Cinnarizine D8

An internal standard for the quantification of cinnarizine

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1mg

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Background

Cinnarizine-d₈ is intended for use as an internal standard for the quantification of cinnarizine by GC- or LC-MS. Cinnarizine is a calcium channel inhibitor and histamine H₄ receptor antagonist (K_i = 142 nM).^1,2,3 It inhibits L- and T-type calcium channels in isolated guinea pig atrial cells in a voltage-dependent manner.¹ Cinnarizine inhibits L-type calcium currents in isolated guinea pig type II vestibular hair cells (IC₅₀ = 1.5 ?M). In vivo, cinnarizine (10 mg/kg) inhibits ethanol-induced gastric ulcer formation in rats.⁴ Formulations containing cinnarizine have been used in the treatment of nausea and vomiting due to vertigo, Meniere's disease, or chemotherapy.

1.Cohen, C.J., Spires, S., and Van Skiver, D.Block of T-type Ca channels in guinea pig atrial cells by antiarrhythmic agents and Ca channel antagonistsJ. Gen. Physiol.100(4)703-728(1992) 2.Arab, S.F., Düwel, P., Jüngling, E., et al.Inhibition of voltage-gated calcium currents in type II vestibular hair cells by cinnarizineNaunyn Schmiedebergs Arch. Pharmacol.369(6)570-575(2004) 3.Nguyen, T., Shapiro, D.A., George, S.R., et al.Discovery of a novel member of the histamine receptor familyMol. Pharmacol.59(3)427-433(2001) 4.Lozeva, V., Marazova, K., and Belcheva, A.Gastric histamine content and ulcer formation in rats with ethanol-induced injury. Effects of cinnarizine and flunarizineAgents Actions41 Spec NoC91-C92(1994)