Search Results - "Salata, Joseph J."

Novel, potent inhibitors of human Kv1.5 K+ channels and ultrarapidly activating delayed rectifier potassium current by Lagrutta, Armando, Wang, Jixin, Fermini, Bernard, Salata, Joseph J

“…We have identified a series of diphenyl phosphine oxide (DPO) compounds that are potent frequency-dependent inhibitors of cloned human Kv1.5 (hKv1.5) channels…”
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Functional and pharmacological properties of canine ERG potassium channels by Wang, Jixin, Della Penna, Kimberly, Wang, Hao, Karczewski, Jerzy, Connolly, Thomas M, Koblan, Kenneth S, Bennett, Paul B, Salata, Joseph J

“…We established HEK-293 cell lines that stably express functional canine ether-à-go-go-related gene (cERG) K(+) channels and examined their biophysical and…”
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Assessing use-dependent inhibition of the cardiac Na± current (INa) in the PatchXpress automated patch clamp by Penniman, Jacob R., Kim, David C., Salata, Joseph J., Imredy, John P.

“…The cardiac Na+ current (INa) underlies the rapid depolarization of the cardiac myocyte, and block of the current slows cardiac conduction and increases the…”
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Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel by Beshore, Douglas C., Liverton, Nigel J., McIntyre, Charles J., Claiborne, Christopher F., Libby, Brian, Culberson, J. Christopher, Salata, Joseph J., Regan, Christopher P., Lynch, Joseph J., Kiss, Laszlo, Spencer, Robert H., Kane, Stephanie A., White, Rebecca B., Yeh, Suzie, Hartman, George D., Dinsmore, Christopher J.

“…A series of triarylethanolamine inhibitors of the Kv1.5 potassium channel have been prepared and evaluated for their effects in vitro and in vivo. The…”
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Improved throughput of PatchXpress hERG assay using intracellular potassium fluoride by Zeng, Haoyu, Penniman, Jacob R, Kinose, Fumi, Kim, David, Trepakova, Elena S, Malik, Manish G, Dech, Spencer J, Balasubramanian, Bharathi, Salata, Joseph J

“…Blockade of the human ether-a-go-go-related gene (hERG) potassium channel, with a consequent possibility of QT prolongation and increased susceptibility to a…”
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MK-0448, a Specific Kv1.5 Inhibitor: Safety, Pharmacokinetics, and Pharmacodynamic Electrophysiology in Experimental Animal Models and Humans by Pavri, Behzad B, Greenberg, Howard E, Kraft, Walter K, Lazarus, Nicole, Lynch, Joseph J, Salata, Joseph J, Bilodeau, Mark T, Regan, Christopher P, Stump, Gary, Fan, Li, Mehta, Anish, Wagner, John A, Gutstein, David E, Bloomfield, Daniel

“…BACKGROUND—We evaluated the viability of IKur as a target for maintenance of sinus rhythm in patients with a history of atrial fibrillation through the testing…”
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Scientific review and recommendations on preclinical cardiovascular safety evaluation of biologics by Vargas, Hugo M., Bass, Alan S., Breidenbach, Alexander, Feldman, Hal S., Gintant, Gary A., Harmer, Alexander R., Heath, Bronagh, Hoffmann, Peter, Lagrutta, Armando, Leishman, Derek, McMahon, Nick, Mittelstadt, Scott, Polonchuk, Liudmila, Pugsley, Michael K., Salata, Joseph J., Valentin, Jean-Pierre

“…Biological therapeutic agents (biologicals), such as monoclonal antibodies (mAbs), are increasingly important in the treatment of human disease, and many types…”
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Saxitoxin is a gating modifier of HERG K+ channels by Wang, Jixin, Salata, Joseph J, Bennett, Paul B

“…Potassium (K+) channels mediate numerous electrical events in excitable cells, including cellular membrane potential repolarization. The hERG K+ channel plays…”
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The anesthetized guinea pig: An effective early cardiovascular derisking and lead optimization model by Morissette, Pierre, Nishida, Masahiro, Trepakova, Elena, Imredy, John, Lagrutta, Armando, Chaves, Alysia, Hoagland, Kimberly, Hoe, Chao-Min Lei, Zrada, Matthew M., Travis, Jeffrey J., Zingaro, Gloria J., Gerenser, Pamela, Friedrichs, Greg, Salata, Joseph J.

