Search Results - "Voorman, Richard L."
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Metabolic Aromatization of N-Alkyl-1,2,3,4-Tetrahydroquinoline Substructures to Quinolinium by Human Liver Microsomes and Horseradish Peroxidase
Published in Drug metabolism and disposition (01-12-2006)“…Metabolic aromatization of xenobiotics is an unusual reaction with some documented examples. For instance, the oxidation of…”
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Prediction of clinical drug-drug interactions of veliparib (ABT-888) with human renal transporters (OAT1, OAT3, OCT2, MATE1, and MATE2K)
Published in Journal of pharmaceutical sciences (01-12-2013)“…Veliparib (ABT-888) is largely eliminated as parent drug in human urine (70% of the dose). Renal unbound clearance exceeds glomerular filtration rate,…”
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Parabens inhibit human skin estrogen sulfotransferase activity: Possible link to paraben estrogenic effects
Published in Toxicology (Amsterdam) (11-04-2007)“…Abstract Parabens ( p -hydroxybenzoate esters) are a group of widely used preservatives in topically applied cosmetic and pharmaceutical products. Parabens…”
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In vitro OATP1B1 and OATP1B3 inhibition is associated with observations of benign clinical unconjugated hyperbilirubinemia
Published in Xenobiotica (01-03-2014)“…Abstract 1. Transient benign unconjugated hyperbilirubinemia has been observed clinically with several drugs including indinavir, cyclosporine, and rifamycin…”
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Interaction of Delavirdine with Human Liver Microsomal Cytochrome P450: Inhibition of CYP2C9, CYP2C19, and CYP2D6
Published in Drug metabolism and disposition (01-01-2001)“…Delavirdine, a non-nucleoside inhibitor of HIV-1 reverse transcriptase, is metabolized primarily through desalkylation catalyzed by CYP3A4 and CYP2D6 and by…”
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Development of in vitro methods to predict induction of CYP1A2 and CYP3A4 in humans
Published in Assay and drug development technologies (01-12-2007)“…The important role of cytochrome P450 (CYP) drug-metabolizing enzymes has been studied for many years, and the potential liabilities of inducing these enzymes…”
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Metabolism of Delavirdine, a Human Immunodeficiency Virus Type-1 Reverse Transcriptase Inhibitor, by Microsomal Cytochrome P450 in Humans, Rats, and Other Species: Probable Involvement of CYP2D6 and CYP3A
Published in Drug metabolism and disposition (01-07-1998)“…The metabolism of delavirdine was examined using liver microsomes from several species with the aim of comparing metabolite formation among species and…”
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Synthesis and Bioactivity of Novel Bis(heteroaryl)piperazine (BHAP) Reverse Transcriptase Inhibitors: Structure−Activity Relationships and Increased Metabolic Stability of Novel Substituted Pyridine Analogs
Published in Journal of medicinal chemistry (20-12-1996)“…The major route of metabolism of the bis(heteroaryl)piperazine (BHAP) class of reverse transcriptase inhibitors (RTIs), atevirdine and delavirdine, is via…”
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Synthesis and Structure−Activity Relationships of the (Alkylamino)piperidine-Containing BHAP Class of Non-Nucleoside Reverse Transcriptase Inhibitors: Effect of 3-Alkylpyridine Ring Substitution
Published in Journal of medicinal chemistry (07-10-1999)“…Development of resistance to currently approved HIV therapies has continued to fuel research efforts to improve the metabolic stability and spectrum of…”
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Microsomal metabolism of delavirdine: evidence for mechanism-based inactivation of human cytochrome P450 3A
Published in The Journal of pharmacology and experimental therapeutics (01-10-1998)“…Administration of delavirdine, an HIV-1 reverse transcriptase inhibitor, to rats or monkeys resulted in apparent loss of hepatic microsomal CYP3A and…”
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Discovery, Synthesis, and Bioactivity of Bis(heteroaryl)piperazines. 1. A Novel Class of Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors
Published in Journal of medicinal chemistry (01-04-1994)“…A variety of analogues of 1-[4-methoxy-3,5-dimethylbenzyl]-4-[3-(ethylamino)-2-pyridyl]piperazine hydrochloride (U-80493E) were synthesized and evaluated for…”
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Targeting Delavirdine/Atevirdine Resistant HIV-1: Identification of (Alkylamino)piperidine-Containing Bis(heteroaryl)piperazines as Broad Spectrum HIV-1 Reverse Transcriptase Inhibitors
Published in Journal of medicinal chemistry (13-09-1996)“…A novel class of bis(heteroaryl)piperazine (BHAP) analogs which possesses the ability to inhibit NNRTI (non-nucleoside reverse transcriptase inhibitor)…”
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Identification of Dioxin-Responsive Genes in Hep G2 Cells Using Differential mRNA Display RT–PCR
Published in Biochemical and biophysical research communications (27-03-1996)“…Differential mRNA display RT–PCR (DD RT–PCR) offers a tool to identify genes which are regulated or responsive to certain receptors or chemicals such as dioxin…”
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Absorption, Distribution, Metabolism, and Excretion of Atevirdine in the Rat
Published in Drug metabolism and disposition (01-10-1998)“…Atevirdine mesylate (U-87201E) is a highly specific nonnucleoside inhibitor of human immunodeficiency virus type 1 reverse transcriptase. The absorption,…”
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