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Leconotide

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Conotoxin peptide under investigation as an analgesic drug Pharmaceutical compound
Leconotide
Clinical data
Routes of
administration
IV
ATC code
  • None
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC107H179N35O36S7
Molar mass2756.24 g·mol

Leconotide (INN; development codes CNSB004 and AM336; also known as ω-conotoxin CVID) is an ω-conotoxin peptide isolated from the venom of Conus catus which is under investigation as an analgesic drug for the treatment of pain conditions.

It acts as an N-type voltage-gated calcium channel (Cav2.2) blocker and is highly selective for this channel over the related P/Q-type voltage-gated calcium channel (Cav2.1).

Relative to ziconotide, leconotide is advantageous in that it is significantly less toxic, and for that reason can be administered intravenously as opposed to via intrathecal injection.

See also

  • Ziconotide, an analgesic peptide derived from the toxin of the cone snail species Conus magus
  • Lacosamide, an approved small molecule analgesic and anti-epileptic
  • Ralfinamide, an investigational small molecule analgesic

References

  1. ^ Allerton C, Fox D (2013). Pain Therapeutics: Current and Future Treatment Paradigms. Royal Society of Chemistry. pp. 225–. ISBN 978-1-84973-645-9.
  2. ^ Stephens G, Mochida S (23 April 2013). Modulation of Presynaptic Calcium Channels. Springer Science & Business Media. pp. 326–. ISBN 978-94-007-6334-0.
  3. Nervous System Diseases: Advances in Research and Treatment: 2011 Edition. ScholarlyEditions. 9 January 2012. pp. 217–. ISBN 978-1-4649-2221-3.
  4. Kolosov A, Goodchild CS, Cooke I (February 2010). "CNSB004 (Leconotide) causes antihyperalgesia without side effects when given intravenously: a comparison with ziconotide in a rat model of diabetic neuropathic pain". Pain Medicine. 11 (2): 262–73. doi:10.1111/j.1526-4637.2009.00741.x. PMID 20002322.
  5. Kolosov A, Aurini L, Williams ED, Cooke I, Goodchild CS (June 2011). "Intravenous injection of leconotide, an omega conotoxin: synergistic antihyperalgesic effects with morphine in a rat model of bone cancer pain". Pain Medicine. 12 (6): 923–41. doi:10.1111/j.1526-4637.2011.01118.x. PMID 21539704.
Analgesics (N02A, N02B)
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Neuropathic pain and fibromyalgia pharmacotherapies
Monoaminergics
Ion channel blockers
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Ion channel modulators
Calcium
VDCCsTooltip Voltage-dependent calcium channels
Blockers
Activators
Potassium
VGKCsTooltip Voltage-gated potassium channels
Blockers
Activators
IRKsTooltip Inwardly rectifying potassium channel
Blockers
Activators
KCaTooltip Calcium-activated potassium channel
Blockers
Activators
K2PsTooltip Tandem pore domain potassium channel
Blockers
Activators
Sodium
VGSCsTooltip Voltage-gated sodium channels
Blockers
Activators
ENaCTooltip Epithelial sodium channel
Blockers
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ASICsTooltip Acid-sensing ion channel
Blockers
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CaCCsTooltip Calcium-activated chloride channel
Blockers
Activators
CFTRTooltip Cystic fibrosis transmembrane conductance regulator
Blockers
Activators
Unsorted
Blockers
Others
TRPsTooltip Transient receptor potential channels
LGICsTooltip Ligand gated ion channels
See also: Receptor/signaling modulatorsTransient receptor potential channel modulators


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