Pharmacological characterization of the P2X(7) receptor on human macrophages using the patch-clamp technique
Whole-cell patch-clamp recordings were made from macrophages derived from human monocytes that had been cultured for 5-7 days. The P2X agonists ATP (100 microM) and 2',3'-(4-benzoyl)-benzoyl ATP (BzATP, 100 microM) induced inward currents. A second application of the agonists was character...
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Published in | Naunyn-Schmiedeberg's archives of pharmacology Vol. 365; no. 2; pp. 168 - 171 |
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Main Authors | , , , |
Format | Journal Article |
Language | English |
Published |
Germany
01.02.2002
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Subjects | |
Online Access | Get full text |
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Summary: | Whole-cell patch-clamp recordings were made from macrophages derived from human monocytes that had been cultured for 5-7 days. The P2X agonists ATP (100 microM) and 2',3'-(4-benzoyl)-benzoyl ATP (BzATP, 100 microM) induced inward currents. A second application of the agonists was characterized by strong desensitisation of the maximum current. Pyridoxal phosphate-6-azophenyl-2',4'-disulphonic acid (PPADS), a non-specific P2X antagonist, and 1-( N, O- bis[5-isoquinolinesulphonyl]- N-methyl- L-tyrosyl)-4-phenylpiperazine (KN62), a potent P2X(7) antagonist at the human receptor, both reduced the ATP-induced inward current. KN62 also inhibited the BzATP-induced current. The P2X(7) antagonist Coomassie Brilliant Blue G (BBG), believed to be potent at the human but even more so potent at the rat receptor, did not reduce the BzATP-induced inward current significantly. These results indicate that the native P2X(7) receptor subtype is expressed in human macrophages and that this receptor subtype is involved in the ATP-mediated inward current. Our experiments suggest that other P2X receptors also appear to be involved in the ATP-mediated current in human monocyte-derived macrophages. |
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0028-1298 |
DOI: | 10.1007/s00210-001-0501-2 |