2-Cyclohexylcarbonylbenzimidazoles as potent, orally available and brain-penetrable opioid receptor-like 1 (ORL1) antagonists

We report identification of 2-cyclohexylcarbonylbenzimidazole 7c as potent, orally available and brain-penetrable ORL1 antagonist. Compound 7c showed satisfactory pharmacokinetic profiles and brain penetrability in laboratory animals, and good in vivo antagonism.