ArticleBritish journal of pharmacology2003
The neuromedin B receptor antagonist, BIM-23127, is a potent antagonist at human and rat urotensin-II receptors.
Article in British journal of pharmacology, 2003. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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17 citing papers in PubMed, 54 citations in OpenAlex.
- Article
- Exploring a Structural Data Mining Approach to Design Linkers for Head-to-Tail Peptide Cyclization.Journal of chemical information and modeling · 2023Article
- The network map of urotensin-II mediated signaling pathway in physiological and pathological conditions.Journal of cell communication and signaling · 2022Article
- Bombesin Receptor Family Activation and CNS/Neural Tumors: Review of Evidence Supporting Possible Role for Novel Targeted Therapy.Frontiers in endocrinology · 2021Review
- Microinjection of urotensin II into the rostral ventrolateral medulla increases sympathetic vasomotor tone via the GPR14/ERK pathway in rats.Hypertension research : official journal of the Japanese Society of Hypertension · 2020Article
- Urotensin-II receptor stimulation of cardiac L-type Ca2+ channels requires the βγ subunits of Gi/o-protein and phosphatidylinositol 3-kinase-dependent protein kinase C β1 isoform.The Journal of biological chemistry · 2015Article
- Discovery of new antagonists aimed at discriminating UII and URP-mediated biological activities: insight into UII and URP receptor activation.British journal of pharmacology · 2013Article
- Urotensin-II Ligands: An Overview from Peptide to Nonpeptide Structures.Journal of amino acids · 2013Article
- Update on the urotensinergic system: new trends in receptor localization, activation, and drug design.Frontiers in endocrinology · 2012Article
- Gastrin-releasing peptide/neuromedin B receptor antagonists PD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors.Molecular pharmacology · 2011Article
- Potential Clinical Implications of the Urotensin II Receptor Antagonists.Frontiers in pharmacology · 2011Article
- International Union of Pharmacology. LXVIII. Mammalian bombesin receptors: nomenclature, distribution, pharmacology, signaling, and functions in normal and disease states.Pharmacological reviews · 2008Review
- Therapeutic potential of blockade of the urotensin II system in systemic hypertension.Current hypertension reports · 2007Review
- The peptidic urotensin-II receptor ligand GSK248451 possesses less intrinsic activity than the low-efficacy partial agonists SB-710411 and urantide in native mammalian tissues and recombinant cell systems.British journal of pharmacology · 2006Article
- Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.British journal of pharmacology · 2005Article
- Urotensin-II-mediated cardiomyocyte hypertrophy: effect of receptor antagonism and role of inflammatory mediators.Naunyn-Schmiedeberg's archives of pharmacology · 2004Article
- Urantide: an ultrapotent urotensin II antagonist peptide in the rat aorta.British journal of pharmacology · 2003Article
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
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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