Search Results - "Lindstrom, Terry D."
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Substituted 3-Imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino- [6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as Highly Selective and Potent Inhibitors of Glycogen Synthase Kinase-3
Published in Journal of medicinal chemistry (29-07-2004)“…Glycogen synthase kinase-3 (GSK3) is involved in signaling from the insulin receptor. Inhibitors of GSK3 are expected to effect lowering of plasma glucose…”
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Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor
Published in The Journal of neuroscience (16-11-2011)“…According to the amyloid cascade hypothesis, cerebral deposition of amyloid-β peptide (Aβ) is critical for Alzheimer's disease (AD) pathogenesis. Aβ generation…”
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The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans
Published in The Journal of neuroscience (21-01-2015)“…BACE1 is a key protease controlling the formation of amyloid β, a peptide hypothesized to play a significant role in the pathogenesis of Alzheimer's disease…”
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Synthesis and Structure−Activity Relationships of Novel Arylpiperazines as Potent and Selective Agonists of the Melanocortin Subtype-4 Receptor
Published in Journal of medicinal chemistry (29-01-2004)“…The melanocortin receptors have been implicated as potential targets for a number of important therapeutic indications, including inflammation, sexual…”
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Synthesis and biological evaluation of an orally active ghrelin agonist that stimulates food consumption and adiposity in rats
Published in Bioorganic & medicinal chemistry letters (06-12-2004)“…LY444711 is an orally active ghrelin agonist that binds with good affinity and is a potent activator of the growth hormone secretagogue receptor 1a (GHS-R1a)…”
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In Vitro Biotransformation and Identification of Human Cytochrome P450 Isozyme-Dependent Metabolism of Tazofelone
Published in Drug metabolism and disposition (01-12-1997)“…Tazofelone is a new inflammatory bowel disease agent. The biotransformation of tazofelone in human livers and the cytochrome P450 responsible for the…”
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Fused Bicyclic Gly-Asp β-Turn Mimics with Specific Affinity for GPIIb-IIIa
Published in Journal of medicinal chemistry (18-11-1999)“…Disubstituted isoquinolones 2 and 3 have affinity for GPIIb-IIIa and represent leads for further structural evaluation. Structure−activity studies centered on…”
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Inhibition of granulocyte cAMP-phosphodiesterase by rolipram in vivo is not sufficient to protect the canine myocardium from reperfusion injury
Published in Journal of cardiovascular pharmacology (01-06-1992)“…The purpose of this study was to determine whether the selective type IV cAMP-phosphodiesterase inhibitor rolipram could reduce the reperfusion injury that…”
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P4-271: Bace inhibitor in vivo proof-of-concept studies in PDAPP mice
Published in Alzheimer's & dementia (01-07-2006)Get full text
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Application of oral bioavailability surrogates in the design of orally active inhibitors of rhinovirus replication
Published in Journal of pharmaceutical sciences (01-08-1999)“…Previous studies in rats and humans demonstrated poor oral bioavailability of potent in vitro 2-aminobenzimidazole inhibitors of rhinovirus replication due to…”
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Fused bicyclic Gly-asp β-turn mimics with potent affinity for GPIIb-IIIa. Exploration of the arginine isostere
Published in Bioorganic & medicinal chemistry letters (21-02-2000)“…6-[4-Amidinobenzoyl]amino]-tetralone-2-acetic acid is a potent antagonist of GPIIb-IIIa. Substitution in the meta position of the benzamidine, or replacement…”
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Stereoselective metabolism of tazofelone, an anti-inflammatory bowel disease agent, in rats and dogs and in human liver microsomes
Published in Chirality (New York, N.Y.) (1999)“…Incubation of (R)‐tazofelone and (S)‐tazofelone in rat, dog, and human liver microsomes demonstrated that the (R)‐tazofelone enantiomer was more rapidly…”
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Benzylamine antioxidants: relationship between structure, peroxyl radical scavenging, lipid peroxidation inhibition and cytoprotection
Published in Journal of medicinal chemistry (01-04-1993)“…Three homologous series of 3,5-dialkoxy-4-hydroxybenzylamines were prepared and tested (1) as peroxyl radical scavengers in homogeneous aqueous solution, (2)…”
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Studies on cytochrome P-450-dependent lipid hydroperoxide reduction
Published in Archives of biochemistry and biophysics (01-01-1984)“…A reconstituted mixed-function oxidase system containing cytochrome P-450, cytochrome P-450 reductase, phosphatidylcholine, and NADPH catalyzed the reduction…”
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Effects of hepatic ischemia-reperfusion injury on the hepatic mixed function oxidase system in rats
Published in Molecular pharmacology (01-12-1990)“…Hepatic ischemia induced in vivo by ligation of the left hepatic lobe of rats for up to 2 hr had no effect on cytochrome P-450, cytochrome c reductase, or lobe…”
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Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins
Published in Journal of medicinal chemistry (01-08-1990)“…The preparation and biological evaluation of a series of 7 beta-[2-(2-aminothiazol-4-yl)-2(Z)-methoximinoacetamido]cep halosporins, substituted at the…”
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Inhibition of microsomal biotransformation by a series of nitrogen and oxygen heterocyclic histamine H2-antagonists
Published in Biochemical pharmacology (15-05-1987)“…A homologous series of potent, long-lasting thiazolo-pyrimidone-pyridine histamine H2-antagonists were examined for their inhibitory effects on rat hepatic…”
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Discovery and development of a novel class of nonsteroidal aromatase inhibitors
Published in Steroids (01-07-1987)“…Efforts to develop a novel class of nonsteroidal aromatase inhibitors began with the discovery that the infertility in male rats exposed to high levels of the…”
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Disposition of the aromatase inhibitor LY56110 and associated induction and inhibition studies in rats, dogs, and monkeys
Published in Fundamental and applied toxicology (01-05-1987)“…Compound LY56110 was well absorbed but slowly excreted in the rat, dog, and monkey. Oral administration of 5 mg/kg of [14C]LY56110…”
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