Search Results - "NELSON, Frederick R"

Identification of a Brain Penetrant PDE9A Inhibitor Utilizing Prospective Design and Chemical Enablement as a Rapid Lead Optimization Strategy by Verhoest, Patrick R, Proulx-Lafrance, Caroline, Corman, Michael, Chenard, Lois, Helal, Christopher J, Hou, Xinjun, Kleiman, Robin, Liu, Shenping, Marr, Eric, Menniti, Frank S, Schmidt, Christopher J, Vanase-Frawley, Michelle, Schmidt, Anne W, Williams, Robert D, Nelson, Frederick R, Fonseca, Kari R, Liras, Spiros

“…By use of chemical enablement and prospective design, a novel series of selective, brain penetrant PDE9A inhibitors have been identified that are capable of…”
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The Effect of Breast Cancer Resistance Protein and P-Glycoprotein on the Brain Penetration of Flavopiridol, Imatinib Mesylate (Gleevec), Prazosin, and 2-Methoxy-3-(4-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)propanoic Acid (PF-407288) in Mice by Zhou, Lin, Schmidt, Kari, Nelson, Frederick R, Zelesky, Veronica, Troutman, Matthew D, Feng, Bo

“…The role of breast cancer resistance protein (Bcrp) and the combined activities of Bcrp and P-glycoprotein (P-gp, Mdr1a/1b) in limiting the brain penetration…”
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Evaluation of Cerebrospinal Fluid Concentration and Plasma Free Concentration As a Surrogate Measurement for Brain Free Concentration by XINGRONG LIU, SMITH, Bill J, HOSEA, Natilie, JIANHUA LIU, NELSON, Frederick R, SZEWC, Mark A, VAN DEUSEN, Jeffrey, CUIPING CHEN, CALLEGARI, Ernesto, BECKER, Stacey L, XI CHEN, CIANFROGNA, Julie, DORAN, Angela C, DORAN, Shawn D, GIBBS, John P

“…This study was designed to evaluate the use of cerebrospinal fluid (CSF) drug concentration and plasma unbound concentration ( C u,plasma ) to predict brain…”
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Use of a physiologically based pharmacokinetic model to study the time to reach brain equilibrium: an experimental analysis of the role of blood-brain barrier permeability, plasma protein binding, and brain tissue binding by Liu, Xingrong, Smith, Bill J, Chen, Cuiping, Callegari, Ernesto, Becker, Stacey L, Chen, Xi, Cianfrogna, Julie, Doran, Angela C, Doran, Shawn D, Gibbs, John P, Hosea, Natilie, Liu, Jianhua, Nelson, Frederick R, Szewc, Mark A, Van Deusen, Jeffery

“…This study was designed 1) to examine the effects of blood-brain barrier (BBB) permeability [quantified as permeability-surface area product (PS)], unbound…”
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Central Nervous System Pharmacokinetics of the Mdr1 P-Glycoprotein Substrate CP-615,003: Intersite Differences and Implications for Human Receptor Occupancy Projections from Cerebrospinal Fluid Exposures by VENKATAKRISHNAN, Karthik, TSENG, Elaine, NELSON, Frederick R, ROLLEMA, Hans, FRENCH, Jonathan L, KAPLAN, Irina V, HORNER, Weldon E, GIBBS, Megan A

“…The central nervous system (CNS) distribution and transport mechanisms of the investigational drug candidate CP-615,003 ( N…”
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In vitro stability and in vivo pharmacokinetics of the novel ketogenic ester, bis hexanoyl (R)-1,3-butanediol by Stubbs, Brianna J., Blade, Thanh, Mills, Scott, Thomas, Jennifer, Yufei, Xu, Nelson, Frederick R., Higley, Nancy, Nikiforov, Andrey I., Rhiner, Marisa O., Verdin, Eric, Newman, John C.

“…A novel ketone ester, bis hexanoyl (R)-1,3-butanediol (BH-BD), has been developed as a means to elevate blood ketones, for use as an energy substrate and a…”
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Modulating inhibitory response control through potentiation of GluN2D subunit-containing NMDA receptors by Callahan, Patrick M., Terry, Alvin V., Nelson, Frederick R., Volkmann, Robert A., Vinod, A.B., Zainuddin, Mohd, Menniti, Frank S.

