Novel ORL1-selective antagonists with oral bioavailability and brain penetrability.
Bioorganic & Medicinal Chemistry Letters（2008）
Abstract
A novel ORL1-selective antagonist with oral bioavailability and brain penetrability, 2-(tert-butylthio)-5-chloro-6-[(2R)-4-(2-hydroxyethyl)-2-methylpiperazin-1-yl]-1H-benzimidazole, was identified in a 5-chloro-6-[piperazin-1-yl]-1H-benzimidazole series.
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Key words
Nociceptin/orphanin FQ,Nociceptin receptor,Opioid receptor-like 1(ORL1) antagonist
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