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Items: 46

1.

In Vitro-In Vivo Extrapolation of Intestinal Availability for Carboxylesterase Substrates Using Portal Vein-Cannulated Monkey.

Trapa PE, Beaumont K, Atkinson K, Eng H, King-Ahmad A, Scott DO, Maurer TS, Di L.

J Pharm Sci. 2017 Mar;106(3):898-905. doi: 10.1016/j.xphs.2016.12.001. Epub 2016 Dec 18.

PMID:
27998705
2.

Extended Clearance Classification System (ECCS) informed approach for evaluating investigational drugs as substrates of drug transporters.

Varma MV, El-Kattan AF, Feng B, Steyn SJ, Maurer TS, Scott DO, Rodrigues AD, Tremaine LM.

Clin Pharmacol Ther. 2017 Jul;102(1):33-36. doi: 10.1002/cpt.595. Epub 2017 Feb 3. No abstract available.

PMID:
27984654
3.

Passive drug permeation through membranes and cellular distribution.

Scott DO, Ghosh A, Di L, Maurer TS.

Pharmacol Res. 2017 Mar;117:94-102. doi: 10.1016/j.phrs.2016.11.028. Epub 2016 Nov 24. Review.

PMID:
27890815
4.

Projecting ADME Behavior and Drug-Drug Interactions in Early Discovery and Development: Application of the Extended Clearance Classification System.

El-Kattan AF, Varma MV, Steyn SJ, Scott DO, Maurer TS, Bergman A.

Pharm Res. 2016 Dec;33(12):3021-3030. Epub 2016 Sep 12.

PMID:
27620173
5.

Evaluation of a Mathematical Model of Rat Body Weight Regulation in Application to Caloric Restriction and Drug Treatment Studies.

Selimkhanov J, Thompson WC, Patterson TA, Hadcock JR, Scott DO, Maurer TS, Musante CJ.

PLoS One. 2016 May 26;11(5):e0155674. doi: 10.1371/journal.pone.0155674. eCollection 2016.

6.

Insights From an Integrated Physiologically Based Pharmacokinetic Model for Brain Penetration.

Trapa PE, Belova E, Liras JL, Scott DO, Steyn SJ.

J Pharm Sci. 2016 Feb;105(2):965-971. doi: 10.1016/j.xphs.2015.12.005.

PMID:
26869440
7.

Rapid Method To Determine Intracellular Drug Concentrations in Cellular Uptake Assays: Application to Metformin in Organic Cation Transporter 1-Transfected Human Embryonic Kidney 293 Cells.

Chien HC, Zur AA, Maurer TS, Yee SW, Tolsma J, Jasper P, Scott DO, Giacomini KM.

Drug Metab Dispos. 2016 Mar;44(3):356-64. doi: 10.1124/dmd.115.066647. Epub 2015 Dec 23.

8.

Toward a unified model of passive drug permeation II: the physiochemical determinants of unbound tissue distribution with applications to the design of hepatoselective glucokinase activators.

Ghosh A, Maurer TS, Litchfield J, Varma MV, Rotter C, Scialis R, Feng B, Tu M, Guimaraes CR, Scott DO.

Drug Metab Dispos. 2014 Oct;42(10):1599-610. doi: 10.1124/dmd.114.058032. Epub 2014 Jul 14.

PMID:
25024402
9.

Towards a unified model of passive drug permeation I: origins of the unstirred water layer with applications to ionic permeation.

Ghosh A, Scott DO, Maurer TS.

Eur J Pharm Sci. 2014 Feb 14;52:109-24. doi: 10.1016/j.ejps.2013.10.004. Epub 2013 Nov 7.

PMID:
24211511
10.

Mechanistic insights from comparing intrinsic clearance values between human liver microsomes and hepatocytes to guide drug design.

Di L, Keefer C, Scott DO, Strelevitz TJ, Chang G, Bi YA, Lai Y, Duckworth J, Fenner K, Troutman MD, Obach RS.

Eur J Med Chem. 2012 Nov;57:441-8. doi: 10.1016/j.ejmech.2012.06.043. Epub 2012 Jul 16.

PMID:
22840492
11.

Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents.

Dow RL, Carpino PA, Gautreau D, Hadcock JR, Iredale PA, Kelly-Sullivan D, Lizano JS, O'Connor RE, Schneider SR, Scott DO, Ward KM.

ACS Med Chem Lett. 2012 Mar 21;3(5):397-401. doi: 10.1021/ml3000325. eCollection 2012 May 10.

12.

Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists.

Cameron KO, Beretta EE, Chen Y, Chu-Moyer M, Fernando D, Gao H, Kohrt J, Lavergne S, Jardine Pda S, Guzman-Perez A, Hoth C, Perry DA, Hadcock JR, Gautreau D, Makowski M, Perez S, Polivkova J, Rogers L, Scott DO, Swick AG, Thiede L, Trebino CE, Trilles RV, Wilmowski J, Zhang Y.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2943-7. doi: 10.1016/j.bmcl.2012.02.049. Epub 2012 Feb 23.

PMID:
22424974
13.

Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.

