Clemastine (HS-592) fumarate
For research use only.
Catalog No.S1847 Synonyms: Meclastine fumarate
CAS No. 14976-57-9
Clemastine Fumarate (HS-592, Meclastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
Selleck's Clemastine (HS-592) fumarate has been cited by 10 publications
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Detection of P2X7 receptor and histamine receptor H1 (HRH1) in hippocampus and mPFC. (A–F) CUMS treatment upregulated the protein expression of the purinergic receptor P2X, ligand-gated ion channel 7 (P2X7R) in both hippocampus and mPFC subregions. In the meantime, continuous intraperitoneal administration of clemastine protected mice from stress-induced upregulation of P2X7R in the hippocampus rather than mPFC. There is no statistical alteration of HRH1 expression in both subfields of hippocampus and mPFC, even when the mice were subjected to stress stimulation or clemastine injection (n = 4 for (A–F), *p < 0.05, **p < 0.01).
Front Cell Neurosci, 2018, 12:412. Clemastine (HS-592) fumarate purchased from Selleck.
(B,C) Analysis indicates the total distance was unchanged between cuprizone-exposed mice with or without clemastine treatment (B), but the distance in the central field decreased upon 6-week exposure to cuprizone, while clemastine gradually rescued the behavioral change (C). *P <0.05, n = 10 animals/group.
Neurosci Bull, 2015, 31(5):617-25. Clemastine (HS-592) fumarate purchased from Selleck.
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Choose Selective Histamine Receptor Inhibitors
|Description||Clemastine Fumarate (HS-592, Meclastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.|
Clemastine Fumarate inhibits histamine induced rise in [Ca2+]i in HL-60 cells with an IC50 of 3 nM as compared with that of chlorpheniramine or diphenhydramine with IC50 values of 20 nM and 100 nM, respectively.  At concentrations of ≥25 μM, Clemastine Fumarate significantly blocks NK and ADCC reactions of lymphocytes against the human erythroleukemia cell line K562 and human B-lymphoblast cell line SB, respectively.  Clemastine Fumarate inhibits histamine-induced contraction of guinea pig ileum with an IC50 of 231 nM.  Clemastine Fumarate potently inhibits the HERG K+ channel in a concentration-dependent manner in HEK 293 cells stably expressing HERG channels with an IC50 of 12 nM, which can be attenuated by the Y652A or F656A mutation of HERG.  Clemastine Fumarate significantly potentiates ATP-induced increase in [Ca2+]i in HEKhP2X7 cells not relying on histamine receptor blockage but on sensitizing P2X7 receptor in a concentration-dependent manner with an EC50 of 10 μM, and increases the IL-1β release from LPS-induced human macrophages. 
Administration of Clemastine Fumarate (5-20 mg/kg) displays significantly inhibitory effect on simultaneously induced zymosan paw oedema and croton oil ear oedema in rats in a dose-dependent manner, with the inhibition of 53.6% and 46.8%, respectively, at the dose of 20 mg/kg, and with ID50 values of 18.0 mg/kg and 20.5 mg/kg, respectively.  Clemastine Fumarate treatment strongly reduces innate immune responses to Listeria monocytogenes in mice by interfering with the extracellular signal-regulated kinase (ERK)-mediated production of proinflammatory cytokines such as TNF-α and IL-6 surprisingly not dependent on blocking the histamine H1 receptor, leading to significantly higher mortality. 
-  Seifert R, et al. Mol Pharmacol, 1992, 42(2), 227-234.
-  Nair MP, et al. Cell Immunol, 1983, 81(1), 45-60.
-  Merlos M, et al. J Pharmacol Exp Ther, 1997, 280(1), 114-121.
|In vitro||DMSO||35 mg/mL warmed (76.09 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02040298||Completed||Drug: Clemastine|Drug: Placebo||Multiple Sclerosis Relapsing-Remitting||University of California San Francisco||January 2014||Phase 2|
|NCT01239719||Unknown status||Drug: Dexamethasone + clemastine|Drug: Dexamethasone||Allergy|Dermatitis||Azidus Brasil||March 2011||Phase 3|
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