Search Results - "Daniels, J Scott"

Metabolism and Distribution of Clozapine-N-oxide: Implications for Nonhuman Primate Chemogenetics by Raper, Jessica, Morrison, Ryan D, Daniels, J. Scott, Howell, Leonard, Bachevalier, Jocelyne, Wichmann, Thomas, Galvan, Adriana

“…The use of Designer Receptors Exclusively Activated by Designer Drugs (DREADDs) in neuroscience has rapidly expanded in rodent studies but has lagged behind in…”
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Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: Development of a highly selective and more potent in vitro probe by Delpire, Eric, Baranczak, Aleksandra, Waterson, Alex G., Kim, Kwangho, Kett, Nathan, Morrison, Ryan D., Scott Daniels, J., David Weaver, C., Lindsley, Craig W.

“…Further chemical optimization of the MLSCN/MLPCN probe ML077 (KCC2 IC50=537nM) proved to be challenging as the effort was characterized by steep SAR. However,…”
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Allosteric activation of M₄ muscarinic receptors improve behavioral and physiological alterations in early symptomatic YAC128 mice by Pancani, Tristano, Foster, Daniel J., Moehle, Mark S., Bichell, Terry Jo, Bradley, Emma, Bridges, Thomas M., Klar, Rebecca, Poslusney, Mike, Rook, Jerri M., Daniels, J. Scott, Niswender, Colleen M., Jones, Carrie K., Wood, Michael R., Bowman, Aaron B., Lindsley, Craig W., Xiang, Zixiu, Conn, P. Jeffrey

“…Mutations that lead to Huntington’s disease (HD) result in increased transmission at glutamatergic corticostriatal synapses at early presymptomatic stages that…”
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A novel in vitro allometric scaling methodology for aldehyde oxidase substrates to enable selection of appropriate species for traditional allometry by Crouch, Rachel D., Hutzler, J. Matthew, Daniels, J. Scott

“…1. Failure to predict human pharmacokinetics of aldehyde oxidase (AO) substrates using traditional allometry has been attributed to species differences in AO…”
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ML297 (VU0456810), the First Potent and Selective Activator of the GIRK Potassium Channel, Displays Antiepileptic Properties in Mice by Kaufmann, Kristian, Romaine, Ian, Days, Emily, Pascual, Conrado, Malik, Adam, Yang, Liya, Zou, Bende, Du, Yu, Sliwoski, Greg, Morrison, Ryan D, Denton, Jerod, Niswender, Colleen M, Daniels, J. Scott, Sulikowski, Gary A, Xie, Xinmin (Simon), Lindsley, Craig W, Weaver, C. David

“…The G-protein activated, inward-rectifying potassium (K+) channels, “GIRKs”, are a family of ion channels (Kir3.1-Kir3.4) that has been the focus of intense…”
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Medication adherence, medical record accuracy, and medication exposure in real-world patients using comprehensive medication monitoring by Ryan, Timothy P, Morrison, Ryan D, Sutherland, Jeffrey J, Milne, Stephen B, Ryan, Kendall A, Daniels, J Scott, Misra-Hebert, Anita, Hicks, J Kevin, Vogan, Eric, Teng, Kathryn, Daly, Thomas M

“…Poor adherence to medication regimens and medical record inconsistencies result in incomplete knowledge of medication therapy in polypharmacy patients. By…”
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Malondialdehyde, a Product of Lipid Peroxidation, Is Mutagenic in Human Cells by Niedernhofer, Laura J., Daniels, J.Scott, Rouzer, Carol A., Greene, Rachel E., Marnett, Lawrence J.

