Flunarizine • 2HCl, a calcium channel protein inhibitor and antagonist, has been shown to inhibit contraction of isolated murine caudal artery preparations. Mechanistic studies suggest that this compound inhibits prostaglandin-induced and Serotonin • HCl (sc-201146) induced components of the contraction via reduction in the amounts of TXB2 (Thromboxane B2) (sc-201452) and ALK-1, and an increase in production of HETE. Experiments on rabbit sino-atrial nodes and isolated guinea-pig papillary muscles have reported that Flunarizine • 2HCl depressed the slow action potentials of K+-depolarized papillary muscle. Additionally, studies indicate that Flunarizine • 2HCl selectively suppresses Ca2+ influx through the cell membrane of sino-atrial nodes.
1. De Clerck, F., et al. 1983. Biochem. Pharmacol. 32: 765-771. PMID: 6404280 2. Kotake, H., et al. 1988. Res. Commun. Chem. Pathol. Pharmacol. 62: 147-160. PMID: 3251331 3. Takahashi, K., et al. 1991. J. Pharmacol. Exp. Ther. 256: 169-175. PMID: 1846413
Soluble in DMSO (25 mg/mL), ethanol (5 mg/mL warm), methanol, 0.1N HCI, and chloroform/methanol (9:1) (50 mg/mL). Insoluble in water, and dilute aqueous base..
Store at -20° C
Sodium channel protein type III alpha subunit: IC50 = 290 nM (rat); Sodium channel protein type V alpha subunit: IC50 = 350 nM (rat); Voltage-gated T-type calcium channel alpha-1H subunit: IC50 = 2200 nM (rat); Sodium channel protein type VIII alpha subunit : IC50 = 290 nM (rat); Voltage-gated T-type calcium channel alpha-1G subunit: IC50 = 2200 nM (rat)
Sodium channel protein type II alpha subunit: Ki= 53 nM (rat); Sodium channel protein type VIII alpha subunit: Ki= 53 nM (rat); Sodium channel protein type III alpha subunit: Ki= 53 nM (rat); Sodium channel protein type I alpha subunit: Ki= 53 nM (rat)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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Takahashi et alTakahashi et al. (PubMed ID 1846413) showed that Flunarizine 2HCl blocked T-type Ca++ channel in rat isolated hippocampal CA1 pyramidal neurons. -SCBT Publication Review
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