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CIAC001 is a Pyruvate Kinase PKM2 inhibitor with anti-neuroinflammatory activity. CIAC001 inhibits LPS-induced proinflammatory nitric oxide (NO) production and protects immunologically active BV-2 cells (IC50=2.5 μM). CIAC001 also has anti-neuroinflammation in mouse models and inhibits chronic morphine-induced addiction[1]. | [in vivo]
CIAC001 (20 μg/kg, and 0.2 mg/kg, i.p, once daily for 7 days) dose-dependently attenuates Naloxone (HY-137279, opioid receptor antagonist) precipitated withdrawal jumps and significantly inhibits the development of morphine-induced behavioral sensitization during the induction period, in morphine-dependent mice[1].
CIAC001 (20 mg/kg, i.p, once daily for 7 days)has no apparent potential for memory decline or cognitive impairment in mice Y maze test[1]. | [References]
[1] Jin S, et al. Cannabidiol Analogue CIAC001 for the Treatment of Morphine-Induced Addiction by Targeting PKM2. J Med Chem. 2023 Aug 24;66(16):11498-11516. DOI:10.1021/acs.jmedchem.3c01029 |
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