Search Results - "BIALECKI, Russell"

Perspectives on using a multiplex human kidney safety biomarker panel to detect cisplatin-induced tubular toxicity in male and female Cynomolgus monkeys by Chen, Yafei, Dale Thurman, J., Kinter, Lewis B., Bialecki, Russell, Eric McDuffie, J.

“…Multiplex biomarker panel assays would enable early de-risking of discovery compound related kidney safety liabilities. The objective of this study was to…”
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The mitochondrial fission protein Drp1 in liver is required to mitigate NASH and prevents the activation of the mitochondrial ISR by Steffen, Janos, Ngo, Jennifer, Wang, Sheng-Ping, Williams, Kevin, Kramer, Henning F., Ho, George, Rodriguez, Carlos, Yekkala, Krishna, Amuzie, Chidozie, Bialecki, Russell, Norquay, Lisa, Nawrocki, Andrea R., Erion, Mark, Pocai, Alessandro, Shirihai, Orian S., Liesa, Marc

“…The mitochondrial fission protein Drp1 was proposed to promote NAFLD, as inhibition of hepatocyte Drp1 early in life prevents liver steatosis induced by…”
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CNS Adverse Effects: From Functional Observation Battery/Irwin Tests to Electrophysiology by Fonck, Carlos, Easter, Alison, Pietras, Mark R, Bialecki, Russell A

“…This chapter describes various approaches for the preclinical assessment of drug-induced central nervous system (CNS) adverse effects. Traditionally, methods…”
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Quantitative pharmacokinetic–pharmacodynamic modelling of baclofen‐mediated cardiovascular effects using BP and heart rate in rats by Kamendi, Harriet, Barthlow, Herbert, Lengel, David, Beaudoin, Marie‐Eve, Snow, Debra, Mettetal, Jerome T, Bialecki, Russell A

“…Background and Purpose While the molecular pathways of baclofen toxicity are understood, the relationships between baclofen‐mediated perturbation of individual…”
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Repeated exposure to low doses of kainic acid activates nuclear factor kappa B (NF-κB) prior to seizure in transgenic NF-κB/EGFP reporter mice by Miller, James A., Kirkley, Kelly A., Padmanabhan, Rachel, Liang, Li-Ping, Raol, Yogendra H., Patel, Manisha, Bialecki, Russell A., Tjalkens, Ronald B.

“…•Seizure liability of new candidate drugs is of primary concern in safety assessment.•The NF-kappaB signaling pathway is an important stress-response pathway…”
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Approaches to seizure risk assessment in preclinical drug discovery by Easter, Alison, Bell, M. Elizabeth, Damewood, James R., Redfern, William S., Valentin, Jean-Pierre, Winter, Matthew J., Fonck, Carlos, Bialecki, Russell A.

“…Assessment of seizure risk traditionally occurs late in the drug discovery process using low-throughput, resource intensive in vivo assays. Such approaches do…”
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Low-dose 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine causes inflammatory activation of astrocytes in nuclear factor-κB reporter mice prior to loss of dopaminergic neurons by Miller, James A., Trout, Briana R., Sullivan, Kelly A., Bialecki, Russell A., Roberts, Ruth A., Tjalkens, Ronald B.

“…Neuroinflammation is implicated in the progression of numerous disease states of the CNS, but early inflammatory signaling events in glial cells that may…”
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An integrative pharmacological approach to radio telemetry and blood sampling in pharmaceutical drug discovery and safety assessment by Litwin, Dennis C, Lengel, David J, Kamendi, Harriet W, Bialecki, Russell A

“…A successful integration of the automated blood sampling (ABS) and telemetry (ABST) system is described. The new ABST system facilitates concomitant collection…”
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A multi-site comparison of in vivo safety pharmacology studies conducted to support ICH S7A & B regulatory submissions by Ewart, Lorna, Milne, Aileen, Adkins, Debbie, Benjamin, Amanda, Bialecki, Russell, Chen, Yafei, Ericsson, Ann-Christin, Gardner, Stacey, Grant, Claire, Lengel, David, Lindgren, Silvana, Lowing, Sarah, Marks, Louise, Moors, Jackie, Oldman, Karen, Pietras, Mark, Prior, Helen, Punton, James, Redfern, Will S., Salmond, Ross, Skinner, Matt, Some, Margareta, Stanton, Andrea, Swedberg, Michael, Finch, John, Valentin, Jean-Pierre

“…Introduction: Parts A and B of the ICH S7 guidelines on safety pharmacology describe the in vivo studies that must be conducted prior to first time in man…”
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Combining radio telemetry and automated blood sampling: A novel approach for integrative pharmacology and toxicology studies by Kamendi, Harriet W., Brott, David A., Chen, Yafei, Litwin, Dennis C., Lengel, David J., Fonck, Carlos, Bui, Khanh H., Gorko, Mary Ann, Bialecki, Russell A.

