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].
Clemastine fumarate/富马酸氯马斯汀 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Microglial cells
20 ng/mL
1 hour
Clemastine inhibited the upregulation of IL-1β and NLRP3 in microglial cells induced by OGD.
J Neuroinflammation. 2020 Feb 15;17(1):57.
Plasmodium falciparum 3D7
10 µM
12-72 hours
To evaluate the inhibitory effect of clemastine on Plasmodium growth, results showed that 10 μM clemastine completely inhibited parasite loads in blood and liver cells.
Proc Natl Acad Sci U S A. 2020 Mar 17;117(11):5810-5817.
Huh-7 cells
20 µM
2 days
Screening for SARS-CoV-2 virus entry inhibitors, Clemastine showed the strongest anti-SARS2 activity (EC50=0.95 ± 0.83 µM).
Acta Pharmacol Sin. 2021 Aug;42(8):1347-1353.
Vero E6 cells
10 µM
24 hours
Validation of Clemastine's inhibitory effect on native SARS-CoV-2 virus, showing significant inhibition of viral replication.
Acta Pharmacol Sin. 2021 Aug;42(8):1347-1353.
Rat oligodendrocyte precursor cells
1 µM
3 days
To evaluate the effect of Clemastine on oligodendrocyte precursor cell differentiation and myelination. Results showed that Clemastine significantly enhanced oligodendrocyte differentiation and myelination.
Nat Med. 2014 Aug;20(8):954-960.
Oligodendrocyte precursor cells (OPCs)
1 µM
5 days
Promotes oligodendrocyte precursor cell maturation and central nervous system myelination
Clemastine reversed the inhibition of IL-1β on OPC maturation and promoted the expression of MBP and CNPase.
J Neuroinflammation. 2020 Feb 15;17(1):57.
Oligodendrocyte precursor cells co-cultured with dorsal root ganglion neurons
500 nM
To evaluate the effect of Clemastine on myelination in a co-culture system. Results showed that Clemastine significantly promoted myelination.
Nat Med. 2014 Aug;20(8):954-960.
Huh7 hepatocytes
10 µM
To evaluate the cytotoxicity of clemastine on human hepatocytes, results showed that 10 μM clemastine did not exhibit cytotoxicity.
Proc Natl Acad Sci U S A. 2020 Mar 17;117(11):5810-5817.
Clemastine fumarate/富马酸氯马斯汀 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Sprague-Dawley rats
Bilateral common carotid artery occlusion (BCCAO) model
Intraperitoneal injection
1 mg/kg
14 consecutive days
Clemastine improved hypomyelination in BCCAO rats and restrained the upregulation of IL-1β and NLRP3.
J Neuroinflammation. 2020 Feb 15;17(1):57.
Mice
Anks1b-deficient mouse models
Intraperitoneal injection
10 mg/kg
Daily for 14 days
Rescues deficits in social preference in Anks1b-deficient mice
Nat Commun. 2023 Dec 21;14(1):8499.
Mice
Pitt–Hopkins syndrome mouse model
Intraperitoneal injection
10 mg/kg
Once daily for 14 days
Clemastine treatment normalized oligodendrocyte precursor cell and oligodendrocyte density and increased the number of axons undergoing myelination.
Brain. 2023 Aug 1;146(8):3331-3346.
Mice
Murine neonatal hypoxic injury model
Oral gavage
10 mg/kg
Once daily from postnatal Days 3–10
Promotes oligodendrocyte precursor cell differentiation, myelination, and functional recovery
Brain. 2018 Jan 1;141(1):85-98
Mice
Experimental autoimmune encephalomyelitis (EAE)
Oral
10 mg/kg
Once daily for 28 days
To evaluate the remyelination efficacy of Clemastine in the EAE model, results showed that Clemastine improved VEP latency and increased the number of remyelinated axons in the optic nerve.
