Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 18

1.

A Decade in the MIST: Learnings from Investigations of Drug Metabolites in Drug Development under the "Metabolites in Safety Testing" Regulatory Guidance.

Schadt S, Bister B, Chowdhury SK, Funk C, Hop CECA, Humphreys WG, Igarashi F, James AD, Kagan M, Khojasteh SC, Nedderman ANR, Prakash C, Runge F, Scheible H, Spracklin DK, Swart P, Tse S, Yuan J, Obach RS.

Drug Metab Dispos. 2018 Jun;46(6):865-878. doi: 10.1124/dmd.117.079848. Epub 2018 Feb 27. Review.

PMID:
29487142
2.

Quantitative projection of human brain penetration of the H3 antagonist PF-03654746 by integrating rat-derived brain partitioning and PET receptor occupancy.

Sawant-Basak A, Chen L, Shaffer CL, Palumbo D, Schmidt A, Tseng E, Spracklin DK, Gallezot JD, Labaree D, Nabulsi N, Huang Y, Carson RE, McCarthy T.

Xenobiotica. 2017 Feb;47(2):119-126. doi: 10.3109/00498254.2016.1166531. Epub 2016 Jun 29.

PMID:
27353353
3.

Biosynthesis of drug metabolites and quantitation using NMR spectroscopy for use in pharmacologic and drug metabolism studies.

Walker GS, Bauman JN, Ryder TF, Smith EB, Spracklin DK, Obach RS.

Drug Metab Dispos. 2014 Oct;42(10):1627-39. doi: 10.1124/dmd.114.059204. Epub 2014 Jul 22.

PMID:
25053618
4.

Deuterium isotope effects on drug pharmacokinetics. I. System-dependent effects of specific deuteration with aldehyde oxidase cleared drugs.

Sharma R, Strelevitz TJ, Gao H, Clark AJ, Schildknegt K, Obach RS, Ripp SL, Spracklin DK, Tremaine LM, Vaz AD.

Drug Metab Dispos. 2012 Mar;40(3):625-34. doi: 10.1124/dmd.111.042770. Epub 2011 Dec 21.

PMID:
22190693
5.

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).

Wager TT, Pettersen BA, Schmidt AW, Spracklin DK, Mente S, Butler TW, Howard H, Lettiere DJ, Rubitski DM, Wong DF, Nedza FM, Nelson FR, Rollema H, Raggon JW, Aubrecht J, Freeman JK, Marcek JM, Cianfrogna J, Cook KW, James LC, Chatman LA, Iredale PA, Banker MJ, Homiski ML, Munzner JB, Chandrasekaran RY.

J Med Chem. 2011 Nov 10;54(21):7602-20. doi: 10.1021/jm200939b. Epub 2011 Oct 7.

PMID:
21928839
6.

Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models.

O'Donnell CJ, Rogers BN, Bronk BS, Bryce DK, Coe JW, Cook KK, Duplantier AJ, Evrard E, Hajós M, Hoffmann WE, Hurst RS, Maklad N, Mather RJ, McLean S, Nedza FM, O'Neill BT, Peng L, Qian W, Rottas MM, Sands SB, Schmidt AW, Shrikhande AV, Spracklin DK, Wong DF, Zhang A, Zhang L.

J Med Chem. 2010 Feb 11;53(3):1222-37. doi: 10.1021/jm9015075.

PMID:
20043678
7.

Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.

O'Donnell CJ, Peng L, O'Neill BT, Arnold EP, Mather RJ, Sands SB, Shrikhande A, Lebel LA, Spracklin DK, Nedza FM.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4747-51. doi: 10.1016/j.bmcl.2009.06.059. Epub 2009 Jun 17.

PMID:
19576766
8.

3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization.

Duplantier AJ, Efremov I, Candler J, Doran AC, Ganong AH, Haas JA, Hanks AN, Kraus KG, Lazzaro JT Jr, Lu J, Maklad N, McCarthy SA, O'Sullivan TJ, Rogers BN, Siuciak JA, Spracklin DK, Zhang L.

Bioorg Med Chem Lett. 2009 May 1;19(9):2524-9. doi: 10.1016/j.bmcl.2009.03.032. Epub 2009 Mar 14.

PMID:
19328692
9.

Differential effects of various typical and atypical antipsychotics on plasma glucose and insulin levels in the mouse: evidence for the involvement of sympathetic regulation.

Savoy YE, Ashton MA, Miller MW, Nedza FM, Spracklin DK, Hawthorn MH, Rollema H, Matos FF, Hajos-Korcsok E.

Schizophr Bull. 2010 Mar;36(2):410-8. doi: 10.1093/schbul/sbn104. Epub 2008 Aug 14.

10.

Concentration-dependent modulation of amyloid-beta in vivo and in vitro using the gamma-secretase inhibitor, LY-450139.

Lanz TA, Karmilowicz MJ, Wood KM, Pozdnyakov N, Du P, Piotrowski MA, Brown TM, Nolan CE, Richter KE, Finley JE, Fei Q, Ebbinghaus CF, Chen YL, Spracklin DK, Tate B, Geoghegan KF, Lau LF, Auperin DD, Schachter JB.

J Pharmacol Exp Ther. 2006 Nov;319(2):924-33. Epub 2006 Aug 18.

PMID:
16920992
11.

The role of muscarinic receptor antagonism in antipsychotic-induced hippocampal acetylcholine release.

Johnson DE, Nedza FM, Spracklin DK, Ward KM, Schmidt AW, Iredale PA, Godek DM, Rollema H.

Eur J Pharmacol. 2005 Jan 4;506(3):209-19. Epub 2004 Dec 15.

PMID:
15627430
12.

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.

Doran A, Obach RS, Smith BJ, Hosea NA, Becker S, Callegari E, Chen C, Chen X, Choo E, Cianfrogna J, Cox LM, Gibbs JP, Gibbs MA, Hatch H, Hop CE, Kasman IN, Laperle J, Liu J, Liu X, Logman M, Maclin D, Nedza FM, Nelson F, Olson E, Rahematpura S, Raunig D, Rogers S, Schmidt K, Spracklin DK, Szewc M, Troutman M, Tseng E, Tu M, Van Deusen JW, Venkatakrishnan K, Walens G, Wang EQ, Wong D, Yasgar AS, Zhang C.

Drug Metab Dispos. 2005 Jan;33(1):165-74. Epub 2004 Oct 22.

PMID:
15502009
13.

Concordance between trifluoroacetic acid and hepatic protein trifluoroacetylation after disulfiram inhibition of halothane metabolism in rats.

Spracklin DK, Emery ME, Thummel KE, Kharasch ED.

Acta Anaesthesiol Scand. 2003 Jul;47(6):765-70.

PMID:
12803597
15.

Human halothane reduction in vitro by cytochrome P450 2A6 and 3A4: identification of low and high KM isoforms.

Spracklin DK, Kharasch ED.

Drug Metab Dispos. 1998 Jun;26(6):605-7. No abstract available.

PMID:
9616199
16.

Cytochrome P450 2E1 is the principal catalyst of human oxidative halothane metabolism in vitro.

Spracklin DK, Hankins DC, Fisher JM, Thummel KE, Kharasch ED.

J Pharmacol Exp Ther. 1997 Apr;281(1):400-11.

PMID:
9103523
17.

Human reductive halothane metabolism in vitro is catalyzed by cytochrome P450 2A6 and 3A4.

Spracklin DK, Thummel KE, Kharasch ED.

Drug Metab Dispos. 1996 Sep;24(9):976-83.

PMID:
8886607

Supplemental Content

Loading ...
Support Center