L-161,982

L-161,982 is a potent and highly selective small molecule antagonist of the Prostaglandin E2 (PGE2) receptor subtype 4 (EP4). Developed by Merck Frosst, it is widely utilized as a pharmacological tool to investigate the physiological and pathological roles of EP4 signaling. The EP4 receptor is a G protein-coupled receptor that typically mediates its effects through the activation of adenylate cyclase, leading to increased intracellular cAMP levels. By competitively binding to the EP4 receptor, L-161,982 inhibits PGE2-induced signaling pathways involved in inflammation, pain, bone remodeling, and cancer progression. Preclinical research has demonstrated its utility in suppressing inflammatory responses in models of rheumatoid arthritis and inflammatory bowel disease, as well as inhibiting tumor cell proliferation and migration in various oncology models. While it is a standard reference compound in prostaglandin research, it has primarily functioned as a laboratory tool rather than a clinical therapeutic candidate.

Other names

4'-[[4,9-dihydro-1-oxo-2-[2-(2-thienyl)ethyl]-1H-pyrano[3,4-b]indol-2-yl]methyl][1,1'-biphenyl]-2-sulfonamideN-[[2'-(aminosulfonyl)[1,1'-biphenyl]-4-yl]methyl]-N-[2-(2-thienyl)ethyl]-9H-pyrido[3,4-b]indole-3-carboxamide