2-Acylamino-4,6-diphenylpyridine derivatives as novel GPR54 antagonists with good brain exposure and in vivo efficacy for plasma LH level in male rats
- Author
- KOBAYASHI, Toshitake1 ; SASAKI, Satoshi1 ; BABA, Atsuo1 ; TOMITA, Naoki1 ; FUKUI, Seiji2 ; NAKAYAMA, Masaharu2 ; KIBA, Atsushi1 ; KUSAKA, Masami1 ; MATSUMOTO, Shin-Ichi2 ; YAMAGUCHI, Masashi2 ; ITOH, Fumio2
[1] Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd, 10 Wadai, Tsukuba-shi, Ibaraki 300-4293, Japan
[2] Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd, 17-85, Jusohonmachi 2-Chome, Yodogawa-ku, Osaka 532-8686, Japan - Source
Bioorganic & medicinal chemistry. 2010, Vol 18, Num 14, pp 5157-5171, 15 p
- ISSN
- 0968-0896
- Scientific domain
- Biochemistry, molecular biology, biophysics; Pharmacology drugs
- Publisher
- Elsevier, Amsterdam
- Publication country
- Netherlands
- Document type
- Article
- Language
- English
- Author keyword
- 2-Acylamino-4,6-diphenylpyridine GPR54 antagonist Kisspeptin Metastin
- Keyword (fr)
- Affinité Animal castré Animal Antagoniste Barrière hématoencéphalique Biodisponibilité Côlon Dérivé de la pipérazine Dérivé de la pyridine Dérivé du benzène Dérivé du furane Halogénophénols Hamster Homme Hormone adénohypophysaire Hétérocycle azote Hétérocycle oxygène In vitro In vivo LH Lignée CHO Lignée cellulaire Nitrile Ovaire Peptide Perméabilité cellulaire Pharmacocinétique Plasma sanguin Rat Relation structure activité Récepteur couplé protéine G Synthèse chimique Système nerveux central Voie intraveineuse 2-Furamide(N-[(3-cyano-6-[4-fluoro-2-hydroxyhényl]-4-[3-pipérazinophényl]-2-pyridyl)amino]) chlorhydrate Kisspeptine Lignée CACO2 Metastine Nicotinonitrile dérivé Fluor Composé organique Mammalia Rodentia Vertebrata
- Keyword (en)
- Affinity Castrated animal Animal Antagonist Blood brain barrier Bioavailability Colon Piperazine derivatives Pyridine derivatives Benzene derivatives Furan derivatives Halophenols Hamster Human Adenohypophyseal hormone Nitrogen heterocycle Oxygen heterocycle In vitro In vivo Luteinizing hormone CHO cell line Cell line Nitrile Ovary Peptides Cell permeability Pharmacokinetics Blood plasma Rat Structure activity relation G protein coupled receptor Chemical synthesis Central nervous system Intravenous administration Fluorine Organic compounds Mammalia Rodentia Vertebrata
- Keyword (es)
- Afinidad Animal castrado Animal Antagonista Barrera hematoencefálica Biodisponibilidad Colón Piperazina derivado Piridina derivado Benceno derivado Furano derivado Halofenoles Hamster Hombre Hormona adenohipofisaria Heterociclo nitrógeno Heterociclo oxígeno In vitro In vivo LH Célula CHO Línea celular Nitrilo Ovario Péptido Permeabilidad celular Farmacocinética Plasma sanguíneo Rata Relación estructura actividad Receptor acoplado proteína G Síntesis química Sistema nervioso central Vía intravenosa Fluor Compuesto orgánico Mammalia Rodentia Vertebrata
- Classification
- Pascal
- 002 Biological and medical sciences / 002B Medical sciences / 002B02 Pharmacology. Drug treatments / 002B02O Hormones. Endocrine system
- Discipline
- Pharmacological treatments
- Origin
- Inist-CNRS
- Database
- PASCAL
- INIST identifier
- 23054864
Sauf mention contraire ci-dessus, le contenu de cette notice bibliographique peut être utilisé dans le cadre d’une licence CC BY 4.0 Inist-CNRS / Unless otherwise stated above, the content of this bibliographic record may be used under a CC BY 4.0 licence by Inist-CNRS / A menos que se haya señalado antes, el contenido de este registro bibliográfico puede ser utilizado al amparo de una licencia CC BY 4.0 Inist-CNRS
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DOI
10.1016/j.bmc.2010.05.061 
https://dx.doi.org/10.1016/j.bmc.2010.05.061
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