AM211 is a potent, selective, and orally bioavailable antagonist of prostaglandin D2 (PGD2) receptor type 2 (DP2). It exhibits IC50 values of 4.9 nM, 7.8 nM, 4.9 nM, and 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively. In the presence of 0.2% serum albumin, AM211 inhibits radiolabeled PGD2 binding to human, mouse, guinea pig, and rat DP2 with IC50 values of 12.2 nM, 20.1 nM, 22.9 nM, and 34.2 nM, respectively. AM211 demonstrates high selectivity for DP2 over other receptors in the prostanoid family, with IC50 values for the inhibition of radioligand binding to human TP, IP, DP1, and FP receptors exceeding 100 μM. AM211 (100 μM) exhibits no activity against COX-1, COX-2 enzymes, as well as the PPAR family of nuclear receptors[1].
体内研究
AM211 administered orally at doses of 1, 10, and 30 mg/kg demonstrates a dose-dependent reduction in the number of DK-PGD2-induced peripheral blood leukocytes, with a calculated ED50 of 0.85 mg/kg. At a dose of 30 mg/kg, AM211 also reduces antigen-induced pulmonary inflammation in guinea pigs. Additionally, at a dose of 10 mg/kg administered orally, AM211 induces a significant decrease in ovalbumin (OVA)-induced sneezing in a mouse model of allergic rhinitis[1].
体外研究
AM211 is a potent, selective, and orally bioavailable antagonist of prostaglandin D2 (PGD2) receptor type 2 (DP2). It exhibits IC50 values of 4.9 nM, 7.8 nM, 4.9 nM, and 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively. In the presence of 0.2% serum albumin, AM211 inhibits radiolabeled PGD2 binding to human, mouse, guinea pig, and rat DP2 with IC50 values of 12.2 nM, 20.1 nM, 22.9 nM, and 34.2 nM, respectively. AM211 demonstrates high selectivity for DP2 over other receptors in the prostanoid family, with IC50 values for the inhibition of radioligand binding to human TP, IP, DP1, and FP receptors exceeding 100 μM. AM211 (100 μM) exhibits no activity against COX-1, COX-2 enzymes, as well as the PPAR family of nuclear receptors[1].
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