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Rovatirelin ameliorates motor dysfunction in the cytosine arabinoside-induced rat model of spinocerebellar degeneration via acetylcholine and dopamine neurotransmission.
Ijiro T, Yaguchi A, Yokoyama A, Kiguchi S. Ijiro T, et al. Clin Exp Pharmacol Physiol. 2022 Sep;49(9):950-958. doi: 10.1111/1440-1681.13675. Epub 2022 Jun 17. Clin Exp Pharmacol Physiol. 2022. PMID: 35637550
Furthermore, rovatirelin caused a significant increase in locomotor activity in a dose-dependent manner. ...Furthermore, the effects of rovatirelin were more potent than those of taltirelin....
Furthermore, rovatirelin caused a significant increase in locomotor activity in a dose-dependent manner. ...Furthermore, the effects …
Ameliorating effect of rovatirelin on the ataxia in rolling mouse Nagoya.
Ijiro T, Yaguchi A, Yokoyama A, Abe Y, Kiguchi S. Ijiro T, et al. Eur J Pharmacol. 2020 Sep 5;882:173271. doi: 10.1016/j.ejphar.2020.173271. Epub 2020 Jun 11. Eur J Pharmacol. 2020. PMID: 32534077
Rovatirelin is a newly synthetized thyrotropin-releasing hormone (TRH) analog. ...Furthermore, rovatirelin increased cerebellar mRNA level of brain derived neurotrophic factor. ...
Rovatirelin is a newly synthetized thyrotropin-releasing hormone (TRH) analog. ...Furthermore, rovatirelin increased cerebella …
Non-clinical pharmacokinetic profiles of rovatirelin, an orally available thyrotropin-releasing hormone analogue.
Kobayashi K, Abe Y, Harada H, Oota E, Endo T, Takeda H. Kobayashi K, et al. Xenobiotica. 2019 Jan;49(1):106-119. doi: 10.1080/00498254.2017.1423130. Epub 2018 Jan 31. Xenobiotica. 2019. PMID: 29300135
The permeability of rovatirelin from blood to brain (permeability-surface area) ranged from 1.04 0.14 to 1.29 0.28 muL/min/g in rats, and rovatirelin was stable in rat plasma and brain homogenates. 3. The metabolite pattern was qualitatively similar in vitro and in …
The permeability of rovatirelin from blood to brain (permeability-surface area) ranged from 1.04 0.14 to 1.29 0.28 muL/min/g in rats, …
Effect of rovatirelin in patients with cerebellar ataxia: two randomised double-blind placebo-controlled phase 3 trials.
Nishizawa M, Onodera O, Hirakawa A, Shimizu Y, Yamada M; Rovatirelin Study Group. Nishizawa M, et al. J Neurol Neurosurg Psychiatry. 2020 Mar;91(3):254-262. doi: 10.1136/jnnp-2019-322168. Epub 2020 Jan 14. J Neurol Neurosurg Psychiatry. 2020. PMID: 31937586 Free PMC article. Clinical Trial.
RESULTS: From October 2013 to May 2014, KPS1301 enrolled 411 patients; 374 were randomised to rovatirelin 1.6 mg (n=125), rovatirelin 2.4 mg (n=126) or placebo (n=123). From November 2016 to August 2017, KPS1305 enrolled 241 patients; 203 were randomised to rovat …
RESULTS: From October 2013 to May 2014, KPS1301 enrolled 411 patients; 374 were randomised to rovatirelin 1.6 mg (n=125), rovatire …
Effect of rovatirelin, a novel thyrotropin-releasing hormone analog, on the central noradrenergic system.
Ijiro T, Nakamura K, Ogata M, Inada H, Kiguchi S, Maruyama K, Nabekura J, Kobayashi M, Ishibashi H. Ijiro T, et al. Eur J Pharmacol. 2015 Aug 15;761:413-22. doi: 10.1016/j.ejphar.2015.05.047. Epub 2015 Jul 2. Eur J Pharmacol. 2015. PMID: 26142830
Furthermore, rovatirelin increased locomotor activity. The increase in NA level and locomotor activity by rovatirelin was more potent and longer acting than those by taltirelin. ...Thus, rovatirelin may have an orally effective therapeutic potential in patien …
Furthermore, rovatirelin increased locomotor activity. The increase in NA level and locomotor activity by rovatirelin was more …
Human mass balance, pharmacokinetics and metabolism of rovatirelin and identification of its metabolic enzymes in vitro.
Kobayshi K, Abe Y, Kawai A, Furihata T, Harada H, Endo T, Takeda H. Kobayshi K, et al. Xenobiotica. 2019 Dec;49(12):1434-1446. doi: 10.1080/00498254.2019.1580796. Epub 2019 Mar 5. Xenobiotica. 2019. PMID: 30747023 Clinical Trial.
