leconotide

{{short description|Conotoxin peptide under investigation as an analgesic drug}}

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| CAS_number = 247207-64-3

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| PubChem = 16132255

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| ChemSpiderID = 17288914

| UNII = 2P1P5JB93S

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| C=107 | H=179 | N=35 | O=36 | S=7

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| routes_of_administration = IV

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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.{{cite book| vauthors = Allerton C, Fox D |title=Pain Therapeutics: Current and Future Treatment Paradigms|url=https://books.google.com/books?id=zUINAgAAQBAJ&pg=PA225|year=2013|publisher=Royal Society of Chemistry|isbn=978-1-84973-645-9|pages=225–}}{{cite book| vauthors = Stephens G, Mochida S|title=Modulation of Presynaptic Calcium Channels|url=https://books.google.com/books?id=2bVEAAAAQBAJ&pg=PA326|date=23 April 2013|publisher=Springer Science & Business Media|isbn=978-94-007-6334-0|pages=326–}}

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.{{cite book|title=Nervous System Diseases: Advances in Research and Treatment: 2011 Edition|url=https://books.google.com/books?id=RQTtLhbqJE4C&pg=PA217|date=9 January 2012|publisher=ScholarlyEditions|isbn=978-1-4649-2221-3|pages=217–}}{{cite journal | vauthors = Kolosov A, Goodchild CS, Cooke I | title = CNSB004 (Leconotide) causes antihyperalgesia without side effects when given intravenously: a comparison with ziconotide in a rat model of diabetic neuropathic pain | journal = Pain Medicine | volume = 11 | issue = 2 | pages = 262–73 | date = February 2010 | pmid = 20002322 | doi = 10.1111/j.1526-4637.2009.00741.x | doi-access = free }}{{cite journal | vauthors = Kolosov A, Aurini L, Williams ED, Cooke I, Goodchild CS | title = Intravenous injection of leconotide, an omega conotoxin: synergistic antihyperalgesic effects with morphine in a rat model of bone cancer pain | journal = Pain Medicine | volume = 12 | issue = 6 | pages = 923–41 | date = June 2011 | pmid = 21539704 | doi = 10.1111/j.1526-4637.2011.01118.x | doi-access = free }}

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

{{Reflist|2}}

{{Analgesics}}

{{Neuropathic pain pharmacotherapies}}

{{Channelergics}}

Category:Analgesics

Category:Calcium channel blockers

Category:Peptides

{{analgesic-stub}}