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Items: 41

1.

Increased Brain Exposure of an Alpha-Synuclein Fibrillization Modulator by Utilization of an Activated Ester Prodrug Strategy.

Cairns AG, Vazquez-Romero A, Mahdi-Moein M, Ådén J, Elmore CS, Takano A, Arakawa R, Varrone A, Almqvist F, Schou M.

ACS Chem Neurosci. 2018 Jun 19. doi: 10.1021/acschemneuro.8b00236. [Epub ahead of print]

PMID:
29901990
2.

New trends and applications in carboxylation for isotope chemistry.

Bragg RA, Sardana M, Artelsmair M, Elmore CS.

J Labelled Comp Radiopharm. 2018 May 8. doi: 10.1002/jlcr.3633. [Epub ahead of print]

PMID:
29740851
3.

Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators.

O'Brien DE, Shaw DM, Cho HP, Cross AJ, Wesolowski SS, Felts AS, Bergare J, Elmore CS, Lindsley CW, Niswender CM, Conn PJ.

Mol Pharmacol. 2018 May;93(5):526-540. doi: 10.1124/mol.117.110114. Epub 2018 Mar 15.

PMID:
29545267
4.

Synthesis of C-14 labeled GABAA α2/α3 selective partial agonists and the investigation of late-occurring and long-circulating metabolites of GABAA receptor modulator AZD7325.

Artelsmair M, Gu C, Lewis RJ, Elmore CS.

J Labelled Comp Radiopharm. 2018 May 15;61(5):415-426. doi: 10.1002/jlcr.3602. Epub 2018 Mar 30.

5.

Late-occurring and Long-circulating Metabolites of GABAAα2,3 Receptor Modulator AZD7325 Involving Metabolic Cyclization and Aromatization: Relevance to MIST Analysis and Application for Patient Compliance.

Gu C, Artelsmair M, Elmore CS, Lewis RJ, Davis P, Hall JE, Dembofsky BT, Christoph G, Smith MA, Chapdelaine M, Sunzel M.

Drug Metab Dispos. 2018 Mar;46(3):303-315. doi: 10.1124/dmd.117.078873. Epub 2018 Jan 8.

PMID:
29311137
6.

[11C]AZ10419096 - a full antagonist PET radioligand for imaging brain 5-HT1B receptors.

Lindberg A, Nag S, Schou M, Takano A, Matsumoto J, Amini N, Elmore CS, Farde L, Pike VW, Halldin C.

Nucl Med Biol. 2017 Nov;54:34-40. doi: 10.1016/j.nucmedbio.2017.07.007. Epub 2017 Jul 21.

PMID:
28950161
7.

The Search for a Subtype-Selective PET Imaging Agent for the GABAA Receptor Complex: Evaluation of the Radiotracer [11C]ADO in Nonhuman Primates.

Lin SF, Bois F, Holden D, Nabulsi N, Pracitto R, Gao H, Kapinos M, Teng JK, Shirali A, Ropchan J, Carson RE, Elmore CS, Vasdev N, Huang Y.

Mol Imaging. 2017 Jan-Dec;16:1536012117731258. doi: 10.1177/1536012117731258.

8.

Synthesis of 2 C-14 labeled cathepsin C inhibitors: The use of a cyanide to displace a Benzotriazole.

Kingston L, Bergare J, Lönn H, Ericsson C, Grönberg G, Chen S, Elmore CS.

J Labelled Comp Radiopharm. 2017 May 30;60(6):294-301. doi: 10.1002/jlcr.3502.

PMID:
28324911
9.

Synthesis of 1β-hydroxydeoxycholic acid in H-2 and unlabeled forms.

Hayes MA, Roberts I, Grönberg G, Lv K, Lin B, Bergare J, Elmore CS.

J Labelled Comp Radiopharm. 2017 Apr;60(4):221-229. doi: 10.1002/jlcr.3495. Epub 2017 Mar 20.

PMID:
28183147
10.

Isotope labelling by reduction of nitriles: Application to the synthesis of isotopologues of tolmetin and celecoxib.

Ellis-Sawyer K, Bragg RA, Bushby N, Elmore CS, Hickey MJ.

J Labelled Comp Radiopharm. 2017 Apr;60(4):213-220. doi: 10.1002/jlcr.3492. Epub 2017 Mar 5.

PMID:
28130854
11.

Design, synthesis, in vitro characterization and preliminary imaging studies on fluorinated bile acid derivatives as PET tracers to study hepatic transporters.

Testa A, Dall'Angelo S, Mingarelli M, Augello A, Schweiger L, Welch A, Elmore CS, Sharma P, Zanda M.

Bioorg Med Chem. 2017 Feb 1;25(3):963-976. doi: 10.1016/j.bmc.2016.12.008. Epub 2016 Dec 9.

