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An EP1 receptor antagonist (Kis 0.6 and 1.7 nM for human and mouse receptors respectively expressed in CHO cells) is selective for EP1 over EP2 EP3 and EP4 (Kis 1000 67 and 1000 nM respectively for mouse receptors expressed in CHO cells) inhibits PGE2-induced increases in intracellular calcium concentrations in cells expressing human or mouse EP1 (EC50s 50 and 210 nM respectively) reduces the incidence of squamous cell carcinoma and severe dysplasia induced by 4-nitroquinoline 1-oxide in a rat model of tongue carcinogenesis at 400 and 800 ppm in the diet
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A triterpenoid with diverse biological activities inhibits ACE (IC50 734 UM) cytotoxic to HepG2 HeLa and Caco-2 cancer cells (IC50s 0.14 0.18 and 0.26 mg/ml respectively) inhibits LPS-induced NO production in BV-2 microglia (IC50 13.77 UM)
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An analytical reference standard categorized as a triazolobenzodiazepine an active metabolite of rilmazafone intended for research and forensic applications
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An antagonist of NR2B subunit-containing NMDA receptors (Ki 72 nM) selective for NR2B subunit-containing NMDA receptors over those containing NR2A subunits (IC50s 47 and 10000 nM respectively) reduces carrageenan-induced hyperalgesia in rats (ED50 5.5 mg/kg) reduces dopaminergic neuron loss in the rat substantia nigra pars compacta and improves measures of ipsilateral curling ipsilateral head positioning and beam walking in a rat model of 6-OHDA-induced Parkinsons disease at 10 mg/kg
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