Search Results - "LaPerle, Jennifer"
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A comprehensive non‐clinical evaluation of the CNS penetration potential of antimuscarinic agents for the treatment of overactive bladder
Published in British journal of clinical pharmacology (01-08-2011)“…WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT • This study provides antimuscarinic agents for overactive bladder (OAB) display variable association with side…”
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THE IMPACT OF P-GLYCOPROTEIN ON THE DISPOSITION OF DRUGS TARGETED FOR INDICATIONS OF THE CENTRAL NERVOUS SYSTEM: EVALUATION USING THE MDR1A/1B KNOCKOUT MOUSE MODEL
Published in Drug metabolism and disposition (01-01-2005)“…Thirty-two structurally diverse drugs used for the treatment of various conditions of the central nervous system (CNS), along with two active metabolites, and…”
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Defining the key pharmacophore elements of PF-04620110: Discovery of a potent, orally-active, neutral DGAT-1 inhibitor
Published in Bioorganic & medicinal chemistry (01-09-2013)“…DGAT-1 is an enzyme that catalyzes the final step in triglyceride synthesis. mRNA knockout experiments in rodent models suggest that inhibitors of this enzyme…”
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Pharmacological inhibition to examine the role of DGAT1 in dietary lipid absorption in rodents and humans
Published in American journal of physiology: Gastrointestinal and liver physiology (01-06-2013)“…Alterations in fat metabolism, in particular elevated plasma concentrations of free fatty acids and triglycerides (TG), have been implicated in the…”
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Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1
Published in ACS medicinal chemistry letters (12-05-2011)“…Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides. DGAT-1 knockout mice have been…”
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Design and synthesis of potent, orally-active DGAT-1 inhibitors containing a dioxino[2,3- d]pyrimidine core
Published in Bioorganic & medicinal chemistry letters (15-10-2011)“…A novel series of potent DGAT-1 inhibitors was developed originating from the lactam-based clinical candidate PF-04620110. Incorporation of a dioxino[2,3-…”
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Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment
Published in ACS medicinal chemistry letters (12-11-2015)“…Recent studies in adipose tissue, pancreas, muscle, and macrophages suggest that MAP4K4, a serine/threonine protein kinase may be a viable target for…”
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A comprehensive non-clinical evaluation of the CNS penetration potential of antimuscarinic agents for the treatment of overactive bladder : Clinical pharmacology of functional disorders of the urogenital system
Published in British journal of clinical pharmacology (2011)Get full text
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An Analytical Method for the Analysis of Tulathromycin, an Equilibrating Triamilide, in Bovine and Porcine Plasma and Lung
Published in Journal of agricultural and food chemistry (21-04-2004)“…Tulathromycin is a novel member of the triamilide class of antibiotics that was developed as a safe and effective single-dose treatment of bovine and porcine…”
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Impact of time-dependent inactivation on the estimation of enzyme kinetic parameters for midazolam
Published in Drug metabolism letters (01-01-2009)“…Enzyme kinetic parameters for midazolam were time-dependent in human liver microsomes, under initial velocity conditions. V(max) and K(m) decreased up to 3.7…”
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