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ER 819762 is a potent EP4 receptor antagonist (IC50 = 59 nM). Suppresses EP4-mediated Th1 differentiation, Th17 cell expansion, and IL-23 secretion by activated dendritic cells. Inhibits Th1 and Th17 cytokine production, suppresses collagen- and GPI-induced arthritis in mice. Attenuates CFA-induced inflammatory pain in rats. Analgesic. Orally bioavailable.
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The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
Chen et al (2010) A novel antagonist of the prostaglandin E2 EP4 receptor inhibits Th1 differentiation and Th17 expansion and is orally active in arthritis models. Br.J.Pharmacol. 160 292 PMID: 20423341
Jones et al (2016) Role of EP2 and EP4 receptors in airway microvascular leak induced by prostaglandin E2. Br.J.Pharmacol. 173 992 PMID: 26639895
Keywords: ER 819762, ER 819762 supplier, ER819762, potent, EP4, receptors, antagonists, prostanoids, PGE2, prostaglandins, high, affinity, orally, active, bioavailable, analgesics, arthritis, inflammatory, pain, inflammation, Prostanoid, Receptors, 5924, Tocris Bioscience
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.