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]
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| Routes of administration | IV |
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| Formula | C107H179N35O36S7 |
| Molar mass | 2756.24 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
edit- 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
edit- ^ a b Allerton C, Fox D (2013). Pain Therapeutics: Current and Future Treatment Paradigms. Royal Society of Chemistry. pp. 225–. ISBN 978-1-84973-645-9.
- ^ a b Stephens G, Mochida S (23 April 2013). Modulation of Presynaptic Calcium Channels. Springer Science & Business Media. pp. 326–. ISBN 978-94-007-6334-0.
- ^ Nervous System Diseases: Advances in Research and Treatment: 2011 Edition. ScholarlyEditions. 9 January 2012. pp. 217–. ISBN 978-1-4649-2221-3.
- ^ 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.
- ^ 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.
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