Pharmacological characterization of the P2X(7) receptor on human macrophages using the patch-clamp technique
| Autor: | Dagmar Eschke, Melinda Wüst, Sunna Hauschildt, Karen Nieber |
|---|---|
| Rok vydání: | 2001 |
| Předmět: |
Purinergic P2 Receptor Agonists
Patch-Clamp Techniques Biology Monocytes Receptor subtype chemistry.chemical_compound Adenosine Triphosphate 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine Purinergic P2 Receptor Antagonists Rosaniline Dyes Humans PPADS Patch clamp Receptor Pyridoxal P2x7 receptor Cells Cultured Pharmacology Receptors Purinergic P2 Coomassie Brilliant Blue Macrophages Antagonist General Medicine Molecular biology Electrophysiology chemistry Pyridoxal Phosphate Receptors Purinergic P2X7 |
| Zdroj: | Naunyn-Schmiedeberg's archives of pharmacology. 365(2) |
| ISSN: | 0028-1298 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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