Leconotide

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.[1][2]

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−1

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).[1][2]

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.[3][4][5]

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. Charlotte Allerton; David Fox (2013). Pain Therapeutics: Current and Future Treatment Paradigms. Royal Society of Chemistry. pp. 225–. ISBN 978-1-84973-645-9.
  2. Gary Stephens; Sumiko Mochida (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, Anton; Goodchild, Colin S.; Cooke, Ian (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): 262–273. doi:10.1111/j.1526-4637.2009.00741.x. ISSN 1526-2375. PMID 20002322.
  5. Kolosov, Anton; Aurini, Lucia; Williams, Elizabeth D.; Cooke, Ian; Goodchild, Colin S. (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): 923–941. doi:10.1111/j.1526-4637.2011.01118.x. ISSN 1526-2375. PMID 21539704.


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