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Atypical P2X7 receptor pharmacology in two human osteoblast-like cell lines

Alqallaf, Sayed Mahmood, Evans, Bronwen Alice James ORCID: and Kidd, Emma Jane ORCID: 2009. Atypical P2X7 receptor pharmacology in two human osteoblast-like cell lines. British Journal of Pharmacology 156 (7) , pp. 1124-1135. 10.1111/j.1476-5381.2009.00119.x

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Background and purpose: The expression and function of P2X7 receptors in osteoclasts is well established, but less is known about their role in osteoblast-like cells. A study in P2X7 receptor knockout mice suggested the involvement of these receptors in bone formation. We have investigated the expression and pharmacology of several P2X receptors in two human osteosarcoma cell lines to see if they could be involved in bone turnover in man. Experimental approach: Reverse transcriptase-polymerase chain reaction and Western blotting were used to study P2X2, P2X4 and P2X7 receptor expression at mRNA and protein levels, respectively, in human osteoblast-like cells. P2X7 receptor pharmacology was studied by measuring pore formation in the presence of different agonists and antagonists using the YO-PRO 1 uptake method. Key results: P2X4 and P2X7 receptor mRNA and protein were found to be expressed by these cell lines. No evidence was found for P2X4/P2X7 receptor heteropolymerization. 2′-3′-O-(4-benzoylbenzoyl)adenosine 5′-triphosphate (DBzATP) was equipotent to ATP and the antagonists used were either ineffective or weakly blocked pore formation. Conclusions and implications: This study demonstrates that P2X4 and P2X7 receptors are expressed by human osteoblast-like cells. The affinities of the different agonists suggest that the P2X7 receptor is mainly responsible for pore formation although P2X4 receptors may also be involved. The low affinity of DBzATP and the weak action of the antagonists support the previously described atypical pharmacology of the P2X7 receptor in osteoblasts. Targeting the P2X7 receptor in osteoblasts could represent a promising new treatment for bone diseases such as osteoporosis and rheumatoid arthritis.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > R Medicine (General)
R Medicine > RM Therapeutics. Pharmacology
Uncontrolled Keywords: P2X7 receptor; human osteoblast-like cells; pore formation; YO-PRO 1; ATP; DBzATP; MG63 cells; SaOS2 cells
Publisher: Nature Publishing Group
ISSN: 0007-1188
Last Modified: 06 Nov 2022 13:34

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