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A lignan with diverse biological activities; induces cell cycle arrest at the G0/G1 phase and inhibits growth of T47D and MDA-MB-231 breast cancer cells at 100 μM; prevents glutamate-induced cytotoxicity, inhibits production of NO and ROS, and preserves the mitochondrial membrane potential in isolated rat cortical cells at 10 and 100 μM; reduces cisplatin-induced apoptosis in HK-2 cells; reverses scopolamine-induced impairment of spatial memory and the passive avoidance response in rats at 1 and 10 mg/kg; enhances oxotremorine-induced tremors in mice; reduces serum levels of IgE, IgG1, IL-4, and IFN-γ in an ovalbumin-sensitized mouse model of allergy at 10 mg/kg
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A lichen metabolite with diverse biological activities; active against various bacteria (MICs = 4-16 μg/ml); prevents UVB-induced apoptosis, cytotoxicity, and cytoskeletal modifications in HaCaT human keratinocytes from 25-800 μM; increases scratch wound healing of HaCaT cells; reduces hydrogen peroxide-induced production of ROS and cytotoxicity in HUVECs at 15 μM
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A polyamine bile amidate; has been found in lion, but not mouse, fecal samples; has been used as a standard in the detection of chenodeoxycholyl-putrescine in mammalian intestinal and fecal samples
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An inhibitor of heteromeric Kir4.1/5.1 channels (IC50 = 0.24 µM); selective for Kir4.1/5.1 channels over a variety of homomeric Kir channels, including Kir4.1 (IC50 = >10 µM), as well as heteromeric Kir3.1/3.2, Kir3.1/3.4, Kir6.2/SUR1, and Kir6.1/SUR2b channels at 30 µM but does inhibit the voltage-gated potassium channel Kv1.1 (IC50 = 6.4 µM); does not inhibit diuresis in mice at 30 and 100 mg/kg due to low oral bioavailability and high hepatic clearance
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A 2,4-disubstituted pyrimidine that, at 2 µM, enhances the survival of hESC more than 30-fold after trypsin-mediated dissociation; increases integrin-dependent attachment of hESC to extracellular matrices
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An acetylated analog of methylone, the MDMA-type designer drug that has been detected in products marketed as bath salts, plant food, and tablets; intended for forensic and research purposes
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An orally bioavailable 5-HT3 antagonist (Ki = 2.9 nM); selective for 5-HT3 over 5-HT1A and 5-HT2 (IC50 = >10 μM for both), as well as D1, D2, α1-, and α2-adrenergic receptors (IC50s = >10 μM); binds to H1 receptors (IC50 = 4.4 μM); inhibits 5-HT-induced contractions in isolated guinea pig ileum (pA2 = 7.04) and isolated rabbit heart (pA2 = 10.06); inhibits cisplatin-induced emesis in dogs and doxorubicin/cyclophosphamide-induced emesis in ferrets at 1 mg/kg
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A nonapeptide hormone primarily synthesized in the hypothalamus with roles in uterine contraction and lactation, social memory and attachment, sexual and maternal behavior, aggression, learning, anxiety, feeding, and pain perception
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A melatonin receptor agonist (Kis = 0.14 and 0.41 nM for MT1 and MT2, respectively) and 5-HT2B and 5-HT2C antagonist (Kis = 0.26 and 0.71 nM, respectively); inhibits the 5-HT2-mediated penile erection response in rats at 40 mg/kg; increases extracellular levels of noradrenaline and dopamine in the frontal cortex of freely moving rats at 20-80 mg/kg; reduces immobility time in the forced swim test and increases the amount of time spent in the open arms of the elevated plus maze in mice in a transgenic neuroendocrine model of depression at 10 mg/kg
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A cAMP-dependent PDE3 inhibitor (IC50s = 0.04 and 0.03 nM for PDE3A and PDE3B, respectively in T84 cell lysates); stimulates cAMP accumulation (10 µM) and increases membrane capacitance in rat juxtaglomerular cells; competitively inhibits multidrug resistant protein 5-mediated export of cGMP from Chinese hamster lung fibroblasts (Ki = 240 nM); reduces collagen-induced platelet aggregation in rabbits (3 UG/kg per minute); reduces collagen-induced decreases in mean arterial blood pressure alone or in combination with prostacyclin
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A triacylglycerol; has been used as a reagent to study the regioselectivity of thermal chlorination reactions between triacylglycerols and organochlorines that result in the formation of MCPD diesters
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A TLR7 and TLR9 antagonist (IC50s = 1.78 and 0.01 µM, respectively); selective for TLR7 and TLR9 over TLR4 (IC50 = 10.58 µM); inhibits CpG ODN2216- or RNA40-induced IL-6 production in isolated mouse BMDCs; prevents increases in left ventricle chamber size and cardiac fibrosis in a mouse model of transverse aortic constriction-induced heart failure at 1.5 mg/animal; increases survival and reduces increases in right ventricular systolic pressure and hypertrophy in a rat model of monocrotaline-induced pulmonary hypertension at 10 mg/kg; has been used to enhance the transfection efficiency of cell-penetrating peptides for the delivery of mRNA in vitro
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