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  • Title: Identification of an orally active opioid receptor-like 1 (ORL1) receptor antagonist 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine as clinical candidate.
    Author: Satoh A, Sagara T, Sakoh H, Hashimoto M, Nakashima H, Kato T, Goto Y, Mizutani S, Azuma-Kanoh T, Tani T, Okuda S, Okamoto O, Ozaki S, Iwasawa Y, Ohta H, Kawamoto H.
    Journal: J Med Chem; 2009 Jul 23; 52(14):4091-4. PubMed ID: 19537798.
    Abstract:
    Our efforts to optimize prototype opioid receptor-like 1 (ORL1) antagonist 1 led to the discovery of 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine 10. 10 showed potent ORL1 antagonistic activity, excellent selectivity over other opioid receptors, and in vivo efficacy after oral dosing. Currently clinical trials of 10 are underway.
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