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A thiazide diuretic; inhibitor of carbonic anhydrase (CA); selective for CAII, VB, VII, IX, XII, and XIV (Kis = 305-235 nM) over CAI, IV, and VI (Kis = 2,840-8,250 nM) and CAIII, VA, and XIII (Kis = >10 µM)
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A colorimetric β-glucuronidase substrate; upon enzymatic cleavage, p-nitrophenol is released, which can be quantified by colorimetric detection at 405 nm as a measure of β-glucuronidase activity
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A potent agonist of the serotonin 4 receptor (5-HT4, Ki = 3.9-31 nM; also acts as an antagonist for the 5-HT2A, 5-HT2B, and 5-HT2C receptors (Ki = 32, 3.9, and 100 nM, respectively); stimulates colonic motility and transit in vivo
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A partial agonist of central benzodiazepine receptors (Ki = 78 nM in a radioligand binding assay); potentiates muscle relaxant and hypnotic effects of diazepam in mice; increases drinking in the Vogel punished drinking task indicating anxiolytic-like activity
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A synthetic glucocorticoid; increases expression of the calcitonin receptor in in murine osteoclast-like cells at 1 μM; reduces heat hyperalgesia and mechano-allodynia and decreases the number of TNF-α-positive mast cells in injured sciatic nerve in a rat model of chronic constriction injury-induced neuropathic pain at 3 mg/kg, s.c.; reduces levels of the glycosaminoglycans hyaluronic acid and chondroitin-4-sulfate in human keloid implants in athymic nude mice
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An NSAID and diethylene glycol ester form of flufenamic acid; inhibits lipoxygenase isolated from guinea pig leukocytes (IC50 = 5.3 μM) and production of PGE2 in stimulated rat peritoneal macrophages; reduces acetic acid-induced vascular permeability in mice and UV-induced erythema in guinea pigs in a dose-dependent manner at doses ranging from 40-320 and 5-20 mg/kg, respectively; inhibits inflammation in a rat model of adjuvant-induced arthritis; decreases the pain response in a silver nitrate-induced rat model of arthritis and the acetic acid-induced writhing test in mice, indicating analgesic activity
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An amino monosaccharide; induces site-specific DNA damage at pyrimidine residues in cell-free assays; 1-amino-1-deoxy-D-fructose moieties have been found as a component of fructosamines
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A structural analog of γBB that inhibits γBB hydroxylase (IC50 = 62 µM) and carnitine acetyltransferase (Ki = 1.6 mM); has cardioprotective and neuroprotective effects; improves cognition and reduces amyloid-β pathology in a mouse model of Alzheimer’s disease
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A PARP1 inhibitor; reduces PARP1 activity in D283 Med cancer cells by 91.7% at 1 µM; selectively inhibits the proliferation of MDA-MB-436 cancer cells expressing mutant BRCA1 (IC50s = 1.3 µM) over MCF-7 cancer cells expressing wild-type BRCA1 and BRCA2 (IC50s = 20.2 µM); potentiates temozolomide-induced growth inhibition in D283 Med and D384 Med cells at 0.4 µM; potentiates temozolomide-induced delays in tumor growth in D283 Med and D384 Med mouse xenograft models at 1 mg/kg per day
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A DPP-4 inhibitor (IC50 = 0.01 µM); selective for DPP-4 over DPP-8, DPP-9, and FAP- α (IC50s = 277.28, 233.72, 418.43 µM, respectively); inhibits DPP-4 activity in isolated human plasma (IC50 = 11.5 nM); scavenges methylglyoxal in vitro and inhibits AGE formation between BSA and methylglyoxal and cross-linking of AGE-BSA with rat tail tendon collagen (IC50s = 1.15, 11.69, and 1.39 mM, respectively); reduces the levels of circulating AGE and red blood cell IgG content in db/db diabetic mice at 100 mg/kg; decreases blood glucose and HbA1c levels and reduces pancreatic β-cell damage in a mouse model of STZ- and high-fat diet-induced diabetes; induces cytotoxicity in SW1736 and TPC-1 cells
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A guanidino compound with epileptogenic activity; induces whole-cell currents in rat hippocampal slices; intrahippocampal administration induces status epilepticus and neuronal cell death in rats
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A partial agonist of α7 subunit-containing nAChRs (IC50 = 22.38 nM); 1,000-fold selective for α7 subunit-containing nAChRs over α4β2 subunit-containing nAChRs at 10 µM, as well as a panel of 60 peptide and nonpeptide receptors, ion channels, and transporters; induces inward currents in Xenopus oocytes expressing human α7 subunit-containing nAChRs (EC50 = 0.16 µM); reverses scopolamine-induced deficits in the novel object recognition task and prevents natural forgetting of a familiar object in rats at 0.1, 0.3, and 1 mg/kg; reduces premature responding in the 5CSRTT in low-attentive female rats
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