Orr ST, Ripp SL, Ballard TE, Henderson JL, Scott DO, Obach RS, Sun H, Kalgutkar AS.

J Med Chem. 2012 Jun 14;55(11):4896-933. doi: 10.1021/jm300065h. Epub 2012 Mar 27. Review. No abstract available.

PMID:
22409598
14.

Impact of genetic polymorphisms of cytochrome P450 2 C (CYP2C) enzymes on the drug metabolism and design of antidiabetics.

Sun H, Scott DO.

Chem Biol Interact. 2011 Nov 15;194(2-3):159-67. doi: 10.1016/j.cbi.2011.08.011. Epub 2011 Sep 10. Review.

PMID:
21939641
16.

Excretion, metabolism, and pharmacokinetics of CP-945,598, a selective cannabinoid receptor antagonist, in rats, mice, and dogs.

Miao Z, Scott DO, Griffith DA, Day R, Prakash C.

Drug Metab Dispos. 2011 Dec;39(12):2191-208. doi: 10.1124/dmd.111.040360. Epub 2011 Aug 29.

PMID:
21875952
17.
18.

Species independence in brain tissue binding using brain homogenates.

Di L, Umland JP, Chang G, Huang Y, Lin Z, Scott DO, Troutman MD, Liston TE.

Drug Metab Dispos. 2011 Jul;39(7):1270-7. doi: 10.1124/dmd.111.038778. Epub 2011 Apr 7.

PMID:
21474681
19.

Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity.

Elliott RL, Cameron KO, Chin JE, Bartlett JA, Beretta EE, Chen Y, Jardine Pda S, Dubins JS, Gillaspy ML, Hargrove DM, Kalgutkar AS, LaFlamme JA, Lame ME, Martin KA, Maurer TS, Nardone NA, Oliver RM, Scott DO, Sun D, Swick AG, Trebino CE, Zhang Y.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6797-801. doi: 10.1016/j.bmcl.2010.08.115. Epub 2010 Sep 28.

PMID:
20851601
20.

Quantitative in vitro and in vivo pharmacological profile of CE-178253, a potent and selective cannabinoid type 1 (CB1) receptor antagonist.

Hadcock JR, Carpino PA, Iredale PA, Dow RL, Gautreau D, Thiede L, Kelly-Sullivan D, Lizano JS, Liu X, Van Deusen J, Ward KM, O'Connor RE, Black SC, Griffith DA, Scott DO.

BMC Pharmacol. 2010 Aug 16;10:9. doi: 10.1186/1471-2210-10-9.

21.

Strategic use of plasma and microsome binding to exploit in vitro clearance in early drug discovery.

Chang G, Steyn SJ, Umland JP, Scott DO.

ACS Med Chem Lett. 2010 Feb 3;1(2):50-3. doi: 10.1021/ml900012h. eCollection 2010 May 13.

22.

In vitro and in vivo pharmacology of CP-945,598, a potent and selective cannabinoid CB(1) receptor antagonist for the management of obesity.

Hadcock JR, Griffith DA, Iredale PA, Carpino PA, Dow RL, Black SC, O'Connor R, Gautreau D, Lizano JS, Ward K, Hargrove DM, Kelly-Sullivan D, Scott DO.

Biochem Biophys Res Commun. 2010 Apr 2;394(2):366-71. doi: 10.1016/j.bbrc.2010.03.015. Epub 2010 Mar 6.

PMID:
20211605
23.

Structure-based drug metabolism predictions for drug design.

Sun H, Scott DO.

Chem Biol Drug Des. 2010 Jan;75(1):3-17. doi: 10.1111/j.1747-0285.2009.00899.x. Epub 2009 Oct 28.

PMID:
19878193
24.

Bioisosteric replacement of the hydrazide pharmacophore of the cannabinoid-1 receptor antagonist SR141716A. Part I: potent, orally-active 1,4-disubstituted imidazoles.

Dow RL, Hadcock JR, Scott DO, Schneider SR, Paight ES, Iredale PA, Carpino PA, Griffith DA, Hammond M, Dasilva-Jardine P.

Bioorg Med Chem Lett. 2009 Sep 15;19(18):5351-4. doi: 10.1016/j.bmcl.2009.07.130. Epub 2009 Aug 6.

PMID:
19683918
25.

Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity.

Dow RL, Carpino PA, Hadcock JR, Black SC, Iredale PA, DaSilva-Jardine P, Schneider SR, Paight ES, Griffith DA, Scott DO, O'Connor RE, Nduaka CI.

J Med Chem. 2009 May 14;52(9):2652-5. doi: 10.1021/jm900255t.

PMID:
19351113
26.

Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist.

Griffith DA, Hadcock JR, Black SC, Iredale PA, Carpino PA, DaSilva-Jardine P, Day R, DiBrino J, Dow RL, Landis MS, O'Connor RE, Scott DO.

J Med Chem. 2009 Jan 22;52(2):234-7. doi: 10.1021/jm8012932.

PMID:
19102698
27.

In silico modeling of nonspecific binding to human liver microsomes.

Gao H, Yao L, Mathieu HW, Zhang Y, Maurer TS, Troutman MD, Scott DO, Ruggeri RB, Lin J.

