Identification of novel selective P2Y<sub>6</sub> receptor antagonists by high-throughput screening assay.

Ito, Masaaki; Egashira, Shin-Ichiro; Yoshida, Kazuki; Mineno, Tomoko; Kumagai, Kazuo; Kojima, Hirotatsu; Okabe, Takayoshi; Nagano, Tetsuo; Ui, Michio; Matsuoka, Isao

Identification of novel selective P2Y₆ receptor antagonists by high-throughput screening assay.

Ito, Masaaki; Egashira, Shin-Ichiro; Yoshida, Kazuki; Mineno, Tomoko; Kumagai, Kazuo; Kojima, Hirotatsu; Okabe, Takayoshi; Nagano, Tetsuo; Ui, Michio; Matsuoka, Isao.

Afiliação

Ito M; Laboratory of Pharmacology, Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki-shi, Gunma 370-0033, Japan. Electronic address: mito@takasaki-u.ac.jp.
Egashira SI; Drug Discovery Initiative, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Yoshida K; Laboratory of Pharmacology, Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki-shi, Gunma 370-0033, Japan.
Mineno T; Laboratory of Medicinal Chemistry, Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki-shi, Gunma 370-0033, Japan.
Kumagai K; Drug Discovery Initiative, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Kojima H; Drug Discovery Initiative, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Okabe T; Drug Discovery Initiative, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Nagano T; Drug Discovery Initiative, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Ui M; Tokyo Metropolitan Institute of Medical Science, 2-1-6 Kamikitazawa, Setagaya-ku, 156-8506 Tokyo, Japan.
Matsuoka I; Laboratory of Pharmacology, Faculty of Pharmacy, Takasaki University of Health and Welfare, Takasaki-shi, Gunma 370-0033, Japan.

Life Sci ; 180: 137-142, 2017 Jul 01.

Article em En | MEDLINE | ID: mdl-28527783

Assuntos

Anti-Inflamatórios/farmacologia; Desenho de Fármacos; Ensaios de Triagem em Larga Escala/métodos; Antagonistas do Receptor Purinérgico P2Y/farmacologia; Receptores Purinérgicos P2/efeitos dos fármacos; Anti-Inflamatórios/administração & dosagem; Anti-Inflamatórios/química; Astrocitoma/metabolismo; Cálcio/metabolismo; Linhagem Celular Tumoral; Relação Dose-Resposta a Droga; Ensaio de Imunoadsorção Enzimática; Humanos; Concentração Inibidora 50; Interleucina-1beta/metabolismo; Interleucina-8/metabolismo; Antagonistas do Receptor Purinérgico P2Y/administração & dosagem; Antagonistas do Receptor Purinérgico P2Y/química; Receptores Purinérgicos P2/metabolismo; Fator de Necrose Tumoral alfa/metabolismo

Palavras-chave

Compound 1 (6-bromo-3-nitro-2-(trifluoromethyl)-2H-chromene, PubChem CID: 11681366); Compound 2 (2-(4-chlorophenyl)-3-nitro-2H-chromene, PubChem CID: 3774501); Compound 3 (2-(4-methoxyphenyl)-3-nitro-2H-chromene, PubChem CID: 2732134); Compound 4 (3-nitro-2-phenyl-2H-chromene, PubChem CID: 42450); High-throughput screening; Interleukin-8; P2Y(6) receptor antagonist; TIM-38 (3-nitro-2-(trifluoromethyl)-2H-chromene, PubChem CID: 16762479)

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Receptores Purinérgicos P2 / Ensaios de Triagem em Larga Escala / Antagonistas do Receptor Purinérgico P2Y / Anti-Inflamatórios Tipo de estudo: Diagnostic_studies / Prognostic_studies / Screening_studies Limite: Humans Idioma: En Revista: Life Sci Ano de publicação: 2017 Tipo de documento: Article

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