clemastine on PACAP38 induced migraine. Cephalalgia. 2019 Apr;39(5):597-607