Brilliant Blue G is triphenylmethane dye that was developed for use in the textile industry but is now commonly used for staining proteins in analytical biochemistry. The Bradford assay is a standard, rapid dye-binding assay that uses Brilliant Blue G to quantify the amount of protein in a solution. Brilliant Blue G also acts as a selective inhibitor of the P2X purinoceptor channel P2X7 (IC50s = 10.1 and 265 nM for rat and human P2X7, respectively). In mice, it inhibits interleukin-1β expression and reduces neurological injury secondary to traumatic brain injury. Brilliant Blue G was used to prepare the protein reagent for the determination of protein content of the collagenase enzyme isolated from fish waste. It may be employed as a stain for the internal limiting membrane (ILM) for the macular hole (MH) and epiretinal membrane (ERM) surgery.

Prochlorperazine is a piperazine phenothiazine antipsychotic which block postsynaptic mesolimbic dopaminergic receptors in the brain and has antiemetic effects by its antagonist actions in the D2 dopamine receptors in the chemoreceptor trigger zone. It also exhibits alpha-adrenergic blocking effect on α1 receptros and may depress the release of hypothalamic and hypophyseal hormones. Prochlorperazine is used for the control of severe nausea and vomiting, for the treatment of schizophrenia. Prochlorperazine is effective for the short-term treatment of generalized non-psychotic anxiety. Prochlorperazine may be an effective treatment of acute headaches and refractory chronic daily headache.

GSK-1482160 is being evaluated for treatment of inflammatory pain (such as arthritis). This compound acts on P2X7 receptors, expressed by cells of innate and adaptive immunity. P2X7 receptors are involved in the production of pro-inflammatory cytokines that are thought to be an important mediator of inflammation. By blocking P2X7 receptors, less inflammatory chemicals are released, which possibly results in less inflammatory pain. Because of its ability to target P2X7R with high selectivity and to be radiolabelled with 11C, GSK-1482160 was suggested to be a useful biomarker for neuroinflammation via positron emission tomography (PET).

AZD9056 was developed as a selective inhibitor of the purinergic receptor P2X7, a key player in the generation and secretion of several proinflammatory cytokines. AZD 9056 participated is phase II clinical trials for osteoarthritis, inflammatory bowel disease, and chronic obstructive pulmonary disease but these studies were discontinued in 2009 because the drug failed to show significant efficacy in trials. In addition, in 2015 AZD 9056 was studied for the treatment of Crohn's disease (CD), although the drug has shown a beneficial risk profile the lack in the change of inflammatory biomarkers questions its anti-inflammatory potential.

CE-224535 is a potent, highly selective, orally bioavailable, non-competitive antagonist of the human P2X7 receptor. Pre-clinical pharmacokinetic studies with CE-224535 indicate limited CNS penetration. In clinical trials, CE-224535 failed to demonstrate efficacy in a 2-week study of knee pain in osteoarthritis or a 12-week study in patients with rheumatoid arthritis. CE-224535 is safe and well tolerated after administration of up to 1600 mg as a single dose or 600 mg every 12 hours for 14 days in healthy subjects and 500 mg every 12 hours for 2 weeks in subjects with osteoarthritis of the knee and 12 weeks in rheumatoid arthritis patients with an inadequate response to methotrexate.

A-740003 is a competitive antagonist of P2X purinoceptor 7 (P2X7) that has been shown to potently block proinflammatory cytokine interleukin-1β (IL-1β) release, and also is a promising candidate for the development of a radiotracer for imaging of neuroinflammation by positron emission tomography.

AZ11645373 is a potent and selective antagonist of human P2X7, that was developed by Astra Pharmaceuticals Ltd for treatment pain. AZ11645373 Inhibits BzATP-mediated calcium influx and inhibits ATP-mediated IL-1β release in vitro. AZ11645373 in addition to its well-characterized ability to inhibit the pro-inflammatory action of ATP demonstrates a broad P2X7 receptor-independent anti-inflammatory activity against chemically different types of inflammatory agonists. This type of polypharmacology may be especially effective for treatment of inflammatory disorders due to a combination of P2X7-dependent and P2X7-independent anti-inflammatory mechanisms. In other words, AZ11645373 has a potential to induce several beneficial effects including inhibition of inflammasome-mediated generation of IL-1β and IL-18, inhibition of inflammatory pain.

KN-62 (1-[N,O-Bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine) is an inhibitor of Ca2+/calmodulin-dependent protein kinase II (Ca2+/CaM kinase II). In addition, it acts as an antagonist of the P2X7 receptor.

Prochlorperazine is a piperazine phenothiazine antipsychotic which block postsynaptic mesolimbic dopaminergic receptors in the brain and has antiemetic effects by its antagonist actions in the D2 dopamine receptors in the chemoreceptor trigger zone. It also exhibits alpha-adrenergic blocking effect on α1 receptros and may depress the release of hypothalamic and hypophyseal hormones. Prochlorperazine is used for the control of severe nausea and vomiting, for the treatment of schizophrenia. Prochlorperazine is effective for the short-term treatment of generalized non-psychotic anxiety. Prochlorperazine may be an effective treatment of acute headaches and refractory chronic daily headache.

Prochlorperazine is a piperazine phenothiazine antipsychotic which block postsynaptic mesolimbic dopaminergic receptors in the brain and has antiemetic effects by its antagonist actions in the D2 dopamine receptors in the chemoreceptor trigger zone. It also exhibits alpha-adrenergic blocking effect on α1 receptros and may depress the release of hypothalamic and hypophyseal hormones. Prochlorperazine is used for the control of severe nausea and vomiting, for the treatment of schizophrenia. Prochlorperazine is effective for the short-term treatment of generalized non-psychotic anxiety. Prochlorperazine may be an effective treatment of acute headaches and refractory chronic daily headache.