Výsledky vyhledávání - "Tamio Sugawara"

Synthesis and Evaluation of in Vivo Anti-hypothermic Effect of the N- and C-Terminus Modified Thyrotropin-Releasing Hormone Mimetic: [(4S,5S)-(5-Methyl-2-oxooxazolidine-4-yl)carbonyl]-[3-(thiazol-4-yl)-L-alanyl]-L-prolinamide

Autor: Norihito Sato, Tamio Sugawara, Tsuyoshi Kihara, Katsumi Koike, Takayoshi Yoshikawa, Naotake Kobayashi, Katsuji Sugita, Yukio Tada

Publikováno v: Chemical and Pharmaceutical Bulletin. 69:314-324

We explored orally effective thyrotropin-releasing hormone (TRH) mimetics, which show high central nervous system effects in structure-activity relationship studies based on in vivo antagonistic activity on reserpine-induced hypothermia (anti-hypothe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fa00aa382cc9f9171b9a5d969fdab8ef
https://doi.org/10.1248/cpb.c20-00454

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Autor: Naotake, Kobayashi, Norihito, Sato, Katsuji, Sugita, Tsuyoshi, Kihara, Katsumi, Koike, Tamio, Sugawara, Yukio, Tada, Takayoshi, Yoshikawa

Publikováno v: Chemicalpharmaceutical bulletin. 69(4)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::27807454b6f03b797a0764f4082b89f8
https://pubmed.ncbi.nlm.nih.gov/33790077

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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)

Autor: Takayoshi Yoshikawa, Katsumi Koike, Yuko Fujimura, Tsuyoshi Kihara, Yukio Tada, Kouji Takahashi, Hiroshi Nakai, Katsuji Sugita, Tamio Sugawara, Norihito Sato, Naotake Kobayashi

Publikováno v: ACS Omega, Vol 3, Iss 10, Pp 13647-13666 (2018)
ACS Omega

We have explored orally effective thyrotropin-releasing hormone (TRH) mimetics, showing oral bioavailability and brain penetration by structure–activity relationship (SAR) study on the basis of in vivo antagonistic activity on reserpine-induced hyp

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e4628309af1aa444d7a8e91e47d82887
https://doaj.org/article/d165d037b7464779bcf5a8df0d389a63

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Synthesis and evaluation of in vivo anti‐hypothermic effect of all stereoisomers of the thyrotropin‐releasing hormone mimetic: Rovatirelin Hydrate

Autor: Yukio Tada, Norihito Sato, Takayoshi Yoshikawa, Naotake Kobayashi, Kouji Takahashi, Katsuji Sugita, Tamio Sugawara

Publikováno v: Journal of Peptide Science. 25

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 sys

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e8ec4791eb1f7aff9b6651dd5455c36
https://doi.org/10.1002/psc.3228

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Conjugation with L-Glutamate forin vivoBrain Drug Delivery

Autor: Teruna J. Siahaan, Fumiaki Hirose, Valentino J. Stella, Toshiyuki Sakaeda, Touko Ryu, Takayoshi Yoshikawa, Kenneth L. Audus, Koichiro Hirano, Yukio Tada, Lidia Kupczyk-Subotkowska, Tamio Sugawara

Publikováno v: Journal of Drug Targeting. 9:23-37

In vitro studies have shown that conjugation of a model compound [p-di(hydroxyethyl)-amino-D-phenylalanine (D-MOD)] with L-Glu can improve D-MOD permeation through the bovine brain microvessel endothelial cell monolayers (Sakaeda et al., 2000). The t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf7ff70e93264a38fc020f3e23a9b65f
https://doi.org/10.3109/10611860108995630

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A novel chemical delivery system for brain targeting

Autor: Koichiro Hirano, Toshiyuki Sakaeda, Takayoshi Yoshikawa, Valentino J. Stella, Tamio Sugawara

Publikováno v: Advanced Drug Delivery Reviews. 36:255-275

Two different chemical approaches for brain drug delivery and targeting are proposed in the present review. One is a chemical drug delivery using a ring-closure reaction to the hydrophilic quaternary thiazolium compound in the brain. The other is a c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::196ad78c0a8ff85cdf28815dfd7458f4
https://doi.org/10.1016/s0169-409x(98)00091-x

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