产品描述:
The prostaglandin E2 (PGE2) receptor EP1 is involved in triggering PGE2-mediated pain, neuronal survival and growth as well as the suppression of tumor metastasis. SC-19220 is a dibenzoxazepine that acts as a selective antagonist of PGE2 at the EP1 receptor.{6742,2681} At doses between 0.3-300 µM, SC-19220 acts as a competitive antagonist of PGE2-induced smooth muscle contractions of guinea pig ileum and stomach.{6911,6856} SC-19220 also acts as a PGE2 antagonist in the EP1 receptor-mediated contraction of guinea pig trachea.{6294} SC-19220 displaces radiolabeled PGE2 from the cloned human EP1 receptor with an IC50 of 6.7 µM and exhibits no binding at the human EP2 receptor.{3176,3186} It binds with apparent low affinity to the cloned mouse EP1 receptor expressed in CHO cells.{6640} In a model of bone resorption, 3-150 μM SC-19220 inhibited both 1,25 dihydroxy vitamin D3- and PGE2-stimulated osteoclastogenesis in mouse osteoclast precursors.{23818} Antagonism of EP1 with 1 μM SC-19220 has been shown to promote metastasis in a mouse model of metastatic breast cancer.{18890} In a rodent model of Parkinson’s disease, 1.5 μM SC-19220 prevented PGE2-mediated loss of dopaminergic neurons from rat substantia nigra.{15975}