Prostaglandin E₂ (PGE₂) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP₂ is a G protein-coupled receptor that has diverse roles, including those in cancer, inflammation, and neuroprotection.^1,2,3 TG4-155 is a brain penetrant EP₂ antagonist (K_B = 2.4 nM) that is over 1000-fold less effective at EP₄ (K_B = 11.4 µM) and a panel of other receptors and channels.^4,5 It blocks the induced expression of inflammatory markers in microglial cells treated with the selective EP₂ agonist butaprost (Item No. 13740) alone or with LPS and IFNγ.^4,6 TG4-155 significantly reduces neurodegeneration in a mouse model of status epilepticus, induced by pilocarpine (Item No. 14487).⁴ It inhibits proliferation, invasion, and inflammatory cytokine expression in cancer cells treated with butaprost.⁵

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1.Majima, M.,Amano, H. and Hayashi, I. Prostanoid receptor signaling relevant to tumor growth and angiogenesis. Trends in Pharamacological Sciences 34(10), 524-529 (2003).

2.Jiang, J. and Dingledine, R. Prostaglandin receptor EP₂ in the crosshairs of anti-inflammation, anti-cancer, and neuroprotection. Trends in Pharamacological Sciences 34(7), 413-423 (2013).

3.Kawahara, K.,Hohjoh, H.,Inazumi, T., et al. Prostaglandin E₂-induced inflammation: Relevance of prostaglandin E receptors. Biochimica et Biophysica Acta 1851(4), 414-421 (2015).

4.Jiang, J.,Ganesh, T.,Du, Y., et al. Small molecule antagonist reveals seizure-induced mediation of neuronal injury by prostaglandin E₂ receptor subtype EP₂. Proceedings of the National Academy of Sciences of the United States of America 109(8), 3149-3154 (2012).

5.Jiang, J. and Dingledine, R. Role of prostaglandin receptor EP₂ in the regulations of cancer cell proliferation, invasion, and inflammation. Journal of Pharmacology and Experimental Therapeutics 344, 360-367 (2013).

6.Quan, Y.,Jiang, J. and Dingledine, R. EP₂ receptor signaling pathways regulate classical activation of microglia. The Journal of Biological Chemisty 288(13), 9293-9302 (2013).