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Page 1
Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH2 (TAK-448), with Highly Potent Testosterone-Suppressive Activity and Excellent Water Solubility.
Nishizawa N, Takatsu Y, Kumano S, Kiba A, Ban J, Tsutsumi S, Matsui H, Matsumoto SI, Yamaguchi M, Ikeda Y, Kusaka M, Ohtaki T, Itoh F, Asami T. Nishizawa N, et al. Among authors: kusaka m. J Med Chem. 2016 Oct 13;59(19):8804-8811. doi: 10.1021/acs.jmedchem.6b00379. Epub 2016 Sep 21. J Med Chem. 2016. PMID: 27589480
Chronic administration of the metastin/kisspeptin analog KISS1-305 or the investigational agent TAK-448 suppresses hypothalamic pituitary gonadal function and depletes plasma testosterone in adult male rats.
Matsui H, Tanaka A, Yokoyama K, Takatsu Y, Ishikawa K, Asami T, Nishizawa N, Suzuki A, Kumano S, Terada M, Kusaka M, Kitada C, Ohtaki T. Matsui H, et al. Among authors: kusaka m. Endocrinology. 2012 Nov;153(11):5297-308. doi: 10.1210/en.2012-1388. Epub 2012 Oct 1. Endocrinology. 2012. PMID: 23027808
Pharmacologic profiles of investigational kisspeptin/metastin analogues, TAK-448 and TAK-683, in adult male rats in comparison to the GnRH analogue leuprolide.
Matsui H, Masaki T, Akinaga Y, Kiba A, Takatsu Y, Nakata D, Tanaka A, Ban J, Matsumoto S, Kumano S, Suzuki A, Ikeda Y, Yamaguchi M, Watanabe T, Ohtaki T, Kusaka M. Matsui H, et al. Among authors: kusaka m. Eur J Pharmacol. 2014 Jul 15;735:77-85. doi: 10.1016/j.ejphar.2014.03.058. Epub 2014 Apr 18. Eur J Pharmacol. 2014. PMID: 24747751
Physicochemically and pharmacokinetically stable nonapeptide KISS1 receptor agonists with highly potent testosterone-suppressive activity.
Asami T, Nishizawa N, Matsui H, Takatsu Y, Suzuki A, Kiba A, Terada M, Nishibori K, Nakayama M, Ban J, Matsumoto S, Tarui N, Ikeda Y, Yamaguchi M, Kusaka M, Ohtaki T, Kitada C. Asami T, et al. Among authors: kusaka m. J Med Chem. 2014 Jul 24;57(14):6105-15. doi: 10.1021/jm5005489. Epub 2014 Jul 7. J Med Chem. 2014. PMID: 24918545
Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor.
Miwa K, Hitaka T, Imada T, Sasaki S, Yoshimatsu M, Kusaka M, Tanaka A, Nakata D, Furuya S, Endo S, Hamamura K, Kitazaki T. Miwa K, et al. Among authors: kusaka m. J Med Chem. 2011 Jul 28;54(14):4998-5012. doi: 10.1021/jm200216q. Epub 2011 Jun 23. J Med Chem. 2011. PMID: 21657270
Differential effects of continuous exposure to the investigational metastin/kisspeptin analog TAK-683 on pulsatile and surge mode secretion of luteinizing hormone in ovariectomized goats.
Tanaka T, Ohkura S, Wakabayashi Y, Kuroiwa T, Nagai K, Endo N, Tanaka A, Matsui H, Kusaka M, Okamura H. Tanaka T, et al. Among authors: kusaka m. J Reprod Dev. 2013 Dec 17;59(6):563-8. doi: 10.1262/jrd.2013-060. Epub 2013 Sep 19. J Reprod Dev. 2013. PMID: 24047956 Free PMC article.
281 results