“…In recent years, the anesthetized guinea pig has been used increasingly to evaluate the cardiovascular effects of drug-candidate molecules during lead…”
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Halide ion effects on human Ether-à-go-go related gene potassium channel properties by Zeng, Haoyu, Balasubramanian, Bharathi, Penniman, Jacob R, Kinose, Fumi, Salata, Joseph J, Lagrutta, Armando

“…The human Ether-à-go-go related gene (hERG) potassium channel has been widely used to counter screen potential pharmaceuticals as a biomarker to predict…”
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The hERG channel and risk of drug-acquired cardiac arrhythmia: an overview by Lagrutta, Armando A, Trepakova, Elena S, Salata, Joseph J

“…This review summarizes current knowledge of the cardiac rapidly activating delayed rectifier potassium current (I(Kr)), and its connection to drug-acquired QT…”
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IV infusion rate affects pharmacokinetics and pharmacodynamic (QTc) response in pentobarbital-anesthetized guinea pigs by Nishida, Masahiro, Morissette, Pierre, Miyazaki, Hiroyasu, Salata, Joseph J.

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Modeling of the adrenergic response of the human IKs current (hKCNQ1/hKCNE1) stably expressed in HEK-293 cells by Imredy, John P, Penniman, Jacob R, Dech, Spencer J, Irving, Winston D, Salata, Joseph J

“…Stable coexpression of human (h)KCNQ1 and hKCNE1 in human embryonic kidney (HEK)-293 cells reconstitutes a nativelike slowly activating delayed rectifier K+…”
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A novel benzodiazepine that activates cardiac slow delayed rectifier K+ currents by Salata, J J, Jurkiewicz, N K, Wang, J, Evans, B E, Orme, H T, Sanguinetti, M C

“…The slowly activating delayed rectifier K+ current, IKs, is an important modulator of cardiac action potential repolarization. Here, we describe a novel…”
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Left ventricular hypertrophy decreases slowly but not rapidly activating delayed rectifier potassium currents of epicardial and endocardial myocytes in rabbits by XIAOPING XU, RIALS, Seth J, YING WU, SALATA, Joseph J, TENGXIAN LIU, BHARUCHA, David B, MARINCHAK, Roger A, KOWEY, Peter R

“…Delayed rectifier K(+) currents are critical to action potential (AP) repolarization. The present study examines the effects of left ventricular hypertrophy…”
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Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine by SALATA, J. J, JURKIEWICZ, N. K, WALLACE, A. A, STUPIENSKI, R. F, GUINOSSO, P. J, LYNCH, J. J

“…We compared the cardiac electrophysiological actions of two types of H1-receptor antagonists--the piperidines, astemizole and terfenadine, and the…”
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Flunarizine is a Highly Potent Inhibitor of Cardiac hERG Potassium Current by Trepakova, Elena S, Dech, Spencer J, Salata, Joseph J

“…Flunarizine has been widely used for the management of a variety of disorders such as peripheral vascular diseases, migraine, and epilepsy. The majority of its…”
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Application of PatchXpress planar patch clamp technology to the screening of new drug candidates for cardiac KCNQ1/KCNE1 (I Ks) activity by Trepakova, Elena S, Malik, Manish G, Imredy, John P, Penniman, Jacob R, Dech, Spencer J, Salata, Joseph J

“…A cardiac safety concern for QT prolongation and potential for pro-arrhythmia exists due to inhibition of the cardiac slowly activating delayed rectifier…”
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Class III Antiarrhythmic Activity in Vivo by Selective Blockade of the Slowly Activating Cardiac Delayed Rectifier Potassium Current I Ks by (R)-2-(2,4- Trifluoromethyl)-N-[2-oxo-5-phenyl- 1-(2,2,2-trifluoroethyl)-2,3-dihydro- 1H-benzo[e][1,4]diazepin-3-yl]acetamide by Selnick, Harold G, Liverton, Nigel J, Baldwin, John J, Butcher, John W, Claremon, David A, Elliott, Jason M, Freidinger, Roger M, King, Stella A, Libby, Brian E, McIntyre, Charles J, Pribush, David A, Remy, David C, Smith, Garry R, Tebben, Andrew J, Jurkiewicz, Nancy K, Lynch, Joseph J, Salata, Joseph J, Sanguinetti, Michael C, Siegl, Peter K. S, Slaughter, Donald E, Vyas, Kamlesh

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Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP by Coleman, Paul J., Schreier, John D., Cox, Christopher D., Fraley, Mark E., Garbaccio, Robert M., Buser, Carolyn A., Walsh, Eileen S., Hamilton, Kelly, Lobell, Robert B., Rickert, Keith, Tao, Weikang, Diehl, Ronald E., South, Vicki J., Davide, Joseph P., Kohl, Nancy E., Yan, Youwei, Kuo, Lawrence, Prueksaritanont, Thomayant, Li, Chunze, Mahan, Elizabeth A., Fernandez-Metzler, Carmen, Salata, Joseph J., Hartman, George D.

“…Dihydropyrazole amides such as 24 are potent inhibitors of KSP with favorable physical properties, pharmacokinetics, and in vivo potency. A diastereoselective…”
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