“…NMDA receptors containing GluN2D subunits are expressed in the subthalamic nucleus and external globus pallidus, key nuclei of the indirect and hyperdirect…”
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Application of Structure-Based Drug Design and Parallel Chemistry to Identify Selective, Brain Penetrant, In Vivo Active Phosphodiesterase 9A Inhibitors by Claffey, Michelle M, Helal, Christopher J, Verhoest, Patrick R, Kang, Zhijun, Fors, Kristina S, Jung, Stanley, Zhong, Jiaying, Bundesmann, Mark W, Hou, Xinjun, Lui, Shenping, Kleiman, Robin J, Vanase-Frawley, Michelle, Schmidt, Anne W, Menniti, Frank, Schmidt, Christopher J, Hoffman, William E, Hajos, Mihaly, McDowell, Laura, O’Connor, Rebecca E, MacDougall-Murphy, Mary, Fonseca, Kari R, Becker, Stacey L, Nelson, Frederick R, Liras, Spiros

“…Phosphodiesterase 9A inhibitors have shown activity in preclinical models of cognition with potential application as novel therapies for treating Alzheimer’s…”
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Use of Structure-Based Design to Discover a Potent, Selective, In Vivo Active Phosphodiesterase 10A Inhibitor Lead Series for the Treatment of Schizophrenia by Helal, Christopher J, Kang, Zhijun, Hou, Xinjun, Pandit, Jayvardhan, Chappie, Thomas A, Humphrey, John M, Marr, Eric S, Fennell, Kimberly F, Chenard, Lois K, Fox, Carol, Schmidt, Christopher J, Williams, Robert D, Chapin, Douglas S, Siuciak, Judith, Lebel, Lorraine, Menniti, Frank, Cianfrogna, Julia, Fonseca, Kari R, Nelson, Frederick R, O’Connor, Rebecca, MacDougall, Mary, McDowell, Laura, Liras, Spiros

“…Utilizing structure-based virtual library design and scoring, a novel chimeric series of phosphodiesterase 10A (PDE10A) inhibitors was discovered by…”
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Peripheral elevation of IGF-1 fails to alter Aβ clearance in multiple in vivo models by Lanz, Thomas A., Salatto, Christopher T., Semproni, Anthony R., Marconi, Michael, Brown, Tracy M., Richter, Karl E.G., Schmidt, Kari, Nelson, Frederick R., Schachter, Joel B.

“…Increasing beta-amyloid (Aβ) clearance may alter the course of Alzheimer's disease progression and attenuate amyloid plaque pathology. Insulin-like growth…”
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β-secretase inhibitors for treatment of Alzheimer's disease by O'Neill, Brian T, Brodney, Michael A, Ambroise, Claude, Borzilleri, Kris, Coffman, Karen, Efremov, Ivan, Hajos-Korcsok, Eva, Helal, Christopher, Kauffman, Gregory, Lanyon, Lorraine, Liston, Dane, JianHua Liu, Lu, Yasong, Martinez-Alsina, Luis, Murray, John, Nelson, Frederick R, Noell, Stephen, Nolan, Charles, Oborski, Christine, Ogilvie, Kevin, Tuttle, Jamison, Vajdos, Felix, Withka, Jane

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Dendritic spine density deficits in the hippocampal CA1 region of young Tg2576 mice are ameliorated with the PDE9A inhibitor PF-04447943 by Kleiman, Robin J, Lanz, Thomas A, Finley, James E, Bove, Susan E, Majchrzak, Mark J, Becker, Stacey L, Carvajal-Gonzales, Santos, Kuhn, A. Max, Wood, Kathleen M, Mariga, Abigail, Nelson, Frederick R, Verhoest, Patrick R, Seymour, Patricia A, Stephenson, Diane T

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H3 receptor antagonism increases methylhistamine levels in the cerebrospinal fluid of dogs and healthy human volunteers by Soares, Holly, Wager, Travis T, Schmidt, Anne W, Sweeney, Francis J, McLellan, Thomas J, Nelson, Frederick R, Spracklin, Doug, Wang, Ellen Q, Faessel, Helene, Pinter, Garry W, Li, Xiaoxi, Chappell, Phillip B

