Thromboxane (TXA₂) activates the T prostanoid (TP) receptor. Prostaglandin E₂ (PGE₂) activates four E prostanoid (EP) receptors, EP_1-4. AH-23848 is a dual antagonist of TP¹ and EP₄ receptors.² It originally was found to inhibit TXA₂-induced platelet aggregation (IC₅₀ = 0.26 μM)¹ and the contraction of human bronchial smooth muscle induced by the TP agonist U-46619.³ AH-23848 was subsequently demonstrated to impair PGE₂-mediated relaxation of piglet saphenous vein by antagonizing the PGE₂ receptor EP₄.² By inhibiting EP₄, it likewise suppresses serum-induced cAMP generation, cyclin A synthesis, and the proliferation of fibroblasts⁴, as well as reduces metastasis in a mouse model of metastatic breast cancer.⁵

≥90%

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1.Brittain, R.T.,Boutal, L.,Carter, M.C., et al. AH23848: A thromboxane receptor-blocking drug that can clarify the pathophysiologic role of thromboxane A₂. Circulation 72, 1208-1218 (1985).

2.Coleman, R.A.,Grix, S.P.,Head, S.A., et al. A novel inhibitory prostanoid receptor in piglet saphenous vein. Prostaglandins 47, 151-168 (1994).

3.Coleman, R.A. and Sheldrick, R.L.G. Prostanoid-induced contraction of human bronchial smooth muscle is mediated by TP-receptors. British Journal of Pharmacology 96, 688-692 (1989).

4.Sanchez, T. and Moreno, J.J. Role of EP₁ and EP₄ PGE₂ subtype receptors in serum-induced 3T6 fibroblast cycle progression and proliferation. American Journal of Physiology.Cell Physiology 282, C280-C288 (2002).

5.Ma, X.,Kundu, N.,Rifat, S., et al. Prostaglandin E receptor EP₄ antagonism inhibits breast cancer metastasis. Cancer Research 66(6), 2923-2927 (2006).