[125I]BQ3020, a novel endothelin agonist selective for the endothelinB receptor subtype

Brain Research Protocols - Tập 1 - Trang 23-26 - 1997
Amy A Assal1, George Gessner1, Michael F Jarvis1
1Rhône-Poulenc Rorer Central Research, Collegeville, PA 19426, USA

Tài liệu tham khảo

Abramson, S.N., McGonigle, P. and Molinoff, P.B., Evaluation of models for analysis of radioligand binding sites, Mol. Pharmacol., 31 (1987) 103–111. Arai, H., Hori, S., Aramoi, I., Ohkubo, H. and Nakanishi, S., Cloning and expression of a cDNA encoding an endothelin receptor, Nature, 348 (1990) 730–732. Bradford, M.M., A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding, Anal. Biochem., 72 (1976) 248–254. Cheng, Y. and Prusoff, W.H., Relationship between the inhibition constant (Ki) and the concentration of an inhibitor that causes a 50% inhibition (I50) of an enzymatic reaction, Biochem. Pharmacol., 22 (1973) 3099–3108. De Lean, A., Hancock, A.A. and Lefkowitz, R.J., Validation and statistical analysis of a computer modeling method for quantitative analysis of radioligand binding data for mixtures of pharmacological receptor subtypes, Mol. Pharmacol., 21 (1989) 5–16. Haynes, W.G., Davenport, A.P. and Webb, D.J., Endothelin: progress in pharmacology and physiology, Trends Pharmacol. Sci., 14 (1993) 225–228. Ihara, M., Saeki, T., Fukuroda, T., Kimura, S., Ozaki, S., Patel, A. and Yano, M., A novel radioligand [125I]BQ-3020 selective for endothelin (ETB) receptors, Life Sci., 51 (1992) PL47–PL52. Inoue, A., Yanagisawa, M., Kimura, S., Kasuya, Y., Miyauchi, T., Goto, K. and Masaki, T., The human endothelin family: three structurally and pharmacologically distinct isopeptides predicted by three separate genes, Proc. Natl. Acad. Sci. USA, 86 (1989) 2863–2867. Jarvis, M.F., Assal, A.A. and Gessner, G., Pharmacological characterization of the rat cerebellar endothelinB (ETB) receptor using the novel agonist radioligand [125I]BQ3020, Brain Res., 665 (1994) 33–38. Kobayashi, M., Ihara, M., Sato, N., Saeki, T., Ozaki, S., Ikemoto, F. and Yano, M., A novel ligand, [125I]BQ-3020, reveals the localization of endothelin ETB receptors, Eur. J. Pharmacol., 235 (1993) 95–100. Masaki, T., Yanagisawa, M. and Goto, K., Physiology and pharmacology of endothelins, Med. Res. Rev., 12 (1992) 391–421. Molenaar, P., Kuc, R.E. and Davenport, A.P., Characterization of two new ETB selective radioligands, [125I]BQ3020 and [125I][Ala1,3,11,15]ET-1 in human heart, Br. J. Pharmacol., 107 (1992) 637–639. Sakurai, T., Yanagisawa, M. and Masaki, T., Molecular characterization of endothelin receptors, Trends Pharmacol. Sci., 13 (1992) 103–108. Sakamoto, A., Yanagisawa, M., Sakurai, T., Takuwa, Y., Yanagisawa, H. and Masaki, T., Cloning and functional expression of human cDNA for the ETB endothelin receptor, Biochem. Biophys. Res. Commun., 178 (1991) 656–663. Williams, M. and Jarvis, M.F., Biochemical approaches to drug discovery and characterization. In C.R. Clark and W.H. Moos (Eds.), Modern Drug Discovery Technologies, VCH/Ellis, Horwood, 1989, pp. 129–166. Yanagisawa, M., Kurihara, H., Kimura, S., Tombe, Y., Kobayashi, M., Mitsui, Y., Yazaki, Y., Goto, K. and Masaki, T., Endothelin: a novel potent vasoconstrictor peptide produced by vascular endothelial cells, Nature, 332 (1988) 411–415.