Description
LEI 101 hydrochloride is potent and selective CB2 partial agonist.
in vitro
LEI-101 behaved as a partial agonist at CB2 receptors using β-arrestin and GTPγS assays and was ~100-fold selective in CB2 /CB1 receptor-binding assays._x000D_
_x000D_
Reference: Br J Pharmacol. 2016 Feb;173(3):446-58. https://pubmed.ncbi.nlm.nih.gov/21923175/
in vivo
Systematic modification of physicochemical properties, such as lipophilicity and basicity, was used to optimize the pharmacokinetic profile and hERG affinity of this novel class of cannabinoid CB2 receptor agonists. This led to the identification of 44 (LEI 101) as a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist (hCB2 pEC(50) = 8.0; hERG pK(i) < 4; F(po) = 100%), which was active in a rat spinal nerve ligation model of neuropathic pain._x000D_
_x000D_
Reference: J Med Chem. 2011 Oct 27;54(20):7350-62. https://pubmed.ncbi.nlm.nih.gov/21923175/
target
LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG.
