Pharmacological properties of the rhesus macaque monkey P2X7 receptor

Helen J. Bradley, Liam E. Browne, Wei Yang, Lin Hua Jiang

    Research output: Contribution to journalArticlepeer-review


    BACKGROUND AND PURPOSE The human P2X7 (hP2X7) receptor exhibits striking pharmacological differences from its rodent counterparts, particularly in terms of its antagonist profile. Here, we characterized the functional and pharmacological properties of the rhesus macaque monkey P2X7 (rmP2X7) receptor in comparison with the hP2X7 receptor. EXPERIMENTAL APPROACH The rmP2X7 and hP2X7 receptors were heterologously expressed in HEK293 cells. The receptor surface and total expression levels were examined by biotin-labelling and Western blotting. The functional and pharmacological properties were characterized using patch-clamp recording and single-cell imaging. KEY RESULTS The rmP2X7 receptor showed strong cell surface expression. Both ATP and 2′(3′)-O-(4-benzoylbenzoyl) adenosine-5′-triphosphate (BzATP) were full agonists in activating the rmP2X7 receptor; the EC 50 values were 802 μM for ATP and 58 μM for BzATP, respectively, in extracellular low divalent cation solution. Prolonged activation of the rmP2X7 receptors induced detectable but low level YO-PRO-1 uptake. KN-62, AZ11645373 and A-438079, three hP2X7 selective antagonists, all potently inhibited the rmP2X7 receptor-mediated currents; the IC 50 values were 86, 23 and 297 nM respectively. CONCLUSION AND IMPLICATIONS The rmP2X7 receptor exhibits similar pharmacological properties to the hP2X7 receptor. The rhesus macaque monkey thus may represent a valuable model species in elucidating the mechanisms and pharmacological interventions of hP2X7 receptor-related diseases. © 2011 The British Pharmacological Society.
    Original languageEnglish
    Pages (from-to)743-754
    Number of pages11
    JournalBritish Journal of Pharmacology
    Issue number2 B
    Publication statusPublished - Sept 2011


    • A-438079
    • ATP
    • AZ11645373
    • BzATP
    • KN-62
    • rhesus macaque monkey P2X7 receptor


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