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ENVIRONMENTAL TOXICOLOGY TOOLS & SERVICESZiconotide is a synthetic version of ω-conopeptide MVIIA, a peptide toxin originally found in the venom of the fish-eating marine snail C. magus, that blocks N-type calcium channels in rat brain membranes (Kds = 1.1-18 pM; IC50s = 2-55 pM).1,2 It blocks high-voltage-activated calcium currents in rat superior cervical ganglion neurons (IC50 = 32 nM) as well as depolarization-induced norepinephrine release by rat peripheral sympathetic efferent neurons and in rat hippocampus (IC50s = 1.2 and 5.5 nM, respectively).1 Intrathecal administration of ziconotide inhibits formalin-induced flinch responses and increases the paw withdrawal threshold in the paw pressure test in rats (ED50s = 0.11 and 0.60 μg, respectively), indicating antinociceptive effects.3 It decreases latency to tail withdrawal in a hot plate test in a rat model of sciatic chronic constriction injury.1 Ziconotide also reduces infarct volume post ischemia in a rat model of transient focal ischemia.4
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1. Ziconotide: A review of its pharmacology and use in the treatment of pain. Neurophyschiatr. Dis. Treat. 3(1), 69-85 (2007).
2. Neuronal calcium channel antagonists. Discrimination between calcium channel subtypes using ω-
3. Interactions of intrathecally administered ziconotide, a selective blocker of neuronal N-
4. The omega-