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Items: 12

1.

Identification and Development of an Irreversible Monoacylglycerol Lipase (MAGL) Positron Emission Tomography (PET) Radioligand with High Specificity.

Zhang L, Butler CR, Maresca KP, Takano A, Nag S, Jia Z, Arakawa R, Piro JR, Samad T, Smith DL, Nason DM, O'Neil S, McAllister L, Schildknegt K, Trapa P, McCarthy TJ, Villalobos A, Halldin C.

J Med Chem. 2019 Sep 26;62(18):8532-8543. doi: 10.1021/acs.jmedchem.9b00847. Epub 2019 Sep 16.

PMID:
31483137
2.

Deuterated active pharmaceutical ingredients: A science-based proposal for synthesis, analysis, and control. Part 1: Framing the problem.

Czeskis B, Elmore CS, Haight A, Hesk D, Maxwell BD, Miller SA, Raglione T, Schildknegt K, Traverse JF, Wang P.

J Labelled Comp Radiopharm. 2019 Apr 29. doi: 10.1002/jlcr.3743. [Epub ahead of print]

PMID:
31034626
3.

Metabolism of a 5HT6 Antagonist, 2-Methyl-1-(Phenylsulfonyl)-4-(Piperazin-1-yl)-1H-Benzo[d]imidazole (SAM-760): Impact of Sulfonamide Metabolism on Diminution of a Ketoconazole-Mediated Clinical Drug-Drug Interaction.

Sawant-Basak A, Obach RS, Doran A, Lockwood P, Schildknegt K, Gao H, Mancuso J, Tse S, Comery TA.

Drug Metab Dispos. 2018 Jul;46(7):934-942. doi: 10.1124/dmd.118.080457. Epub 2018 Apr 25.

PMID:
29695615
4.

Novel Application of the Two-Period Microtracer Approach to Determine Absolute Oral Bioavailability and Fraction Absorbed of Ertugliflozin.

Raje S, Callegari E, Sahasrabudhe V, Vaz A, Shi H, Fluhler E, Woolf EJ, Schildknegt K, Matschke K, Alvey C, Zhou S, Papadopoulos D, Fountaine R, Saur D, Terra SG, Stevens L, Gaunt D, Cutler DL.

Clin Transl Sci. 2018 Jul;11(4):405-411. doi: 10.1111/cts.12549. Epub 2018 Mar 25.

5.

Identification of a Novel Positron Emission Tomography (PET) Ligand for Imaging β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE-1) in Brain.

Zhang L, Chen L, Dutra JK, Beck EM, Nag S, Takano A, Amini N, Arakawa R, Brodney MA, Buzon LM, Doran SD, Lanyon LF, McCarthy TJ, Bales KR, Nolan CE, O'Neill BT, Schildknegt K, Halldin C, Villalobos A.

J Med Chem. 2018 Apr 26;61(8):3296-3308. doi: 10.1021/acs.jmedchem.7b01769. Epub 2018 Feb 2.

PMID:
29356535
6.

Identification and Profiling of a Selective and Brain Penetrant Radioligand for in Vivo Target Occupancy Measurement of Casein Kinase 1 (CK1) Inhibitors.

Wager TT, Galatsis P, Chandrasekaran RY, Butler TW, Li J, Zhang L, Mente S, Subramanyam C, Liu S, Doran AC, Chang C, Fisher K, Grimwood S, Hedde JR, Marconi M, Schildknegt K.

ACS Chem Neurosci. 2017 Sep 20;8(9):1995-2004. doi: 10.1021/acschemneuro.7b00155. Epub 2017 Jun 30.

PMID:
28609096
7.

Determination of Antibody-Drug Conjugate Released Payload Species Using Directed in Vitro Assays and Mass Spectrometric Interrogation.

Bessire AJ, Ballard TE, Charati M, Cohen J, Green M, Lam MH, Loganzo F, Nolting B, Pierce B, Puthenveetil S, Roberts L, Schildknegt K, Subramanyam C.

Bioconjug Chem. 2016 Jul 20;27(7):1645-54. doi: 10.1021/acs.bioconjchem.6b00192. Epub 2016 Jun 13.

PMID:
27206324
8.

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
9.

Metabolism, pharmacokinetics, and excretion of the 5-hydroxytryptamine1b receptor antagonist elzasonan in humans.

Kamel A, Obach RS, Colizza K, Wang W, O'Connell TN, Coelho RV Jr, Kelley RM, Schildknegt K.

Drug Metab Dispos. 2010 Nov;38(11):1984-99. doi: 10.1124/dmd.110.034595. Epub 2010 Jul 28.

PMID:
20668248
10.

Genotoxicity of 2-(3-chlorobenzyloxy)-6-(piperazinyl)pyrazine, a novel 5-hydroxytryptamine2c receptor agonist for the treatment of obesity: role of metabolic activation.

Kalgutkar AS, Dalvie DK, Aubrecht J, Smith EB, Coffing SL, Cheung JR, Vage C, Lame ME, Chiang P, McClure KF, Maurer TS, Coelho RV Jr, Soliman VF, Schildknegt K.

Drug Metab Dispos. 2007 Jun;35(6):848-58. Epub 2007 Mar 7.

PMID:
17344339
11.
12.

Regiocontrol in an intramolecular Schmidt reaction: total synthesis of (+)-aspidospermidine.

Iyengar R, Schildknegt K, Aubé J.

Org Lett. 2000 Jun 1;2(11):1625-7.

PMID:
10841495

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