Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Brian, Gemzik"'
Autor:
Yang Wu, Dieter M. Drexler, Joseph B. Santella, Thomas Brodie, Janet DiPiero, Stefan Ruepp, Umesh Hanumegowda, Brian Gemzik, Ching-Chiang Su, Evan B. Janovitz, Randy White, Michael J. Hageman, Julie Carman, John Hynes, Duohai Pan, John R. Megill
Publikováno v:
Journal of Pharmacological and Toxicological Methods. 96:1-8
Introduction Low intrinsic solubility leading to poor oral bioavailability is a common challenge in drug discovery that can often be overcome by formulation strategies, however, it remains a potential limitation that can pose challenges for early ris
Autor:
Jeffrey A. Robl, Michael Thomas, Mary Ann Pelleymounter, Brian Gemzik, Anthony V. Azzara, Brian J. Murphy, Sharon N. Bisaha, Helen E. Godonis, Daniel Longhi, Neil Flynn, William N. Washburn, Kenneth W. Rohrbach, Khehyong Ngu, Saleem Ahmad, Susan Harvey, Christine Huang, Evan B. Janovitz, Andres S. Hernandez, James Devenny, Hongwei Zhang, Lisa Zhang, Susan Glick, Suzanne Rooney, Wei Wang
Publikováno v:
Journal of Medicinal Chemistry. 59:8848-8858
The potent MCHR1 in vitro and in vivo antagonist activity of a series of cyclic tertiary alcohols derived from compound 2b is described. Subsequent pharmacokinetic and pharmacodynamic studies identified BMS-814580 (compound 10) as a highly efficaciou
Autor:
Jeffrey A. Robl, Guohua Zhao, Joel C. Barrish, Bei Wang, Brad D. Maxwell, Christian Caporuscio, Hongwei Zhang, James Devenny, Mary F. Grubb, Zhenghua Wang, Suzanne Rooney, James Mignone, Lisa Zhang, Brian J. Murphy, Wei Wang, Daniel Longhi, William N. Washburn, Kenneth W. Rohrbach, Evan B. Janovitz, Mark C. Manfredi, Mary Ann Pelleymounter, Michael Thomas, Hong Yang, Paul Stetsko, Saleem Ahmad, Atsu Apedo, Mary Jane Cullen, Brian Gemzik, Ning Huang, Chris Freeden, Susan Harvey, Anthony V. Azzara, Khehyong Ngu, Christine Huang, Rulin Zhao, Susan Glick, Neil Flynn, Pratik Devasthale, Andres S. Hernandez, Helen E. Godonis
Publikováno v:
Journal of Medicinal Chemistry. 57:7509-7522
Identification of MCHR1 antagonists with a preclinical safety profile to support clinical evaluation as antiobesity agents has been a challenge. Our finding that a basic moiety is not required for MCHR1 antagonists to achieve high affinity allowed us
Autor:
Monicah A. Otieno, Evan B. Janovitz, Yimer Callejas, Lois D. Lehman-McKeeman, William B. Foster, Vasanthi Bhaskaran, William N. Washburn, John R. Megill, Brian Gemzik
Publikováno v:
Toxicological sciences : an official journal of the Society of Toxicology. 155(2)
The objective of this work was to investigate the mechanisms of hepatobiliary toxicity caused by thienopyrimidone MCHR1 antagonists using BMS-773174 as a tool molecule. Co-administration of the pan CYP inhibitor 1-aminobenzotriazole with BMS-773174 p
Autor:
Saleem, Ahmad, William N, Washburn, Andres S, Hernandez, Sharon, Bisaha, Khehyong, Ngu, Wei, Wang, Mary Ann, Pelleymounter, Daniel, Longhi, Neil, Flynn, Anthony V, Azzara, Kenneth, Rohrbach, James, Devenny, Suzanne, Rooney, Michael, Thomas, Susan, Glick, Helen, Godonis, Susan, Harvey, Hongwei, Zhang, Brian, Gemzik, Evan B, Janovitz, Christine, Huang, Lisa, Zhang, Jeffrey A, Robl, Brian J, Murphy
Publikováno v:
Journal of medicinal chemistry. 59(19)
The potent MCHR1 in vitro and in vivo antagonist activity of a series of cyclic tertiary alcohols derived from compound 2b is described. Subsequent pharmacokinetic and pharmacodynamic studies identified BMS-814580 (compound 10) as a highly efficaciou
Autor:
Brian Gemzik, Matthew Z. Dieter, Linda Watson, David M. Nelson, Harvey Wong, Lois D. Lehman-McKeeman, Curtis D. Klaassen, Lloyd Lecureux
Publikováno v:
Toxicological Sciences. 108:482-491
The hepatobiliary disposition of thyroxine (T4) was evaluated in Groningen Yellow transport deficient (TR(-)) rats lacking functional multidrug resistance-associated protein 2 (Mrp2; Abcc2). Male Wistar and TR(-) rats were dosed orally (4 days) with
Autor:
Christian Trendelenburg, Sian Ratcliffe, Laszlo Urban, Brian Gemzik, Andreas Hartmann, Donna Dambach, Patrick Y. Muller
Publikováno v:
Drug discovery today. 20(9)
Treatment-related suicidal ideation and behavior (SIB) adverse events are under increasing public, legal and regulatory scrutiny. Prospective assessment of SIB is emerging as a challenging safety requirement by health authorities for the development
Autor:
I.P. Chaudhary, A. Parkinson, Larry W. Robertson, Brian Gemzik, Robert A. Blouin, Abhik Bandyopadhyay
Publikováno v:
Archives of Biochemistry and Biophysics. 307:386-390
The present study determined the effect of genetic obesity and phenobarbital (PB) treatment on the expression and regulation of the hepatic cytochrome P450 enzyme (CYP2CL1) in Fa/? and fa/fa Zucker rats. Hepatic CYP2C1 1 levels as determined by Weste
Autor:
Larry W. Robertson, Inder Chaudhary, Brian Gemzik, Abhik Bandyopadhyay, Robert A. Blouin, Andrew Parkinson
Publikováno v:
Archives of Biochemistry and Biophysics. 303:313-320
The present study describes the mechanism of the dampened induction of the CYP2B1 and CYP2B2 genes following phenobarbital treatment in the phenotypically obese fa/fa Zucker rat. The fa/fa Zucker rat demonstrated a threefold lower level of CYP2B1/2B2
Publikováno v:
Pharmaceutical Sciences Encyclopedia
Accurate determination of therapeutic indices from nonclinical studies across multiple species provides an invaluable tool for advancing compounds with reduced potential for harm and reduced likelihood of attrition for safety concerns. The robustness
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59d3e2f9bc455d98914ab23eb7020c7a
https://doi.org/10.1002/9780470571224.pse281
https://doi.org/10.1002/9780470571224.pse281