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An active, estrogenic metabolite of daidzein; has vasodilatory action on rat isolated aortic rings at 1 UG/ml; stimulates the estrogen receptor-dependent growth of breast cancer MCF-7 cells at micromolar concentrations
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A β-lactamase inhibitor; inhibits Ambler class A serine penicillinases and class C cephalosporinases, including TEM-1, SHV-1, and P99 (IC50s = 97, 150, and 8.5 nM) and the class D oxacillinase OXA-2 (IC50 = 10 nM); active against Gram-positive (MIC90s = 2-128 UG/ml) and Gram-negative bacteria (MIC90s = 4-128 UG/ml) when used in combination with piperacillin; potentiates the activity of ceftolozane against Enterobacteriaceae in a neutropenic mouse model of thigh infection
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An α2-adrenergic receptor agonist (effective concentrations 10-100 nM) with hypotensive effects; competes for imidazoline I2-binding sites in brown adipose tissue (Ki = 97 nM)
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A synthetic analog of PEA which incorporates an (R)-methyl group vicinal to the alcohol on the ethanolamine moiety, which may protect the molecule from enzymatic hydrolysis, leading to prolonged duration of action and enhanced potency in vivo; expected to show enhancement of the inhibitory activity of PEA on mast cells and other cells known to express the CB2 receptor
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A psychoactive aminoindan which can be found in recreational drug mixtures; potently inhibits serotonin uptake (IC50 = 212 nM) and stimulates its release without inducing neurotoxicity
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An essential ω-6 PUFA; the most abundant PUFA in a variety of foods; dietary sources include vegetable oils, meats, nuts, seeds, and eggs; increases migration of IEC-6 rat intestinal epithelial cells in a wound healing assay at 30 μM; rats fed a linoleate-deficient diet exhibit decreased body weight and an increased ratio of eicosatrienoate to arachidonate in liver and serum phospholipids compared with rats fed a control diet, as well as mild scaling of forepaw skin
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A β1-AR antagonist (Ki = 47 nM in CHO cells expressing the human receptor); selective for β1- over β2- and β3-ARs (Kis = 2,730 and >10,000 nM, respectively, in CHO cells expressing the human receptors); reduces GTP-induced AC activity in CHO cells expressing β1- and β2-ARs at 4.7 µM; reduces the pulse rate in isolated rat atria in a concentration-dependent manner; reduces increased heart rate and MAP at 30 mg/kg in a rat model of systolic hypertension induced by a fructose-rich diet
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An ω-7 monounsaturated fatty acid; increases basal and insulin-stimulated glucose uptake and Glut4 protein levels in 3T3-L1 adipocytes at 200 µM; ex vivo, increases glucose uptake and aerobic and anaerobic glycolysis and reduces de novo fatty acid synthesis and activity of the lipogenic enzymes ACL and G6PDH in isolated murine adipocytes at 300 mg/kg; dietary administration reduces high-fat diet-induced insulin resistance and liver inflammation in mice at 300 mg/kg
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A channel blocker that acts on several TRP channels, including TRPM2, TRPM8, and TRPC6 (IC50 = 1.7, 3.8, and 2.3 μM, respectively); inhibits PLA2, blocking the release of arachidonic acid when given at 50 μM
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An indole-based SERM that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM); antagonizes 17β-estradiol-dependent and hormone-independent growth of breast cancer cell proliferation (80% reduction with 10 nM) in a manner related to cell cycle arrest and downregulation of cyclin D1 and ERα
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A bioactive sphingolipid; inhibits IL-4 production by 16% in PMA-stimulated EL4 T cells at 10 μM; cytotoxic to SK-BR-3 and MCF-7/Adr breast cancer cells (IC50s = 15.9 and 19.9 μM, respectively); increases maturation and stability of F508del-CFTR proteins, enhances cAMP-activated chloride secretion, and suppresses secretion of IL-8 in primary epithelial cells isolated from patients with cystic fibrosis
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A potent and selective antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 0.06 nM); has little or no effect at other 5-HT receptor subtypes or at adrenergic or histamine receptors
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