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KLS-13019 is a cannabidiol-derived small molecule neuroprotective agent developed to improve upon the potency, safety, and bioavailability of cannabidiol. It is structurally modified on the side chain to enhance solubility and tissue penetration. KLS-13019 acts primarily as an antagonist at G protein-coupled receptor 55 (GPR55) and modulates the mitochondrial sodium-calcium exchanger 1 (NCX1), conferring both neuroprotective and anti-inflammatory properties. Preclinical studies have demonstrated that it is significantly more potent and safer than cannabidiol, with improved oral bioavailability. Unlike cannabidiol, KLS-13019 has been shown to both prevent and reverse neuropathic pain in models of chemotherapy-induced peripheral neuropathy (CIPN), without binding to opioid receptors or presenting a risk for chemical dependency. The drug also shows potential for treating other neuroinflammatory conditions such as hepatic encephalopathy, traumatic brain injury, peripheral nerve injuries, inflammation-related disorders, and possibly Parkinson’s disease[1][2][3][4][5][6][7].
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