Clemastine fumarate is a selective histamine H1 Receptor antagonist with IC50 of 3 nM. Clemastine Fumarate inhibits histamine induced rise in [Ca2+]i in HL-60 cells with an IC50 of 3 nM. Clemastine Fumarate significantly potentiates ATP-induced increase in [Ca2+]i in HEKhP2X7 cells not relying on histamine receptor blockage but on sensitizing P2X7 receptor.
1. Thomas, J.S., et al. 1977. Ann Allergy. 38: 169-174. PMID: 320916 2. Dockhorn, R.J., et al. 1982. Mo Med. 79: 748-750. PMID: 7177096 3. Nair, M.P., et al. 1983. Cell. Immunol. 81: 45-60. PMID: 6225527
Soluble in water (5 mM), methanol, DMSO (35 mg/ml), ethanol (3 mg/ml), and alcohol (slightly).
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Ridley JM; et alRidley JM; et al. (PubMed ID: 16288909) determined that Clemastine fumarate is a potent inhibitor of Human ether- -go-go-related gene and has a high affinity for HERG channel pore cavity. -SCBT Publication Review
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