“…A novel automated blood sampling and telemetry (ABST) system was developed to integrate pharmacokinetic (PK), pharmacodynamic (PD) and toxicology studies. The…”
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Design, Synthesis, and SAR of Tachykinin Antagonists:  Modulation of Balance in NK1/NK2 Receptor Antagonist Activity by Albert, Jeffrey S, Aharony, David, Andisik, Donald, Barthlow, Herbert, Bernstein, Peter R, Bialecki, Russell A, Dedinas, Robert, Dembofsky, Bruce T, Hill, Daniel, Kirkland, Karin, Koether, Gerard M, Kosmider, Benedict J, Ohnmacht, Cyrus, Palmer, William, Potts, William, Rumsey, William, Shen, Lihong, Shenvi, Ashok, Sherwood, Scott, Warwick, Paul J, Russell, Keith

“…Through optimization of compounds based on the dual NK1/NK2 antagonist ZD6021, it was found that alteration of two key regions could modulate the balance of…”
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Effects of M274773, a neurokinin-2 receptor antagonist, on bladder function in chronically spinalized rats by Abdel-Karim, Aly M, Barthlow, Herbert G, Bialecki, Russell A, Elhilali, Mostafa M

“…Increased afferent nerve activity may have an important role in the pathogenesis of neurogenic detrusor overactivity. We tested the efficacy of the neuokinin-2…”
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Effects of ZD6169 and ZD0947, 2 potassium adenosine triphosphate channel openers, on bladder function of spinalized rats by Abdel-Karim, Aly M, Bialecki, Russell A, Elhilali, Mostafa M

“…The use of K+ channel openers is emerging as an attractive possibility for treating bladder overactivity. We tested the efficacy of the 2 adenosine…”
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Discovery of novel, orally active dual NK1/NK2 antagonists by BERNSTEIN, Peter R, AHARONY, David, KOSMIDER, Benedict J, KIRKLAND, Karin, OHNMACHT, Cyrus J, POTTS, William, RUMSEY, William L, LIHONG SHEN, SHENVI, Ashok, SHERWOOD, Scott, STOLLMAN, David, RUSSELL, Keith, ALBERT, Jeffrey S, ANDISIK, Donald, BARTHLOW, Herbert G, BIALECKI, Russell, DAVENPORT, Timothy, DEDINAS, Robert F, DEMBOFSKY, Bruce T, KOETHER, Gerard

“…Exploration of the SAR around selective NK2 antagonists, SR48968 and ZD7944, led to the discovery that naphth-1-amide analogues provide potent dual NK1 and NK2…”
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The potential value of an in vitro hippocampal brain slice assay for the preclinical assessment of seizure liability of anti-infective drugs by Easter, Alison, Bialecki, Russell

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The discovery of non-basic atrial natriuretic peptide clearance receptor antagonists. part 1 by Veale, Chris A, Alford, Vernon C, Aharony, David, Banville, Debra L, Bialecki, Russell A, Brown, Frederick J, Damewood, James R, Dantzman, Cathy L, Edwards, Philip D, Jacobs, Robert T, Mauger, Russell C, Murphy, Megan M, Palmer, Willam E, Pine, Kara K, Rumsey, William L, Garcia-Davenport, Laura E, Shaw, Andrew, Steelman, Gary B, Surian, Jean M, Vacek, Edward P

“…The cyclic peptide ANP 4-23 and the linear peptide analogue AP-811 have been shown to be selective ANP-CR antagonists. Via alanine scanning and truncation…”
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A novel orally active endothelin-A receptor antagonist, ZD1611, prevents chronic hypoxia-induced pulmonary hypertension in the rat by Bialecki, R A, Stinson-Fisher, C, Murdoch, W, Bertelsen, D, Desiato, M, Rumsey, W

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Doxorubicin: Comparison between 3-h continuous and bolus intravenous administration paradigms on cardio-renal axis, mitochondrial sphingolipids and pathology by Kamendi, Harriet, Zhou, Ying, Crosby, Meredith, Keirstead, Natalie, Snow, Debra, Bentley, Patricia, Patel, Nilaben, Barthlow, Herbert, Luo, Wenli, Dragan, Yvonne, Bialecki, Russell

“…Doxorubicin (DOX) is a potent and effective broad-spectrum anthracycline antitumor agent, but its clinical usefulness is restricted by cardiotoxicity. This…”
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Chapter 5: Recent advances in pulmonary hypertension therapy by Bialecki, Russell A

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Comparison of neurobehavioral assessment outcomes between cynomolgus macaque and human using six reference drugs by Chen, Yafei, Liu, Yongzhen, Lengel, David, Barthlow, Herbert, Bialecki, Russell

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