AZ11645373 is a selective and potent human P2X7 purinoceptor antagonist. AZ11645373 has been used in the rhesus macaque monkey to elucidate the mechanisms and pharmacological interventions of P2X7 receptor-related diseases.
Ações bioquímicas/fisiológicas
AZ11645373 is a selective and potent human P2X7 purinoceptor antagonist. KB values range from 5-20 nM for human P2X7 receptor inhibition. It is 500-fold less effective ats an inhibitor of rat P2X7 receptor responses.
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This compound is featured on the P2 Receptors: P2X Ion Channel Family page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by AstraZeneca. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
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British journal of pharmacology, 157(7), 1215-1224 (2009-06-26)
P2X receptors are widely expressed in cells of the immune system with varying functions. This study sought to characterize P2X receptor expression in the LAD2 human mast cell line and human lung mast cells (HLMCs). Reverse transcriptase polymerase chain reaction
British journal of pharmacology, 149(7), 880-887 (2006-10-13)
The ATP-gated P2X(7) receptor has been shown to play a role in several inflammatory processes, making it an attractive target for anti-inflammatory drug discovery. We have recently identified a novel set of cyclic imide compounds that inhibited P2X(7) receptor-mediated dye
Structure (London, England : 1993), 28(2), 157-168 (2019-12-28)
The interactions between SUMO proteins and SUMO-interacting motif (SIM) in nuclear bodies formed by the promyelocytic leukemia (PML) protein (PML-NBs) have been shown to be modulated by either phosphorylation of the SIMs or acetylation of SUMO proteins. However, little is
British journal of pharmacology, 164(2b), 743-754 (2011-04-05)
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
Journal of immunology (Baltimore, Md. : 1950), 185(4), 2611-2619 (2010-07-20)
The ATP-gated P2X(7) receptor (P2X(7)R) is a promising therapeutic target in chronic inflammatory diseases with highly specific antagonists currently under clinical trials for rheumatoid arthritis. Anti-inflammatory actions of P2X(7)R antagonists are considered to result from inhibition of P2X(7)R-induced release of
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