Search Results - "VanAlstine, Melissa A"
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Syntheses of novel high affinity ligands for opioid receptors
Published in Bioorganic & medicinal chemistry letters (15-04-2009)“…High binding affinity [ K i values (μ) = 0.072–1.3 nM] to opioid receptors is seen in a novel series of 3-desoxy-3-carboxamido-4-hydroxymorphinans where the…”
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Syntheses and opioid receptor binding properties of carboxamido-substituted opioids
Published in Bioorganic & medicinal chemistry letters (2009)“…A series of 15 novel opioid derivatives were made where the prototypic phenolic-OH group of traditional opioids was replaced by a carboxamido (CONH 2) group. A…”
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Cytochrome P450 2C24: Expression, Tissue Distribution, High-Throughput Assay, and Pharmacological Inhibition
Published in Acta pharmaceutica Sinica. B (01-04-2012)“…Cytochrome P450 (CYP)-mediated epoxidation of arachidonic acid (AA) contributes to important biological functions, including the pain-relieving responses…”
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Effects of Acetylenic Epoxygenase Inhibitors on Recombinant Cytochrome P450s
Published in Drug metabolism and disposition (01-07-2011)“…Arachidonate epoxidation, which mediates important biological functions in several tissues, is catalyzed by specific cytochrome P450 (P450) enzymes. Two fatty…”
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Opioids activate brain analgesic circuits through cytochrome P450/epoxygenase signaling
Published in Nature neuroscience (01-03-2010)“…To assess the importance of brain cytochrome P450 (P450) activity in μ opioid analgesic action, we generated a mutant mouse with brain neuron-specific…”
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Insight into the Mechanism of the Pechmann Condensation Reaction Using NMR
Published in Journal of organic chemistry (18-09-2015)“…The mechanism of the Pechmann condensation is still controversial despite the technological and biochemical importance of coumarins. Here, we present NMR…”
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Redefining the structure–activity relationships of 2,6-methano-3-benzazocines. Part 8. High affinity ligands for opioid receptors in the picomolar Ki range: Oxygenated N-(2-[1,1′-biphenyl]-4-ylethyl) analogues of 8-CAC
Published in Bioorganic & medicinal chemistry letters (15-12-2012)“…N-[2-(4′-methoxy[1,1′-biphenyl]-4-yl)ethyl]-8-CAC (1) is a high affinity (Ki=0.084nM) ligand for the μ opioid receptor and served as the lead compound for this…”
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Redefining the structure–activity relationships of 2,6-methano-3-benzazocines. Part 9: Synthesis, characterization and molecular modeling of pyridinyl isosteres of N-BPE-8-CAC (1), a high affinity ligand for opioid receptors
Published in Bioorganic & medicinal chemistry letters (01-04-2013)“…Derivatives of the lead compound N-BPE-8-CAC (1) where each CH of the biphenyl group was individually replaced by N were prepared in hopes of identifying high…”
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Brain P450 epoxygenase activity is required for the antinociceptive effects of improgan, a nonopioid analgesic
Published in Pain (Amsterdam) (01-04-2011)“…The search for the mechanism of action of improgan (a nonopioid analgesic) led to the recent discovery of CC12, a compound that blocks improgan…”
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Redefining the structure–activity relationships of 2,6-methano-3-benzazocines. 5. Opioid receptor binding properties of N-((4′-phenyl)-phenethyl) analogues of 8-CAC
Published in Bioorganic & medicinal chemistry (01-12-2007)“…Novel analogues of 8-carboxamidocyclazocine have very high affinity for opioid receptors. A series of aryl-containing N-monosubstituted analogues of the lead…”
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Determining the IC50 Values for Vorozole and Letrozole, on a Series of Human Liver Cytochrome P450s, to Help Determine the Binding Site of Vorozole in the Liver
Published in Enzyme research (2015)“…Vorozole and letrozole are third-generation aromatase (cytochrome P450 19A1) inhibitors. [11C]-Vorozole can be used as a radiotracer for aromatase in living…”
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Determining the IC 50 Values for Vorozole and Letrozole, on a Series of Human Liver Cytochrome P450s, to Help Determine the Binding Site of Vorozole in the Liver
Published in Enzyme research (2015)“…Vorozole and letrozole are third-generation aromatase (cytochrome P450 19A1) inhibitors. [(11)C]-Vorozole can be used as a radiotracer for aromatase in living…”
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Structure‐activity relationships of fragment‐based inhibitors of Trichomonas vaginalis adenosine/guanosine preferring nucleoside ribohydrolase
Published in The FASEB journal (01-04-2019)“…Trichomoniasis is a sexually transmitted infection caused by the parasite, Trichomonas vaginalis. Infections are currently treated with 5‐nitroimidazole drugs,…”
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Brain P450 Epoxygenase Activity is Required for the Antinociceptive Effects of Improgan, a Non-Opioid Analgesic
Published in Pain (Amsterdam) (01-04-2011)“…The search for the mechanism of action of improgan (a non-opioid analgesic) led to the recent discovery of CC12, a compound which blocks improgan…”
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Determining the [IC.sub.50] values for vorozole and letrozole, on a series of human liver cytochrome P450s, to help determine the binding site of vorozole in the liver
Published in Enzyme research (01-01-2015)“…Vorozole and letrozole are third-generation aromatase (cytochrome P450 19A1) inhibitors. [[sup.11]C]-Vorozole can be used as a radiotracer for aromatase in…”
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