PMID:
28011201
12.

The synthesis of a tritium, carbon-14, and stable isotope-labeled cathepsin C inhibitors.

Allen P, Bragg RA, Caffrey M, Ericsson C, Hickey MJ, Kingston LP, Elmore CS.

J Labelled Comp Radiopharm. 2017 Feb;60(2):124-129. doi: 10.1002/jlcr.3483. Epub 2016 Dec 21.

PMID:
27868229
13.

The synthesis of tritium, carbon-14 and stable isotope labelled selective estrogen receptor degraders.

Bragg RA, Bushby N, Ericsson C, Kingston LP, Ji H, Elmore CS.

J Labelled Comp Radiopharm. 2016 Sep;59(11):454-61. doi: 10.1002/jlcr.3437. Epub 2016 Aug 24.

PMID:
27558079
14.

Synthesis of [(3) H] and [(2) H6 ]AZD6642, an inhibitor of 5-lipoxygenase activating protein (FLAP).

Lindelöf Å, Ericsson C, Simonsson R, Nilsson G, Grönberg G, Elmore CS.

J Labelled Comp Radiopharm. 2016 Jul;59(9):340-5. doi: 10.1002/jlcr.3409. Epub 2016 Jun 14.

PMID:
27298225
15.

Editorial.

Maxwell BD, Elmore CS.

J Labelled Comp Radiopharm. 2016 May 30;59(6):232. doi: 10.1002/jlcr.3401. No abstract available.

PMID:
27169759
16.

Abstracts of the 24th international isotope society (UK group) symposium: synthesis and applications of labelled compounds 2015.

Aigbirhio FI, Allwein S, Anwar A, Atzrodt J, Audisio D, Badman G, Bakale R, Berthon F, Bragg R, Brindle KM, Bushby N, Campos S, Cant AA, Chan MY, Colbon P, Cornelissen B, Czarny B, Derdau V, Dive V, Dunscombe M, Eggleston I, Ellis-Sawyer K, Elmore CS, Engstrom P, Ericsson C, Fairlamb IJ, Georgin D, Godfrey SP, He L, Hickey MJ, Huscroft IT, Kerr WJ, Lashford A, Lenz E, Lewinton S, L'Hermite MM, Lindelöf Å, Little G, Lockley WJ, Loreau O, Maddocks S, Marguerit M, Mirabello V, Mudd RJ, Nilsson GN, Owens PK, Pascu SI, Patriarche G, Pimlott SL, Pinault M, Plastow G, Racys DT, Reif J, Rossi J, Ruan J, Sarpaki S, Sephton SM, Simonsson R, Speed DJ, Sumal K, Sutherland A, Taran F, Thuleau A, Wang Y, Waring M, Watters WH, Wu J, Xiao J.

J Labelled Comp Radiopharm. 2016 Apr;59(4):175-86. doi: 10.1002/jlcr.3377. Epub 2016 Mar 18.

PMID:
26991121
17.

Determining the isotopic abundance of a labeled compound by mass spectrometry and how correcting for natural abundance distribution using analogous data from the unlabeled compound leads to a systematic error.

Schenk DJ, Lockley WJ, Elmore CS, Hesk D, Roberts D.

J Labelled Comp Radiopharm. 2016 Apr;59(4):136-46. doi: 10.1002/jlcr.3370. Epub 2016 Feb 24.

PMID:
26916110
18.

PET Tracers To Study Clinically Relevant Hepatic Transporters.

Testa A, Zanda M, Elmore CS, Sharma P.

Mol Pharm. 2015 Jul 6;12(7):2203-16. doi: 10.1021/acs.molpharmaceut.5b00059. Epub 2015 Jun 16. Review.

PMID:
26034841
19.

Isotope chemistry; a useful tool in the drug discovery arsenal.

Elmore CS, Bragg RA.

Bioorg Med Chem Lett. 2015 Jan 15;25(2):167-71. doi: 10.1016/j.bmcl.2014.11.051. Epub 2014 Nov 26. Review.

20.

Multiple compound-related adverse properties contribute to liver injury caused by endothelin receptor antagonists.

Kenna JG, Stahl SH, Eakins JA, Foster AJ, Andersson LC, Bergare J, Billger M, Elebring M, Elmore CS, Thompson RA.

J Pharmacol Exp Ther. 2015 Feb;352(2):281-90. doi: 10.1124/jpet.114.220491. Epub 2014 Dec 2.

21.

Evaluation of UV-HPLC and mass spectrometry methods for specific activity determination.

Elmore CS, Schenk DJ, Arent R, Kingston L.

J Labelled Comp Radiopharm. 2014 Sep;57(11):645-51. doi: 10.1002/jlcr.3234. Epub 2014 Sep 16.

