Chemistry:Leconotide
From HandWiki
Short description: Conotoxin peptide under investigation as an analgesic drug
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| Routes of administration | IV |
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| Formula | C107H179N35O36S7 |
| Molar mass | 2756.24 g·mol−1 |
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]
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
- ↑ 1.0 1.1 Pain Therapeutics: Current and Future Treatment Paradigms. Royal Society of Chemistry. 2013. pp. 225–. ISBN 978-1-84973-645-9. https://books.google.com/books?id=zUINAgAAQBAJ&pg=PA225.
- ↑ 2.0 2.1 Modulation of Presynaptic Calcium Channels. Springer Science & Business Media. 23 April 2013. pp. 326–. ISBN 978-94-007-6334-0. https://books.google.com/books?id=2bVEAAAAQBAJ&pg=PA326.
- ↑ Nervous System Diseases: Advances in Research and Treatment: 2011 Edition. ScholarlyEditions. 9 January 2012. pp. 217–. ISBN 978-1-4649-2221-3. https://books.google.com/books?id=RQTtLhbqJE4C&pg=PA217.
- ↑ "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. February 2010. doi:10.1111/j.1526-4637.2009.00741.x. PMID 20002322.
- ↑ "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. June 2011. doi:10.1111/j.1526-4637.2011.01118.x. PMID 21539704.
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