Drug Metab Dispos. 2008 Oct;36(10):2130-5. doi: 10.1124/dmd.107.020131. Epub 2008 Jul 7.

PMID:
18606744
28.

A nonprostanoid EP4 receptor selective prostaglandin E2 agonist restores bone mass and strength in aged, ovariectomized rats.

Ke HZ, Crawford DT, Qi H, Simmons HA, Owen TA, Paralkar VM, Li M, Lu B, Grasser WA, Cameron KO, Lefker BA, DaSilva-Jardine P, Scott DO, Zhang Q, Tian XY, Jee WS, Brown TA, Thompson DD.

J Bone Miner Res. 2006 Apr;21(4):565-75. Epub 2006 Apr 5.

29.

Discovery of highly selective EP4 receptor agonists that stimulate new bone formation and restore bone mass in ovariectomized rats.

Cameron KO, Lefker BA, Chu-Moyer MY, Crawford DT, Jardine PD, DeNinno SL, Gilbert S, Grasser WA, Ke H, Lu B, Owen TA, Paralkar VM, Qi H, Scott DO, Thompson DD, Tjoa CM, Zawistoski MP.

Bioorg Med Chem Lett. 2006 Apr 1;16(7):1799-802. Epub 2006 Jan 26.

PMID:
16442794
30.

A new chemical tool for exploring the physiological function of the PDE2 isozyme.

Chambers RJ, Abrams K, Garceau NY, Kamath AV, Manley CM, Lilley SC, Otte DA, Scott DO, Sheils AL, Tess DA, Vellekoop AS, Zhang Y, Lam KT.

Bioorg Med Chem Lett. 2006 Jan 15;16(2):307-10. Epub 2005 Nov 3.

PMID:
16275071
31.

New bicyclic cannabinoid receptor-1 (CB1-R) antagonists.

Carpino PA, Griffith DA, Sakya S, Dow RL, Black SC, Hadcock JR, Iredale PA, Scott DO, Fichtner MW, Rose CR, Day R, Dibrino J, Butler M, Debartolo DB, Dutcher D, Gautreau D, Lizano JS, O'connor RE, Sands MA, Kelly-Sullivan D, Ward KM.

Bioorg Med Chem Lett. 2006 Feb;16(3):731-6. Epub 2005 Nov 2.

PMID:
16263283
32.

Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice.

Maurer TS, Debartolo DB, Tess DA, Scott DO.

Drug Metab Dispos. 2005 Jan;33(1):175-81. Epub 2004 Oct 22.

PMID:
15502010
33.

Comparison of in vitro BBMEC permeability and in vivo CNS uptake by microdialysis sampling.

Hansen DK, Scott DO, Otis KW, Lunte SM.

J Pharm Biomed Anal. 2002 Mar 1;27(6):945-58.

PMID:
11836058
34.

Evaluation of the BBMEC model for screening the CNS permeability of drugs.

Otis KW, Avery ML, Broward-Partin SM, Hansen DK, Behlow HW Jr, Scott DO, Thompson TN.

J Pharmacol Toxicol Methods. 2001 Jan-Feb;45(1):71-7. Review.

PMID:
11489667
36.
37.

Urinary and biliary disposition of the lactone and carboxylate forms of 20(S)-camptothecin in rats.

Scott DO, Bindra DS, Sutton SC, Stella VJ.

Drug Metab Dispos. 1994 May-Jun;22(3):438-42.

PMID:
8070321
38.

Plasma pharmacokinetics of lactone and carboxylate forms of 20(S)-camptothecin in anesthetized rats.

Scott DO, Bindra DS, Stella VJ.

Pharm Res. 1993 Oct;10(10):1451-7.

PMID:
8272406
39.
40.

Enzymatic formation and electrochemical characterization of multiply substituted glutathione conjugates of hydroquinone.

Puckett-Vaughn DL, Stenken JA, Scott DO, Lunte SM, Lunte CE.

Life Sci. 1993;52(14):1239-47.

PMID:
8450717
41.

Intravenous microdialysis sampling in awake, freely-moving rats.

Telting-Diaz M, Scott DO, Lunte CE.

Anal Chem. 1992 Apr 1;64(7):806-10.

PMID:
1524225
42.

In vivo microdialysis sampling for pharmacokinetic investigations.

Scott DO, Sorenson LR, Steele KL, Puckett DL, Lunte CE.

Pharm Res. 1991 Mar;8(3):389-92.

PMID:
2052531
43.

Microdialysis sampling for determination of plasma protein binding of drugs.

Herrera AM, Scott DO, Lunte CE.

Pharm Res. 1990 Oct;7(10):1077-81.

PMID:
2281040
44.

In vivo microdialysis sampling coupled to liquid chromatography for the study of acetaminophen metabolism.

Scott DO, Sorensen LR, Lunte CE.

J Chromatogr. 1990 May 11;506:461-9.

PMID:
2376606
46.

Microdialysis-perfusion sampling for the investigation of phenol metabolism.

Scott DO, Bell MA, Lunte CE.

J Pharm Biomed Anal. 1989;7(11):1249-59.

PMID:
2488171

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