التفاصيل البيبلوغرافية
| العنوان: |
Radioligand Binding and Functional Characterization of Recombinant Human NmU1 and NmU2 Receptors Stably Expressed in Clonal Human Embryonic Kidney-293 Cells. |
| المؤلفون: |
Aiyara, Nambi, Disa, Jyoti, Foley, James J., Buckley, Peter T., Wixted, William E., Pullen, Mark, Shabon, Usman, Dul, Edward, Szekeres, Philip G., Elshourbagy, Nabil A., Sarau, Henry M., Appelbaum, Edward, Bolaky, Jane |
| المصدر: |
Pharmacology; Sep2004, Vol. 72 Issue 1, p33-41, 9p |
| مصطلحات موضوعية: |
PEPTIDES, MUSCLE contraction, RADIOLIGAND assay, ANALYTICAL biochemistry, PROTEIN binding, PROTEINS |
| 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 μmol/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 [ABSTRACT FROM AUTHOR] |
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| قاعدة البيانات: |
Complementary Index |
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