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. 2013 Sep 5;18(9):10953–10972. doi: 10.3390/molecules180910953

Table 2.

Recently evaluated compounds with promising antagonistic activity against P2X7R.

Compound Company Study Trial Phase Completed Observed Result Observed Side Effect Reference
A-438079 Abbott Laboratories Neuropathic and inflammatory pain Pre-clinical Yes Inhibited mechanical allodynia and effective in the formalin pain model Not evaluated [114]
A-740003 Abbott Laboratories Neuropathic and inflammatory pain Pre-clinical Yes Analgesic effect in inflammatory and neuropathic pain in rat Not evaluated [52]
A804598 Abbott Laboratories Neuropathic and inflammatory pain Pre-clinical Yes Analgesic effect in inflammatory and neuropathic pain in rat Not evaluated [25]
A847227 Abbott Laboratories Anti-inflammatory and neuropathic pain Pre-clinical Yes Antiallodynic activity and reduced the release of IL-1β in the zymosan mouse model Not evaluated [55]
AZ10606120 AstraZeneca Ligand interaction and binding with P2X7R Pre-clinical Yes Its molecule binds to a site different from which ATP binds, but it acts as a negative allosteric modulator Not evaluated [25]
AZ11645373 AstraZeneca Selective potency Pre-clinical Yes Inhibited hP2X7R and its pharmacologic properties Not evaluated [53]
AZD9056 AstraZeneca Rheumatoid arthritis II Yes No efficacy Gastrointestinal (nausea, diarrhea, and vomiting) [84]
CE-224,835 Pfizer Rheumatoid arthritis II Yes No efficacy Gastrointestinal (nausea and diarrhea) [83]
EVT-401 Evotec The pharmacokinetic profile and pharmacodynamic effects I Yes Safe and well tolerated Not related [78]
GSK314118A Glaxo Inflammatory pain Pre-clinical Yes Analgesic activity in rat CFA model of inflammatory hyperalgesia Not related [55]