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Discovery of Two Clinical Histamine H 3 Receptor Antagonists: trans - N -Ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans -3-Fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]- N -(2-methylpropyl)cyclobutanecarboxamide (PF-03654764) by Wager, Travis T., Pettersen, Betty A., Schmidt, Anne W., Spracklin, Douglas K., Mente, Scot, Butler, Todd W., Howard, Harry, Lettiere, Daniel J., Rubitski, David M., Wong, Diane F., Nedza, Frank M., Nelson, Frederick R., Rollema, Hans, Raggon, Jeffrey W., Aubrecht, Jiri, Freeman, Jody K., Marcek, John M., Cianfrogna, Julie, Cook, Karen W., James, Larry C., Chatman, Linda A., Iredale, Philip A., Banker, Michael J., Homiski, Michael L., Munzner, Jennifer B., Chandrasekaran, Rama Y.

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The Effect of Breast Cancer Resistance Protein and P-Glycoprotein on the Brain Penetration of Flavopiridol, Imatinib Mesylate (Gleevec), Prazosin, and 2-Methoxy-3-4-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)phenylpropanoic Acid (PF-407288) in Mice by LIN ZHOU, SCHMIDT, Kari, NELSON, Frederick R, ZELESKY, Veronica, TROUTMAN, Matthew D, BO FENG

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P3‐380: Dendritic spine density deficits in the hippocampal CA1 region of young Tg2576 mice are ameliorated with the PDE9A inhibitor PF‐04447943 by Kleiman, Robin J., Lanz, Thomas A., Finley, James E., Bove, Susan E., Majchrzak, Mark J., Becker, Stacey L., Carvajal-Gonzales, Santos, Kuhn, A. Max, Wood, Kathleen M., Mariga, Abigail, Nelson, Frederick R., Verhoest, Patrick R., Seymour, Patricia A., Stephenson, Diane T.

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P3‐282: β‐secretase inhibitors for treatment of Alzheimer's disease by O'Neill, Brian T., Brodney, Michael A., Ambroise, Claude, Borzilleri, Kris, Coffman, Karen, Efremov, Ivan, Hajos-Korcsok, Eva, Helal, Christopher, Kauffman, Gregory, Lanyon, Lorraine, Liston, Dane, JianHua Liu, Lu, Yasong, Martinez-Alsina, Luis, Murray, John, Nelson, Frederick R., Noell, Stephen, Nolan, Charles, Oborski, Christine, Ogilvie, Kevin, Tuttle, Jamison, Vajdos, Felix, Withka, Jane

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P1‐264: H 3 receptor antagonism increases methylhistamine levels in the cerebrospinal fluid of dogs and healthy human volunteers by Soares, Holly, Wager, Travis T., Schmidt, Anne W., Sweeney, Francis J., McLellan, Thomas J., Nelson, Frederick R., Spracklin, Doug, Wang, Ellen Q., Faessel, Helene, Pinter, Garry W., Li, Xiaoxi, Chappell, Phillip B.

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P1‐264: H3 receptor antagonism increases methylhistamine levels in the cerebrospinal fluid of dogs and healthy human volunteers by Soares, Holly, Wager, Travis T., Schmidt, Anne W., Sweeney, Francis J., McLellan, Thomas J., Nelson, Frederick R., Spracklin, Doug, Wang, Ellen Q., Faessel, Helene, Pinter, Garry W., Li, Xiaoxi, Chappell, Phillip B.

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Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764) by Wager, Travis T, Pettersen, Betty A, Schmidt, Anne W, Spracklin, Douglas K, Mente, Scot, Butler, Todd W, Howard, Harry, Lettiere, Daniel J, Rubitski, David M, Wong, Diane F, Nedza, Frank M, Nelson, Frederick R, Rollema, Hans, Raggon, Jeffrey W, Aubrecht, Jiri, Freeman, Jody K, Marcek, John M, Cianfrogna, Julie, Cook, Karen W, James, Larry C, Chatman, Linda A, Iredale, Philip A, Banker, Michael J, Homiski, Michael L, Munzner, Jennifer B, Chandrasekaran, Rama Y

“…The discovery of two histamine H(3) antagonist clinical candidates is disclosed. The pathway to identification of the two clinical candidates, 6 (PF-03654746)…”
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