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] |