KLS-13019 explained
KLS-13019 is a cannabidiol derivative that has been modified on the side chain to improve solubility and tissue penetration properties. It was developed and patented by Neuropathix subsidiary Kannalife and found to be 50x more potent than cannabidiol as a neuroprotective agent, thought to be mediated by modulation of the sodium-calcium exchanger channel. It also had a higher therapeutic index than cannabidiol.[1] [2] [3] Both KLS-13019 and cannabidiol, prevented the development of CIPN, while only KLS-13019 uniquely reversed neuropathic pain from chemotherapy. KLS-13019 binds to fewer biological targets than cannabidiol and KLS-13019 may possess the unique ability to reverse addictive behaviour, an effect not observed with cannabidiol.[4]
See also
Notes and References
- Kinney WA, McDonnell ME, Zhong HM, Liu C, Yang L, Ling W, Qian T, Chen Y, Cai Z, Petkanas D, Brenneman DE . 6 . Discovery of KLS-13019, a Cannabidiol-Derived Neuroprotective Agent, with Improved Potency, Safety, and Permeability . ACS Medicinal Chemistry Letters . 7 . 4 . 424–8 . April 2016 . 27096053 . 4834656 . 10.1021/acsmedchemlett.6b00009 .
- Brenneman DE, Petkanas D, Kinney WA . Pharmacological Comparisons Between Cannabidiol and KLS-13019 . Journal of Molecular Neuroscience . 66 . 1 . 121–134 . September 2018 . 30109468 . 6150782 . 10.1007/s12031-018-1154-7 .
- Brenneman DE, Kinney WA, Ward SJ . Knockdown siRNA Targeting the Mitochondrial Sodium-Calcium Exchanger-1 Inhibits the Protective Effects of Two Cannabinoids Against Acute Paclitaxel Toxicity . Journal of Molecular Neuroscience . 68 . 4 . 603–619 . August 2019 . 31077084 . 6615992 . 10.1007/s12031-019-01321-z .
- Foss JD, Farkas DJ, Huynh LM, Kinney WA, Brenneman DE, Ward SJ . Behavioral and pharmacological effects of cannabidiol (CBD) and the CBD analogue KLS‐13019 in mouse models of pain and reinforcement . British Journal of Pharmacology . April 2021 . 178 . 15 . 3067–3078 . 33822373 . 10.1111/bph.15486 . 233035597 . free .