“…Malondialdehyde (MDA) is an endogenous genotoxic product of enzymatic and oxygen radical-induced lipid peroxidation whose adducts are known to exist in DNA…”
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Selective Activation of M4 Muscarinic Acetylcholine Receptors Reverses MK-801-Induced Behavioral Impairments and Enhances Associative Learning in Rodents by Bubser, Michael, Bridges, Thomas M, Dencker, Ditte, Gould, Robert W, Grannan, Michael, Noetzel, Meredith J, Lamsal, Atin, Niswender, Colleen M, Daniels, J. Scott, Poslusney, Michael S, Melancon, Bruce J, Tarr, James C, Byers, Frank W, Wess, Jürgen, Duggan, Mark E, Dunlop, John, Wood, Michael W, Brandon, Nicholas J, Wood, Michael R, Lindsley, Craig W, Conn, P. Jeffrey, Jones, Carrie K

“…Positive allosteric modulators (PAMs) of the M4 muscarinic acetylcholine receptor (mAChR) represent a novel approach for the treatment of psychotic symptoms…”
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Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor by Salovich, James M., Vinson, Paige N., Sheffler, Douglas J., Lamsal, Atin, Utley, Thomas J., Blobaum, Anna L., Bridges, Thomas M., Le, Uyen, Jones, Carrie K., Wood, Michael R., Scott Daniels, J., Jeffrey Conn, P., Niswender, Colleen M., Lindsley, Craig W., Hopkins, Corey R.

“…Herein we describe the discovery and development of a novel class of M4 positive allosteric modulators, culminating in the discovery of ML293. ML293 exhibited…”
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Design, Synthesis, and Biological Evaluation of Halogenated N-(2-(4-Oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: Discovery of an Isoform-Selective Small Molecule Phospholipase D2 Inhibitor by Lavieri, Robert R, Scott, Sarah A, Selvy, Paige E, Kim, Kwangho, Jadhav, Satyawan, Morrison, Ryan D, Daniels, J. Scott, Brown, H. Alex, Lindsley, Craig W

“…Phospholipase D (PLD) catalyzes the conversion of phosphatidylcholine to the lipid second messenger phosphatidic acid. Two mammalian isoforms of PLD have been…”
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Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5 by Felts, Andrew S., Bollinger, Katrina A., Brassard, Christopher J., Rodriguez, Alice L., Morrison, Ryan D., Scott Daniels, J., Blobaum, Anna L., Niswender, Colleen M., Jones, Carrie K., Jeffrey Conn, P., Emmitte, Kyle A., Lindsley, Craig W.

“…[Display omitted] •Identification of the minimum pharmacophore of auglurant.•Development of novel saturated ethers that enhanced sp3 character.•Ether head…”
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Design of 4‑Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2 by Felts, Andrew S, Rodriguez, Alice L, Smith, Katrina A, Engers, Julie L, Morrison, Ryan D, Byers, Frank W, Blobaum, Anna L, Locuson, Charles W, Chang, Sichen, Venable, Daryl F, Niswender, Colleen M, Daniels, J. Scott, Conn, P. Jeffrey, Lindsley, Craig W, Emmitte, Kyle A

“…Both orthosteric and allosteric antagonists of the group II metabotropic glutamate receptors (mGlus) have been used to establish a link between mGlu2/3…”
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Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354 by Wen, Wandong, Young, Summer E., Duvernay, Matthew T., Schulte, Michael L., Nance, Kellie D., Melancon, Bruce J., Engers, Julie, Locuson, Charles W., Wood, Michael R., Daniels, J. Scott, Wu, Wenjun, Lindsley, Craig W., Hamm, Heidi E., Stauffer, Shaun R.

“…Herein we report the discovery and SAR of an indole-based protease activated receptor-4 (PAR-4) antagonist scaffold derived from a similarity search of the…”
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Development of a highly selective, orally bioavailable and CNS penetrant M₁ agonist derived from the MLPCN probe ML071 by Lebois, Evan P, Digby, Gregory J, Sheffler, Douglas J, Melancon, Bruce J, Tarr, James C, Cho, Hyekyung P, Miller, Nicole R, Morrison, Ryan, Bridges, Thomas M, Xiang, Zixiu, Scott Daniels, J, Wood, Michael R, Conn, P. Jeffrey, Lindsley, Craig W

