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EP4 receptor antagonist that is selective over all other members of the prostanoid receptor family (Ki values are 0.024, 0.71, 1.90, 5.10, 5.63, 6.74, 19 and 23 μM for human EP4, TP, EP3, DP, FP, IP, EP1 and EP2 receptors respectively). Suppresses PGE2-induced bone formation in rats and prevents the nociceptive response induced by misoprostol in formalin-injected mice.
|Storage||Desiccate at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 654.72. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.53 mL||7.64 mL||15.27 mL|
|5 mM||0.31 mL||1.53 mL||3.05 mL|
|10 mM||0.15 mL||0.76 mL||1.53 mL|
|50 mM||0.03 mL||0.15 mL||0.31 mL|
References are publications that support the biological activity of the product.
Machwate et al (2001) Prostaglandin receptor EP4 mediates the bone anabolic effects of PGE2. Mol.Pharmacol. 60 36 PMID: 11408598
Oliva et al (2006) Role of periaqueductal grey prostaglandin receptors in formalin-induced hyperalgesia. Eur.J.Pharmacol. 530 40 PMID: 16360148
Balzary et al (2006) Lipopolysaccharide induces epithelium- and prostaglandin E2-dependent relaxation of mouse isolated trachea through activation of cyclooxygenase (COX)-1 and COX-2. J.Pharmacol.Exp.Ther. 317 806 PMID: 16464966
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Keywords: L-161,982, L-161,982 supplier, Selective, EP4, receptors, antagonists, Prostanoid, prostaglandins, prostacyclins, eicosanoids, L161982, Receptors, 2514, Tocris Bioscience
2 Citations for L-161,982
Citations are publications that use Tocris products. Selected citations for L-161,982 include:
Chia et al (2011) Protection of protease-activated receptor 2 mediated vasodilatation against angiotensin II-induced vascular dysfunction in mice. BMC Pharmacol 11 10 PMID: 21955547
Sun et al (2011) Lubiprostone reverses the inhibitory action of mor. on mucosal secretion in human small intestine. Dig Dis Sci 56 330 PMID: 21181441
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in vivo survival assay
Literature in this Area
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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.