PMID:
25223538
22.

Synthesis of three alpha 7 agonists in labeled form.

Elmore CS, Landvatter S, Dorff PN, Powell ME, Killick D, Blake T, Hall J, Heys JR, Harding J, Urbanek R, Ernst G.

J Labelled Comp Radiopharm. 2014 May 15;57(5):342-9. doi: 10.1002/jlcr.3186. Epub 2014 Apr 4.

PMID:
24700683
23.

Synthesis of ximelagatran, melagatran, hydroxymelagatran, and ethylmelagatran in H-3 labeled form.

Simonsson R, Stenhagen G, Ericsson C, Elmore CS.

J Labelled Comp Radiopharm. 2013 May 30;56(6):334-7. doi: 10.1002/jlcr.3028. Epub 2013 Feb 16.

PMID:
24285415
24.

An integrated strategy for in vivo metabolite profiling using high-resolution mass spectrometry based data processing techniques.

Guo J, Zhang M, Elmore CS, Vishwanathan K.

Anal Chim Acta. 2013 May 30;780:55-64. doi: 10.1016/j.aca.2013.04.012. Epub 2013 Apr 16.

PMID:
23680551
25.

Contribution of artifacts to N-methylated piperazine cyanide adduct formation in vitro from N-alkyl piperazine analogs.

Zhang M, Resuello CM, Guo J, Powell ME, Elmore CS, Hu J, Vishwanathan K.

Drug Metab Dispos. 2013 May;41(5):1023-34. doi: 10.1124/dmd.112.050450. Epub 2013 Feb 19.

26.

Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.

Brown DG, Bernstein PR, Wu Y, Urbanek RA, Becker CW, Throner SR, Dembofsky BT, Steelman GB, Lazor LA, Scott CW, Wood MW, Wesolowski SS, Nugiel DA, Koch S, Yu J, Pivonka DE, Li S, Thompson C, Zacco A, Elmore CS, Schroeder P, Liu J, Hurley CA, Ward S, Hunt HJ, Williams K, McLaughlin J, Hoesch V, Sydserff S, Maier D, Aharony D.

ACS Med Chem Lett. 2012 Nov 12;4(1):46-51. doi: 10.1021/ml300262e. eCollection 2013 Jan 10.

27.

In vitro binding of a radio-labeled positive allosteric modulator for metabotropic glutamate receptor subtype 5.

Zysk JR, Spear N, Fieles W, Stein MM, Sygowski LS, King MM, Hoesch V, Hastings R, Brockel B, Do M, Ström P, Gadient R, Chhajlani V, Elmore CS, Maier DL.

Synapse. 2013 Mar;67(3):135-44. doi: 10.1002/syn.21625. Epub 2012 Dec 6.

PMID:
23150216
28.

Development of new carbon-11 labelled radiotracers for imaging GABAA- and GABAB-benzodiazepine receptors.

Moran MD, Wilson AA, Elmore CS, Parkes J, Ng A, Sadovski O, Graff A, Daskalakis ZJ, Houle S, Chapdelaine MJ, Vasdev N.

Bioorg Med Chem. 2012 Jul 15;20(14):4482-8. doi: 10.1016/j.bmc.2012.05.046. Epub 2012 May 24.

PMID:
22717238
29.

Metabolism of a G protein-coupled receptor modulator, including two major 1,2,4-oxadiazole ring-opened metabolites and a rearranged cysteine-piperazine adduct.

Gu C, Elmore CS, Lin J, Zhou D, Luzietti R, Dorff P, Grimm SW.

Drug Metab Dispos. 2012 Jun;40(6):1151-63. doi: 10.1124/dmd.112.044636. Epub 2012 Mar 7.

30.

Use of radiolabeled compounds in drug metabolism and pharmacokinetic studies.

Isin EM, Elmore CS, Nilsson GN, Thompson RA, Weidolf L.

Chem Res Toxicol. 2012 Mar 19;25(3):532-42. doi: 10.1021/tx2005212. Epub 2012 Feb 28.

PMID:
22372867
31.

[³H]Chiba-1001(methyl-SSR180711) has low in vitro binding affinity and poor in vivo selectivity to nicotinic alpha-7 receptor in rodent brain.

Ding M, Ghanekar S, Elmore CS, Zysk JR, Werkheiser JL, Lee CM, Liu J, Chhajlani V, Maier DL.

Synapse. 2012 Apr;66(4):315-22. doi: 10.1002/syn.21513. Epub 2011 Dec 29.

PMID:
22108786
32.

In vitro and in vivo metabolism of a selective δ-opioid receptor.

Guo J, Gu C, Zhou D, Elmore CS, Bui KH, Grimm SW.

