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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: tanaka a. 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: tanaka a. 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
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: tanaka a. 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.
Suppression of the hypothalamic-pituitary-gonadal axis by TAK-385 (relugolix), a novel, investigational, orally active, small molecule gonadotropin-releasing hormone (GnRH) antagonist: studies in human GnRH receptor knock-in mice.
Nakata D, Masaki T, Tanaka A, Yoshimatsu M, Akinaga Y, Asada M, Sasada R, Takeyama M, Miwa K, Watanabe T, Kusaka M. Nakata D, et al. Among authors: tanaka a. Eur J Pharmacol. 2014 Jan 15;723:167-74. doi: 10.1016/j.ejphar.2013.12.001. Epub 2013 Dec 11. Eur J Pharmacol. 2014. PMID: 24333551
An administration of TAK-683 at a minimally effective dose for luteinizing hormone stimulation under the absence of the ovary induces luteinizing hormone surge in ovary-intact goats.
Kanai N, Endo N, Ohkura S, Wakabayashi Y, Matsui H, Matsumoto H, Ishikawa K, Tanaka A, Watanabe T, Okamura H, Tanaka T. Kanai N, et al. Among authors: tanaka a, tanaka t. J Reprod Dev. 2017 Jun 21;63(3):305-310. doi: 10.1262/jrd.2016-184. Epub 2017 Mar 24. J Reprod Dev. 2017. PMID: 28344194 Free PMC article.
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: tanaka a. J Med Chem. 2011 Jul 28;54(14):4998-5012. doi: 10.1021/jm200216q. Epub 2011 Jun 23. J Med Chem. 2011. PMID: 21657270
6,209 results