AA sequence: Cys1-Lys-Gly-Lys-Gly-Ala-Lys-Cys8-Ser-Arg-Leu-Met-Tyr-Asp-Cys15-Cys16-Thr-Gly-Ser-Cys20-Arg-Ser-Gly-Lys-Cys25-NH2
Disulfide bonds: Cys1-Cys16, Cys8-Cys20 and Cys15-Cys25
Length (aa): 25
Formula: C102H172N36O32S7
Molecular Weight: 2639.18 Da
Appearance: White lyophilized solid
Solubility: water and saline buffer
CAS number: [107452-89-1]
Source: Synthetic
Purity rate: > 97 %
ω-Conotoxin-MVIIA
ω Conotoxin MVIIA, a potent blocker of Cav2.2
ω conotoxin MVIIA (omega conotoxin MVIIA) has been isolated from the venom of the cone Conus magus. Omega-conotoxins act at presynaptic membranes, they bind and block voltage-sensitive calcium channels (VSCC). ω conotoxin MVIIA blocks N-type voltage-gated calcium channels (Cav2.2/CACNA1B). ω conotoxin MVIIA is available as analgesic drug under the name Prialt®. It blocks acute pain in patients who no longer obtain relief from opiate drugs. It is 100 to 1.000 times more potent than morphine. This toxin blocks calcium channels and disables nerves that transmit pain signals.
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Ziconotide: neuronal calcium channel blocker for treating severe chronic pain
Ziconotide (PRIALT) is a neuroactive peptide in the final stages of clinical development as a novel non-opioid treatment for severe chronic pain. It is the synthetic equivalent of omega-MVIIA, a component of the venom of the marine snail, Conus magus. The mechanism of action underlying ziconotide’s therapeutic profile derives from its potent and selective blockade of neuronal N-type voltage-sensitive calcium channels (N-VSCCs). Direct blockade of N-VSCCs inhibits the activity of a subset of neurons, including pain-sensing primary nociceptors. This mechanism of action distinguishes ziconotide from all other analgesics, including opioid analgesics. In fact, ziconotide is potently anti-nociceptive in animal models of pain in which morphine exhibits poor anti-nociceptive activity. Moreover, in contrast to opiates, tolerance to ziconotide is not observed. Clinical studies of ziconotide in more than 2,000 patients reveal important correlations to ziconotide’s non-clinical pharmacology. For example, ziconotide provides significant pain relief to severe chronic pain sufferers who have failed to obtain relief from opiate therapy and no evidence of tolerance to ziconotide is seen in these patients. Contingent on regulatory approval, ziconotide will be the first in a new class of neurological drugs: the N-type calcium channel blockers, or NCCBs. Its novel mechanism of action as a non-opioid analgesic suggests ziconotide has the potential to play a valuable role in treatment regimens for severe chronic pain. If approved for clinical use, ziconotide will further validate the neuroactive venom peptides as a source of new and useful medicines.
Miljanich, G. P. (2004) Ziconotide: neuronal calcium channel blocker for treating severe chronic pain, Curr Med Chem. PMID: 15578997
Neuronal calcium channel antagonists. Discrimination between calcium channel subtypes using omega-conotoxin from Conus magus venom
The omega-conotoxins from the venom of fish-hunting cone snails are probably the most useful of presently available ligands for neuronal Ca channels from vertebrates. Two of these peptide toxins, omega-conotoxins MVIIA and MVIIB from the venom of Conus magus, were purified. The amino acid sequences show significant differences from omega-conotoxins from Conus geographus. Total synthesis of omega-conotoxin MVIIA was achieved, and biologically active radiolabeled toxin was produced by iodination. Although omega-conotoxins from C. geographus (GVIA) and C. magus (MVIIA) appear to compete for the same sites in mammalian brain, in amphibian brain the high-affinity binding of omega conotoxin MVIIA has narrower specificity. In this system, it is demonstrated that a combination of two omega-conotoxins can be used for biochemically defining receptor subtypes and suggested that these correspond to subtypes of neuronal Ca2+ channels.Olivera, B. M., et al. (1987) Neuronal calcium channel antagonists. Discrimination between calcium channel subtypes using omega-conotoxin from Conus magus venom, Biochemistry. PMID: 2441741