Drug Metab Dispos. 2011 Oct;39(10):1883-94. doi: 10.1124/dmd.111.040980. Epub 2011 Jul 13.

33.

2,6-Disubstituted pyrazines and related analogs as NR2B site antagonists of the NMDA receptor with anti-depressant activity.

Brown DG, Maier DL, Sylvester MA, Hoerter TN, Menhaji-Klotz E, Lasota CC, Hirata LT, Wilkins DE, Scott CW, Trivedi S, Chen T, McCarthy DJ, Maciag CM, Sutton EJ, Cumberledge J, Mathisen D, Roberts J, Gupta A, Liu F, Elmore CS, Alhambra C, Krumrine JR, Wang X, Ciaccio PJ, Wood MW, Campbell JB, Johansson MJ, Xia J, Wen X, Jiang J, Wang X, Peng Z, Hu T, Wang J.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3399-403. doi: 10.1016/j.bmcl.2011.03.117. Epub 2011 Apr 8.

PMID:
21524576
34.

Pre-clinical validation of a novel alpha-7 nicotinic receptor radiotracer, [(3)H]AZ11637326: target localization, biodistribution and ligand occupancy in the rat brain.

Maier DL, Hill G, Ding M, Tuke D, Einstein E, Gurley D, Gordon JC, Bock MJ, Smith JS, Bialecki R, Eisman M, Elmore CS, Werkheiser JL.

Neuropharmacology. 2011 Jul-Aug;61(1-2):161-71. doi: 10.1016/j.neuropharm.2011.03.024. Epub 2011 Apr 7.

PMID:
21497612
35.

Development of a PET radioligand for the central 5-HT1B receptor: radiosynthesis and characterization in cynomolgus monkeys of eight radiolabeled compounds.

Andersson JD, Pierson ME, Finnema SJ, Gulyás B, Heys R, Elmore CS, Farde L, Halldin C.

Nucl Med Biol. 2011 Feb;38(2):261-72. doi: 10.1016/j.nucmedbio.2010.08.006. Epub 2010 Dec 3.

PMID:
21315282
36.

[¹²⁵I]YP20: a novel radioligand specific for the extracellular domain of the CRF₁ receptor.

Gordon JC, Edwards P, Elmore CS, Lazor LA, Paschetto K, Bostwick R, Sylvester M, Mauger R, Scott C, Aharony D.

Eur J Pharmacol. 2010 Dec 15;649(1-3):59-63. doi: 10.1016/j.ejphar.2010.09.008. Epub 2010 Sep 18.

PMID:
20854803
37.

Absence of direct effects on the dopamine D2 receptor by mGluR2/3-selective receptor agonists LY 354,740 and LY 379,268.

Zysk JR, Widzowski D, Sygowski LA, Knappenberger KS, Spear N, Elmore CS, Dorff P, Liu H, Doherty J, Chhajlani V.

Synapse. 2011 Jan;65(1):64-8. doi: 10.1002/syn.20817.

PMID:
20506301
38.

D2 receptor occupancy in conscious rat brain is not significantly distinguished with [3H]-MNPA, [3H]-(+)-PHNO, and [3H]-raclopride.

Peng T, Zysk J, Dorff P, Elmore CS, Ström P, Malmquist J, Ding M, Tuke D, Werkheiser J, Widzowski D, Mrzljak L, Maier D.

Synapse. 2010 Aug;64(8):624-33. doi: 10.1002/syn.20771.

PMID:
20340171
39.

[N-methyl-3H3]AZ10419369 binding to the 5-HT1B receptor: in vitro characterization and in vivo receptor occupancy.

Maier DL, Sobotka-Briner C, Ding M, Powell ME, Jiang Q, Hill G, Heys JR, Elmore CS, Pierson ME, Mrzljak L.

J Pharmacol Exp Ther. 2009 Jul;330(1):342-51. doi: 10.1124/jpet.109.150722. Epub 2009 Apr 28.

40.

Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs.

Beconi MG, Reed JR, Teffera Y, Xia YQ, Kochansky CJ, Liu DQ, Xu S, Elmore CS, Ciccotto S, Hora DF, Stearns RA, Vincent SH.

Drug Metab Dispos. 2007 Apr;35(4):525-32. Epub 2007 Jan 12.

41.

Metabolism and excretion of the dipeptidyl peptidase 4 inhibitor [14C]sitagliptin in humans.

Vincent SH, Reed JR, Bergman AJ, Elmore CS, Zhu B, Xu S, Ebel D, Larson P, Zeng W, Chen L, Dilzer S, Lasseter K, Gottesdiener K, Wagner JA, Herman GA.

Drug Metab Dispos. 2007 Apr;35(4):533-8. Epub 2007 Jan 12.

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