L-161,982

Description

Prostaglandin E₂ (PGE₂) exerts its effects through four separate G coupled-protein receptors (EP_1-4). L-161,982 is a potent and selective EP₄ receptor antagonist. It demonstrates selective binding to human EP₄ receptors with a K_i value of 0.024 μM compared to other receptors of the prostanoid family, EP₁, EP₂, EP₃, DP, FP, and IP, with K_i values of 17, 23, 1.9, 5.1, 5.6, and 6.7 μM, respectively. L-161,982 at 10 mg/kg/day suppresses PGE₂-stimulated bone formation in young rats and at 100 nM reverses the anti-inflammatory action of PGE₂ in LPS-activated human macrophages. At 10 μM L-161982 blocks PGE₂-induced cell proliferation in HCA-7 colon cancer cells.

Uses

L-161,982 is an EP4 receptor antagonist, which blocks prostaglandin E2-induced signal transduction and cell proliferation in HCA-7 colon cancer cells.

Definition

ChEBI: N-[2-[4-[[3-butyl-5-oxo-1-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-4-yl]methyl]phenyl]phenyl]sulfonyl-3-methyl-2-thiophenecarboxamide is a member of biphenyls.

Biological Activity

EP 4 receptor antagonist that is selective over all other members of the prostanoid receptor family (K i values are 0.024, 0.71, 1.90, 5.10, 5.63, 6.74, 19 and 23 μ M for human EP 4 , TP, EP 3 , DP, FP, IP, EP 1 and EP 2 receptors respectively). Suppresses PGE 2 -induced bone formation in rats and prevents the nociceptive response induced by misoprostol in formalin-injected mice.

Biochem/physiol Actions

L-161,982 is a potent 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.

storage

Desiccate at +4°C