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Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist.
Satoh A, Nagatomi Y, Hirata Y, Ito S, Suzuki G, Kimura T, Maehara S, Hikichi H, Satow A, Hata M, Ohta H, Kawamoto H. Satoh A, et al. Among authors: kawamoto h. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5464-8. doi: 10.1016/j.bmcl.2009.07.097. Epub 2009 Jul 23. Bioorg Med Chem Lett. 2009. PMID: 19674894
Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide (FTIDC).
Suzuki G, Kimura T, Satow A, Kaneko N, Fukuda J, Hikichi H, Sakai N, Maehara S, Kawagoe-Takaki H, Hata M, Azuma T, Ito S, Kawamoto H, Ohta H. Suzuki G, et al. Among authors: kawamoto h. J Pharmacol Exp Ther. 2007 Jun;321(3):1144-53. doi: 10.1124/jpet.106.116574. Epub 2007 Mar 14. J Pharmacol Exp Ther. 2007. PMID: 17360958
Novel ORL1-selective antagonists with oral bioavailability and brain penetrability.
Okamoto O, Kobayashi K, Kawamoto H, Ito S, Yoshizumi T, Yamamoto I, Hashimoto M, Shimizu A, Takahashi H, Ishii Y, Ozaki S, Ohta H. Okamoto O, et al. Among authors: kawamoto h. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3282-5. doi: 10.1016/j.bmcl.2008.04.037. Epub 2008 Apr 28. Bioorg Med Chem Lett. 2008. PMID: 18448337
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. Among authors: kawamoto h. 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
Pharmacological effects of the metabotropic glutamate receptor 1 antagonist compared with those of the metabotropic glutamate receptor 5 antagonist and metabotropic glutamate receptor 2/3 agonist in rodents: detailed investigations with a selective allosteric metabotropic glutamate receptor 1 antagonist, FTIDC [4-[1-(2-fluoropyridine-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide].
Satow A, Maehara S, Ise S, Hikichi H, Fukushima M, Suzuki G, Kimura T, Tanak T, Ito S, Kawamoto H, Ohta H. Satow A, et al. Among authors: kawamoto h. J Pharmacol Exp Ther. 2008 Aug;326(2):577-86. doi: 10.1124/jpet.108.138107. Epub 2008 May 16. J Pharmacol Exp Ther. 2008. PMID: 18487514
Unique antipsychotic activities of the selective metabotropic glutamate receptor 1 allosteric antagonist 2-cyclopropyl-5-[1-(2-fluoro-3-pyridinyl)-5-methyl-1H-1,2,3-triazol-4-yl]-2,3-dihydro-1H-isoindol-1-one.
Satow A, Suzuki G, Maehara S, Hikichi H, Murai T, Murai T, Kawagoe-Takaki H, Hata M, Ito S, Ozaki S, Kawamoto H, Ohta H. Satow A, et al. Among authors: kawamoto h. J Pharmacol Exp Ther. 2009 Jul;330(1):179-90. doi: 10.1124/jpet.109.151118. Epub 2009 Apr 9. J Pharmacol Exp Ther. 2009. PMID: 19359526
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: kawamoto h. J Med Chem. 2009 Jul 23;52(14):4091-4. doi: 10.1021/jm900581g. J Med Chem. 2009. PMID: 19537798
Correlation of receptor occupancy of metabotropic glutamate receptor subtype 1 (mGluR1) in mouse brain with in vivo activity of allosteric mGluR1 antagonists.
Suzuki G, Kawagoe-Takaki H, Inoue T, Kimura T, Hikichi H, Murai T, Satow A, Hata M, Maehara S, Ito S, Kawamoto H, Ozaki S, Ohta H. Suzuki G, et al. Among authors: kawamoto h. J Pharmacol Sci. 2009 Jul;110(3):315-25. doi: 10.1254/jphs.09011fp. Epub 2009 Jun 19. J Pharmacol Sci. 2009. PMID: 19542684 Free article.
Identification of a novel transmembrane domain involved in the negative modulation of mGluR1 using a newly discovered allosteric mGluR1 antagonist, 3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one.
Fukuda J, Suzuki G, Kimura T, Nagatomi Y, Ito S, Kawamoto H, Ozaki S, Ohta H. Fukuda J, et al. Among authors: kawamoto h. Neuropharmacology. 2009 Sep;57(4):438-45. doi: 10.1016/j.neuropharm.2009.06.017. Epub 2009 Jun 24. Neuropharmacology. 2009. PMID: 19559036
1,010 results