Brain. 2022 Nov 21;145(11):3943-3952
Mice
Fear memory model
Intraperitoneal injection
10 mg/kg
Once daily from 3 days pre-conditioning to 21 days post-conditioning
Promotes new myelin formation, improves remote memory recall and promotes fear generalization
Nat Neurosci. 2020 Apr;23(4):487-499
Mice
Cuprizone-mediated demyelination model
Gavage
10 mg/kg
Once daily for three weeks
Clemastine enhances oligodendrocyte gain during remyelination but is less effective than LL-341070, failing to fully eliminate the regeneration deficit after severe demyelination.
Nat Commun. 2025 Jan 16;16(1):732
C57BL/6J mice
Chronic microelectrode implantation model
Intraperitoneal injection
10 mg/kg
Daily administration for 16 weeks
Clemastine administration significantly elevated the signal detectability and quality, rescued the loss of multi-unit activity, and increased functional interlaminar connectivity over 16-weeks of implantation. Additionally, post-mortem immunohistochemistry showed that increased oligodendrocyte density and myelination coincided with increased survival of both excitatory and inhibitory neurons near the implant.
Biomaterials. 2023 Oct;301:122210
Rat
Neonatal hypoxic-ischemic brain injury model
Intraperitoneal injection
10 mg/kg
Once daily for 6 consecutive days
Clemastine promotes oligodendrocyte proliferation through the MAPK/ERK pathway, reduces white matter injury, and exhibits neuroprotective effects.
Int J Mol Sci. 2024 Jul 27;25(15):8204
Mice
Chronic hypoxia model
Oral gavage
10 mg/kg per day
Once daily from P3 to P10
Enhancing myelination and promoting functional recovery
Neuron. 2018 Aug 22;99(4):689-701.e5
C57BL/6 mice
Cuprizone-induced mouse model of demyelination
Oral
10 mg/kg per day
Daily for 3 weeks
Clemastine treatment greatly enhanced myelin repair in the demyelinated regions with increased mature oligodendrocytes (APC-positive) and myelin basic protein. More importantly, compared to vehicle, clemastine treatment rescued the schizophrenia-like behavioral changes in the open field test and the Y-maze, suggesting a beneficial effect via promoting myelin repair.
Neurosci Bull. 2015 Oct;31(5):617-25
Mice
Toxic injury model in spinal cord white matter tracts
Oral gavage
10 mg/kg/day
Once daily for 14 days
To evaluate the effect of Clemastine on remyelination. Results showed that Clemastine significantly accelerated the kinetics of remyelination and reduced the proportion of unmyelinated axons.
Nat Med. 2014 Aug;20(8):954-960.
Mice
C57BL/6 mice
Oral
10 mg/kg/day
Once daily for 4 months
Enhanced myelination and improved spatial memory in aged mice
Nat Neurosci. 2020 Apr;23(4):481-486
Mice
APP/PS1 transgenic mouse model
Oral
10 mg/kg/day
Daily for 3 months
Enhancing myelination to improve memory-related task performance and hippocampal sharp wave ripples in APP/PS1 mice
Neuron. 2021 Jul 21;109(14):2292-2307.e5
Plasmodium berghei ANKA
Liver-stage malaria model
10 μM
To evaluate the inhibitory effect of clemastine on liver-stage Plasmodium, results showed that 10 μM clemastine completely inhibited parasite loads in liver cells.
Proc Natl Acad Sci U S A. 2020 Mar 17;117(11):5810-5817.
Xenopus laevis tadpoles
Tg(mbp:GFP-NTR) transgenic model
Water solution administration
200 nM
3 days
To evaluate the effect of Clemastine on promoting remyelination, results showed that the number of GFP+ oligodendrocytes in the clemastine-treated group was 1.5-fold higher than the control group, and the visual avoidance index improved by 1.4-fold.
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 <<
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 <<
United States, California
... 展开 >>
Sandler Neurosciences Building, Neurological Clinical Research Unit
San Francisco, California, United States, 94107 收起 <<
United States, California
... 展开 >>
University of California San Francisco
Recruiting
San Francisco, California, United States, 94158
Contact: Tracy Tran, BA 415-353-2707 tracy.tran@ucsf.edu 收起 <<
搜索
