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Literature DB >> 12770925

The neuromedin B receptor antagonist, BIM-23127, is a potent antagonist at human and rat urotensin-II receptors.

Christopher L Herold¹, David J Behm, Peter T Buckley, James J Foley, William E Wixted, Henry M Sarau, Stephen A Douglas.

Abstract

The functional activity of the peptidic neuromedin B receptor antagonist BIM-23127 was investigated at recombinant and native urotensin-II receptors (UT receptors). Human urotensin-II (hU-II) promoted intracellular calcium mobilization in HEK293 cells expressing the human UT (hUT) or rat UT (rUT) receptors with pEC(50) values of 9.80+/-0.34 (n=6) and 9.06+/-0.32 (n=4), respectively. While BIM-23127 alone had no effect on calcium responses in either cell line, it was a potent and competitive antagonist at both hUT (pA(2)=7.54+/-0.14; n=3) and rUT (pA(2)=7.70+/-0.05; n=3) receptors. Furthermore, BIM-23127 reversed hU-II-induced contractile tone in the rat-isolated aorta with a pIC(50) of 6.66+/-0.04 (n=4). In conclusion, BIM- 23127 is the first hUT receptor antagonist identified to date and should not be considered as a selective neuromedin B receptor antagonist.

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Year: 2003 PMID： 12770925 PMCID： PMC1573850 DOI： 10.1038/sj.bjp.0705251

Source DB: PubMed Journal: Br J Pharmacol ISSN： 0007-1188 Impact factor: 8.739

19 in total

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Journal: Br J Pharmacol Date: 2000-12 Impact factor: 8.739

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14 in total

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Journal: Br J Pharmacol Date: 2013-02 Impact factor: 8.739

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Journal: Mol Pharmacol Date: 2010-10-13 Impact factor: 4.436

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Authors: Yuan Zhang; Jiaoqian Ying; Dongsheng Jiang; Zhigang Chang; Hua Li; Guoqiang Zhang; Shan Gong; Xinghong Jiang; Jin Tao
Journal: J Biol Chem Date: 2015-02-12 Impact factor: 5.157

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Authors: D A B Rex; G P Suchitha; Akhina Palollathil; Anagha Kanichery; T S Keshava Prasad; Shobha Dagamajalu
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Review 8. International Union of Pharmacology. LXVIII. Mammalian bombesin receptors: nomenclature, distribution, pharmacology, signaling, and functions in normal and disease states.

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Authors: Douglas G Johns; Zhaohui Ao; Diane Naselsky; Christopher L Herold; Kristeen Maniscalco; Lea Sarov-Blat; Klaudia Steplewski; Nambi Aiyar; Stephen A Douglas
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10. Urotensin-II Ligands: An Overview from Peptide to Nonpeptide Structures.

Authors: Francesco Merlino; Salvatore Di Maro; Ali Munaim Yousif; Michele Caraglia; Paolo Grieco
Journal: J Amino Acids Date: 2013-02-25