The mass balance, pharmacokinetics and metabolism of rovatirelin were characterised in healthy male subjects after a single oral dose of [(14)C]rovatirelin. [(14)C]Rovatirelin was steadily absorbed, and the peak concentrations of radioactivity and rovatire …
The mass balance, pharmacokinetics and metabolism of rovatirelin were characterised in healthy male subjects after a single oral dose …
Pharmacokinetic Drug Interactions of an Orally Available TRH Analog (Rovatirelin) With a CYP3A4/5 and P-Glycoprotein Inhibitor (Itraconazole).
Kobayashi K, Abe Y, Kawai A, Furihata T, Endo T, Takeda H. Kobayashi K, et al. J Clin Pharmacol. 2020 Oct;60(10):1314-1323. doi: 10.1002/jcph.1628. Epub 2020 May 27. J Clin Pharmacol. 2020. PMID: 32459872
Concentrations of rovatirelin and (thiazolylalanyl)methylpyrrolidine (TAMP), the major metabolite of rovatirelin formed by cytochrome P450 (CYP) 3A4/5, were determined in plasma and urine. ...In vitro studies showed that rovatirelin is a substrate for P-gp bu …
Concentrations of rovatirelin and (thiazolylalanyl)methylpyrrolidine (TAMP), the major metabolite of rovatirelin formed by cyt …
Discovery of the Orally Effective Thyrotropin-Releasing Hormone Mimetic: 1-{N-[(4S,5S)-(5-Methyl-2-oxooxazolidine-4-yl)carbonyl]-3-(thiazol-4-yl)-l-alanyl}-(2R)-2-methylpyrrolidine Trihydrate (Rovatirelin Hydrate).
Kobayashi N, Sato N, Fujimura Y, Kihara T, Sugita K, Takahashi K, Koike K, Sugawara T, Tada Y, Nakai H, Yoshikawa T. Kobayashi N, et al. ACS Omega. 2018 Oct 31;3(10):13647-13666. doi: 10.1021/acsomega.8b01481. Epub 2018 Oct 19. ACS Omega. 2018. PMID: 30411045 Free PMC article.
Further SAR optimization studies of this lead compound led to discovery of a novel orally effective TRH mimetic: 1-{N-[(4S,5S)-(5-methyl-2-oxooxazolidine-4-yl)carbonyl]-3-(thiazol-4-yl)-l-alanyl}-(2R)-2-methylpyrrolidine trihydrate (rovatirelin hydrate), which was selected …
Further SAR optimization studies of this lead compound led to discovery of a novel orally effective TRH mimetic: 1-{N-[(4S,5S)-(5-methyl-2-o …
Synthesis and evaluation of in vivo anti-hypothermic effect of all stereoisomers of the thyrotropin-releasing hormone mimetic: Rovatirelin Hydrate.
Kobayashi N, Sato N, Sugita K, Takahashi K, Sugawara T, Tada Y, Yoshikawa T. Kobayashi N, et al. J Pept Sci. 2019 Dec;25(12):e3228. doi: 10.1002/psc.3228. Epub 2019 Nov 12. J Pept Sci. 2019. PMID: 31713944
We discovered the orally active thyrotropin-releasing hormone (TRH) mimetic: (4S,5S)-5-methyl-N-{(2S)-1-[(2R)-2-methylpyrrolidin-1-yl]-1-oxo-3-(1,3-thiazol-4-yl)propan-2-yl}-2-oxo-1,3-oxazolidine-4-carboxamide 1 (rovatirelin). The central nervous system (CNS) effect of …
We discovered the orally active thyrotropin-releasing hormone (TRH) mimetic: (4S,5S)-5-methyl-N-{(2S)-1-[(2R)-2-methylpyrrolidin-1-yl]-1-oxo …
Correction to Discovery of the Orally Effective Thyrotropin-Releasing Hormone Mimetic: 1-{N-[(4S,5S)-(5-Methyl-2-oxooxazolidine-4-yl)carbonyl]-3-(thiazol-4-yl)-l-alanyl}-(2R)-2-methylpyrrolidine Trihydrate (Rovatirelin Hydrate).
Kobayashi N, Sato N, Fujimura Y, Kihara T, Sugita K, Takahashi K, Koike K, Sugawara T, Tada Y, Nakai H, Yoshikawa T. Kobayashi N, et al. ACS Omega. 2019 Apr 17;4(4):6977-6978. doi: 10.1021/acsomega.9b00827. eCollection 2019 Apr 30. ACS Omega. 2019. PMID: 31459810 Free PMC article.