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Optimization of benzimidazole series as opioid receptor-like 1 (ORL1) antagonists: SAR study directed toward improvement of selectivity over hERG activity.
Kobayashi K, Kato T, Yamamoto I, Shimizu A, Mizutani S, Asai M, Kawamoto H, Ito S, Yoshizumi T, Hirayama M, Ozaki S, Ohta H, Okamoto O. Kobayashi K, et al. Among authors: okamoto o. Bioorg Med Chem Lett. 2009 Jun 1;19(11):3100-3. doi: 10.1016/j.bmcl.2009.04.022. Epub 2009 Apr 11. Bioorg Med Chem Lett. 2009. PMID: 19398200
Identification of novel benzimidazole series of potent and selective ORL1 antagonists.
Okamoto O, Kobayashi K, Kawamoto H, Ito S, Satoh A, Kato T, Yamamoto I, Mizutani S, Hashimoto M, Shimizu A, Sakoh H, Nagatomi Y, Iwasawa Y, Takahashi H, Ishii Y, Ozaki S, Ohta H. Okamoto O, et al. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3278-81. doi: 10.1016/j.bmcl.2008.04.054. Epub 2008 Apr 25. Bioorg Med Chem Lett. 2008. PMID: 18468891
A novel class of cycloalkano[b]pyridines as potent and orally active opioid receptor-like 1 antagonists with minimal binding affinity to the hERG K+ channel.
Yoshizumi T, Takahashi H, Miyazoe H, Sugimoto Y, Tsujita T, Kato T, Ito H, Kawamoto H, Hirayama M, Ichikawa D, Azuma-Kanoh T, Ozaki S, Shibata Y, Tani T, Chiba M, Ishii Y, Okuda S, Tadano K, Fukuroda T, Okamoto O, Ohta H. Yoshizumi T, et al. Among authors: okamoto o. J Med Chem. 2008 Jul 10;51(13):4021-9. doi: 10.1021/jm701590h. Epub 2008 Jun 7. J Med Chem. 2008. PMID: 18537234
2-Cyclohexylcarbonylbenzimidazoles as potent, orally available and brain-penetrable opioid receptor-like 1 (ORL1) antagonists.
Kobayashi K, Uchiyama M, Takahashi H, Kawamoto H, Ito S, Yoshizumi T, Nakashima H, Kato T, Shimizu A, Yamamoto I, Asai M, Miyazoe H, Ohno A, Hirayama M, Ozaki S, Tani T, Ishii Y, Tanaka T, Mochidome T, Tadano K, Fukuroda T, Ohta H, Okamoto O. Kobayashi K, et al. Among authors: okamoto o. Bioorg Med Chem Lett. 2009 Jun 1;19(11):3096-9. doi: 10.1016/j.bmcl.2009.04.023. Epub 2009 Apr 11. Bioorg Med Chem Lett. 2009. PMID: 19394217
.; Ito, S.; Yoshizumi, T.; Hirayama, M.; Ozaki, S.; Ohta, H.; Okamoto, O. Bioorg. Med. Chem. Lett., in press] to the carbonyl linker effectively reduces susceptibility to P-glycoprotein (P-gp) efflux. ...
.; Ito, S.; Yoshizumi, T.; Hirayama, M.; Ozaki, S.; Ohta, H.; Okamoto, O. Bioorg. Med. Chem. Lett., in press] to the carbonyl …
Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists.
Kobayashi K, Uchiyama M, Ito H, Takahashi H, Yoshizumi T, Sakoh H, Nagatomi Y, Asai M, Miyazoe H, Tsujita T, Hirayama M, Ozaki S, Tani T, Ishii Y, Ohta H, Okamoto O. Kobayashi K, et al. Among authors: okamoto o. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3627-31. doi: 10.1016/j.bmcl.2009.04.116. Epub 2009 May 3. Bioorg Med Chem Lett. 2009. PMID: 19447610
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.
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. Satoh A, et al. Among authors: okamoto o. J Med Chem. 2009 Jul 23;52(14):4091-4. doi: 10.1021/jm900581g. J Med Chem. 2009. PMID: 19537798
195 results