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Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel non-basic 1-(2H-indazole-5-yl)pyridin-2(1H)-one derivatives and mitigation of mutagenicity in Ames test.
Igawa H, Takahashi M, Ikoma M, Kaku H, Kakegawa K, Kina A, Aida J, Okuda S, Kawata Y, Noguchi T, Hotta N, Yamamoto S, Nakayama M, Nagisa Y, Kasai S, Maekawa T. Igawa H, et al. Among authors: okuda s. Bioorg Med Chem. 2016 Jun 1;24(11):2504-2518. doi: 10.1016/j.bmc.2016.04.013. Epub 2016 Apr 7. Bioorg Med Chem. 2016. PMID: 27117261
Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel 1-(1H-benzimidazol-6-yl)pyridin-2(1H)-one derivatives and design to avoid CYP3A4 time-dependent inhibition.
Igawa H, Takahashi M, Shirasaki M, Kakegawa K, Kina A, Ikoma M, Aida J, Yasuma T, Okuda S, Kawata Y, Noguchi T, Yamamoto S, Fujioka Y, Kundu M, Khamrai U, Nakayama M, Nagisa Y, Kasai S, Maekawa T. Igawa H, et al. Among authors: okuda s. Bioorg Med Chem. 2016 Jun 1;24(11):2486-2503. doi: 10.1016/j.bmc.2016.04.011. Epub 2016 Apr 6. Bioorg Med Chem. 2016. PMID: 27112449
A novel and selective melanin-concentrating hormone receptor 1 antagonist ameliorates obesity and hepatic steatosis in diet-induced obese rodent models.
Kawata Y, Okuda S, Hotta N, Igawa H, Takahashi M, Ikoma M, Kasai S, Ando A, Satomi Y, Nishida M, Nakayama M, Yamamoto S, Nagisa Y, Takekawa S. Kawata Y, et al. Among authors: okuda s. Eur J Pharmacol. 2017 Feb 5;796:45-53. doi: 10.1016/j.ejphar.2016.12.018. Epub 2016 Dec 13. Eur J Pharmacol. 2017. PMID: 27986627
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: okuda s. J Med Chem. 2008 Jul 10;51(13):4021-9. doi: 10.1021/jm701590h. Epub 2008 Jun 7. J Med Chem. 2008. PMID: 18537234
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: okuda s. J Med Chem. 2009 Jul 23;52(14):4091-4. doi: 10.1021/jm900581g. J Med Chem. 2009. PMID: 19537798
Effects of a novel metabotropic glutamate receptor 7 negative allosteric modulator, 6-(4-methoxyphenyl)-5-methyl-3-pyridin-4-ylisoxazonolo[4,5-c]pyridin-4(5H)-one (MMPIP), on the central nervous system in rodents.
Hikichi H, Murai T, Okuda S, Maehara S, Satow A, Ise S, Nishino M, Suzuki G, Takehana H, Hata M, Ohta H. Hikichi H, et al. Among authors: okuda s. Eur J Pharmacol. 2010 Aug 10;639(1-3):106-14. doi: 10.1016/j.ejphar.2009.08.047. Epub 2010 Apr 2. Eur J Pharmacol. 2010. PMID: 20371227
1,280 results