“…Herein we report the discovery and SAR of a novel series of M₁ agonists based on the MLPCN probe, ML071. From this, VU0364572 emerged as a potent, orally…”
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State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 – Relation to antipsychotic-like drug effects by Gould, Robert W., Nedelcovych, Michael T., Gong, Xuewen, Tsai, Erica, Bubser, Michael, Bridges, Thomas M., Wood, Michael R., Duggan, Mark E., Brandon, Nicholas J., Dunlop, John, Wood, Michael W., Ivarsson, Magnus, Noetzel, Meredith J., Daniels, J. Scott, Niswender, Colleen M., Lindsley, Craig W., Conn, P. Jeffrey, Jones, Carrie K.

“…Accumulating evidence indicates direct relationships between sleep abnormalities and the severity and prevalence of other symptom clusters in schizophrenia…”
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HUMAN METABOLISM OF THE PROTEASOME INHIBITOR BORTEZOMIB: IDENTIFICATION OF CIRCULATING METABOLITES by PEKOL, Teresa, DANIELS, J. Scott, LABUTTI, Jason, PARSONS, Ian, NIX, Darrell, BARONAS, Elizabeth, HSIEH, Frank, GAN, Liang-Shang, MIWA, Gerald

“…Bortezomib [ N -(2,3-pyrazine)carbonyl- l -phenylalanine- l -leucine boronic acid] is a potent first-in-class dipeptidyl boronic acid proteasome inhibitor that…”
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First-in-human study assessing safety, tolerability, and pharmacokinetics of 2-hydroxybenzylamine acetate, a selective dicarbonyl electrophile scavenger, in healthy volunteers by Pitchford, Lisa M, Rathmacher, John A, Fuller, Jr, John C, Daniels, J Scott, Morrison, Ryan D, Akers, Wendall S, Abumrad, Naji N, Amarnath, Venkataraman, Currey, Patricia M, Roberts, L Jackson, Oates, John A, Boutaud, Olivier

“…2-Hydroxybenzylamine (2-HOBA) is a selective scavenger of dicarbonyl electrophiles that protects proteins and lipids from being modified by these…”
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Discovery and SAR of a novel series of non-MPEP site mGlu5 PAMs based on an aryl glycine sulfonamide scaffold by Rodriguez, Alice L., Zhou, Ya, Williams, Richard, David Weaver, C., Vinson, Paige N., Dawson, Eric S., Steckler, Thomas, Lavreysen, Hilde, Mackie, Claire, Bartolomé, José M., Macdonald, Gregor J., Scott Daniels, J., Niswender, Colleen M., Jones, Carrie K., Jeffrey Conn, P., Lindsley, Craig W., Stauffer, Shaun R.

“…Herein we report the discovery and SAR of a novel series of non-MPEP site metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs) based…”
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The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5 by Morrison, Ryan D, Blobaum, Anna L, Byers, Frank W, Santomango, Tammy S, Bridges, Thomas M, Stec, Donald, Brewer, Katrina A, Sanchez-Ponce, Raymundo, Corlew, Melany M, Rush, Roger, Felts, Andrew S, Manka, Jason, Bates, Brittney S, Venable, Daryl F, Rodriguez, Alice L, Jones, Carrie K, Niswender, Colleen M, Conn, P Jeffrey, Lindsley, Craig W, Emmitte, Kyle A, Daniels, J Scott

“…Negative allosteric modulation (NAM) of metabotropic glutamate receptor subtype 5 (mGlu₅) represents a therapeutic strategy for the treatment of childhood…”
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Use of a novel rapid and resource‐efficient cassette dosing approach to determine the pharmacokinetics and CNS distribution of small molecule 7‐transmembrane receptor allosteric modulators in rat by Bridges, Thomas. M., Morrison, Ryan D., Byers, Frank W., Luo, Shuanghui, Scott Daniels, J.

“…Approaches to efficiently and accurately define the pharmacokinetics (PK) of large sets of small molecules in rodents have been previously described. Likewise,…”
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