Biochemical and Pharmacological Profile of a Potent and Selective Endothelin B-Receptor Antagonist, BQ-788

We describe the characteristics of a potent and selective endothelin (ET) B-receptor antagonist, BQ-788 [N-cis-2,6-dimethylpiperidinocarbonyl-L-γ-methylleucyl-D-1 -methoxycarbonyltryptophanyl-D-norleucine]. In vitro, this compound potently and competitively inhibits125I-labeled endothelin 1 (ET-1) b...

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Veröffentlicht in:	Proceedings of the National Academy of Sciences - PNAS 1994-05, Vol.91 (11), p.4892-4896
Hauptverfasser:	Ishikawa, Kiyofumi, Ihara, Masaki, Noguchi, Kazuhito, Mase, Toshiaki, Mino, Nobuyuki, Saeki, Toshihiko, Fukuroda, Takahiro, Fukami, Takehiro, Ozaki, Satoshi, Nagase, Toshio, Nishikibe, Masaru, Yano, Mitsuo
Format:	Artikel
Sprache:	eng
Schlagworte:	Agonists Amino Acid Sequence Animals Biochemistry Blood pressure Boluses Bronchoconstrictors Cell Line Cell lines Endothelin Receptor Antagonists Endothelins Guinea Pigs Humans Inhibitory concentration 50 Male Molecular Sequence Data Neurons Oligopeptides - metabolism Oligopeptides - pharmacology Pharmacology Piperidines - metabolism Piperidines - pharmacology Rabbits Rats Rats, Sprague-Dawley Receptor, Endothelin B Receptors Tumor Cells, Cultured Vehicles
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