دورية أكاديمية
Radioligand binding and functional characterization of recombinant human NmU1 and NmU2 receptors stably expressed in clonal human embryonic kidney-293 cells.
| العنوان: | Radioligand binding and functional characterization of recombinant human NmU1 and NmU2 receptors stably expressed in clonal human embryonic kidney-293 cells. |
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| المؤلفون: | Aiyar N; Vascular Biology, Cardiovascular and Urogenital Center of Excellence for Drug Discovery, GlaxoSmithKline, King of Prussia, PA 19406-0939, USA. nambi_aiyar-1@gsk.com, Disa J, Foley JJ, Buckley PT, Wixted WE, Pullen M, Shabon U, Dul E, Szekeres PG, Elshourbagy NA, Sarau HM, Appelbaum E, Bolaky J |
| المصدر: | Pharmacology [Pharmacology] 2004 Sep; Vol. 72 (1), pp. 33-41. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Karger Country of Publication: Switzerland NLM ID: 0152016 Publication Model: Print Cited Medium: Print ISSN: 0031-7012 (Print) Linking ISSN: 00317012 NLM ISO Abbreviation: Pharmacology Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Basel (Switzerland) : Karger, |
| مواضيع طبية MeSH: | Membrane Proteins/*metabolism , Receptors, Neurotransmitter/*metabolism, Binding Sites ; Cells, Cultured ; Clone Cells ; Humans ; Kidney/metabolism ; Membrane Proteins/genetics ; Membrane Proteins/physiology ; Oligonucleotide Array Sequence Analysis ; Radioligand Assay ; Receptors, Neurotransmitter/genetics ; Receptors, Neurotransmitter/physiology ; Signal Transduction |
| مستخلص: | Neuromedin U (NmU) is a smooth muscle contracting peptide. Recently, two G-protein-coupled receptors for NmU (NmU1R and NmU2R) have been cloned having approximately 50% homology. They have distinct patterns of expression suggesting they may have different biological functions. This study provides a comprehensive characterization of both NmU receptors expressed in human embryonic kidney 293 cells. [125I]hNmU binding to the recombinant NmU receptors was rapid, saturable, of high affinity and to a single population of binding sites. Exposure of these cells to NmU isopeptides resulted in an increase in intracellular [Ca2+]i release (EC50 value of 0.50 +/- 0.10 nmol/l) and inositol phosphate formation (EC50 1.6 +/- 0.2 and 1.50 +/- 0.4 nmol/l for NmU1R and NmU2R respectively). Furthermore, hNmU inhibited forskolin (3 micromol/l)-stimulated accumulation of cAMP in intact HEK-293 cells expressing either NmU1R or NmU2R. The inhibitory effect was significant for the cells expressing NmU2R with IC50 value of 0.80 +/- 0.21 nmol/l. In summary, both NmU1R and NmU2R in HEK-293 cells have similar signaling capability. (Copyright 2004 S. Karger AG, Basel) |
| المشرفين على المادة: | 0 (Membrane Proteins) 0 (Receptors, Neurotransmitter) 0 (neuromedin U receptor) |
| تواريخ الأحداث: | Date Created: 20040805 Date Completed: 20041026 Latest Revision: 20041117 |
| رمز التحديث: | 20240829 |
| DOI: | 10.1159/000078630 |
| PMID: | 15292653 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 0031-7012 |
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| DOI: | 10.1159/000078630 |