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Items: 1 to 20 of 122

1.

Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer.

Hu E, Ma J, Biorn C, Lester-Zeiner D, Cho R, Rumfelt S, Kunz RK, Nixey T, Michelsen K, Miller S, Shi J, Wong J, Hill Della Puppa G, Able J, Talreja S, Hwang DR, Hitchcock SA, Porter A, Immke D, Allen JR, Treanor J, Chen H.

J Med Chem. 2012 May 24;55(10):4776-87. doi: 10.1021/jm3002372. Epub 2012 May 11.

PMID:
22548439
2.

AMG 580: a novel small molecule phosphodiesterase 10A (PDE10A) positron emission tomography tracer.

Chen H, Lester-Zeiner D, Shi J, Miller S, Glaus C, Hu E, Chen N, Able J, Biorn C, Wong J, Ma J, Michelsen K, Hill Della Puppa G, Kazules T, Dou HH, Talreja S, Zhao X, Chen A, Rumfelt S, Kunz RK, Ye H, Thiel OR, Williamson T, Davis C, Porter A, Immke D, Allen JR, Treanor J.

J Pharmacol Exp Ther. 2015 Feb;352(2):327-37. doi: 10.1124/jpet.114.220517. Epub 2014 Dec 11.

3.

Preclinical evaluation of 18F-JNJ41510417 as a radioligand for PET imaging of phosphodiesterase-10A in the brain.

Celen S, Koole M, De Angelis M, Sannen I, Chitneni SK, Alcazar J, Dedeurwaerdere S, Moechars D, Schmidt M, Verbruggen A, Langlois X, Van Laere K, Andrés JI, Bormans G.

J Nucl Med. 2010 Oct;51(10):1584-91. doi: 10.2967/jnumed.110.077040. Epub 2010 Sep 16.

4.

Radiosynthesis and initial characterization of a PDE10A specific PET tracer [18F]AMG 580 in non-human primates.

Hwang DR, Hu E, Allen JR, Davis C, Treanor J, Miller S, Chen H, Shi B, Narayanan TK, Barret O, Alagille D, Yu Z, Slifstein M.

Nucl Med Biol. 2015 Aug;42(8):654-63. doi: 10.1016/j.nucmedbio.2015.04.004. Epub 2015 Apr 16.

PMID:
25935386
5.

Development of a series of novel carbon-11 labeled PDE10A inhibitors.

Stepanov V, Miura S, Takano A, Amini N, Nakao R, Hasui T, Nakashima K, Taniguchi T, Kimura H, Kuroita T, Halldin C.

J Labelled Comp Radiopharm. 2015 May 15;58(5):202-8. doi: 10.1002/jlcr.3284. Epub 2015 Apr 19.

PMID:
25891816
6.

Characterization of binding and inhibitory properties of TAK-063, a novel phosphodiesterase 10A inhibitor.

Harada A, Suzuki K, Kamiguchi N, Miyamoto M, Tohyama K, Nakashima K, Taniguchi T, Kimura H.

PLoS One. 2015 Mar 27;10(3):e0122197. doi: 10.1371/journal.pone.0122197. eCollection 2015.

7.

Characterization of the binding properties of T-773 as a PET radioligand for phosphodiesterase 10A.

Harada A, Suzuki K, Miura S, Hasui T, Kamiguchi N, Ishii T, Taniguchi T, Kuroita T, Takano A, Stepanov V, Halldin C, Kimura H.

Nucl Med Biol. 2015 Feb;42(2):146-54. doi: 10.1016/j.nucmedbio.2014.09.005. Epub 2014 Sep 28.

PMID:
25451212
8.

Initial characterization of a PDE10A selective positron emission tomography tracer [11C]AMG 7980 in non-human primates.

Hwang DR, Hu E, Rumfelt S, Easwaramoorthy B, Castrillon J, Davis C, Allen JR, Chen H, Treanor J, Abi-Dargham A, Slifstein M.

Nucl Med Biol. 2014 Apr;41(4):343-9. doi: 10.1016/j.nucmedbio.2014.01.007. Epub 2014 Jan 17.

PMID:
24607437
9.

Preclinical evaluation of a promising C-11 labeled PET tracer for imaging phosphodiesterase 10A in the brain of living subject.

Liu H, Jin H, Yue X, Zhang X, Yang H, Li J, Flores H, Su Y, Perlmutter JS, Tu Z.

Neuroimage. 2015 Nov 1;121:253-62. doi: 10.1016/j.neuroimage.2015.07.049. Epub 2015 Jul 26.

10.

Preclinical evaluation of [(18)F]JNJ42259152 as a PET tracer for PDE10A.

Celen S, Koole M, Ooms M, De Angelis M, Sannen I, Cornelis J, Alcazar J, Schmidt M, Verbruggen A, Langlois X, Van Laere K, Andrés JI, Bormans G.

Neuroimage. 2013 Nov 15;82:13-22. doi: 10.1016/j.neuroimage.2013.04.123. Epub 2013 May 9.

PMID:
23664955
11.

Further evaluation of [11C]MP-10 as a radiotracer for phosphodiesterase 10A: PET imaging study in rhesus monkeys and brain tissue metabolite analysis.

Lin SF, Labaree D, Chen MK, Holden D, Gallezot JD, Kapinos M, Teng JK, Najafzadeh S, Plisson C, Rabiner EA, Gunn RN, Carson RE, Huang Y.

Synapse. 2015 Feb;69(2):86-95. doi: 10.1002/syn.21792. Epub 2014 Dec 11.

12.

Discovery and development of 11C-Lu AE92686 as a radioligand for PET imaging of phosphodiesterase10A in the brain.

Kehler J, Kilburn JP, Estrada S, Christensen SR, Wall A, Thibblin A, Lubberink M, Bundgaard C, Brennum LT, Steiniger-Brach B, Christoffersen CT, Timmermann S, Kreilgaard M, Antoni G, Bang-Andersen B, Nielsen J.

J Nucl Med. 2014 Sep;55(9):1513-8. doi: 10.2967/jnumed.114.140178. Epub 2014 Jul 3.

13.

Synthesis of Fluorine-Containing Phosphodiesterase 10A (PDE10A) Inhibitors and the In Vivo Evaluation of F-18 Labeled PDE10A PET Tracers in Rodent and Nonhuman Primate.

Li J, Zhang X, Jin H, Fan J, Flores H, Perlmutter JS, Tu Z.

J Med Chem. 2015 Nov 12;58(21):8584-600. doi: 10.1021/acs.jmedchem.5b01205. Epub 2015 Oct 15.

14.

Design and synthesis of a novel 2-oxindole scaffold as a highly potent and brain-penetrant phosphodiesterase 10A inhibitor.

Yoshikawa M, Kamisaki H, Kunitomo J, Oki H, Kokubo H, Suzuki A, Ikemoto T, Nakashima K, Kamiguchi N, Harada A, Kimura H, Taniguchi T.

Bioorg Med Chem. 2015 Nov 15;23(22):7138-49. doi: 10.1016/j.bmc.2015.10.002. Epub 2015 Oct 9.

PMID:
26494583
15.

Discovery of [¹¹C]MK-8193 as a PET tracer to measure target engagement of phosphodiesterase 10A (PDE10A) inhibitors.

Cox CD, Hostetler ED, Flores BA, Evelhoch JL, Fan H, Gantert L, Holahan M, Eng W, Joshi A, McGaughey G, Meng X, Purcell M, Raheem IT, Riffel K, Yan Y, Renger JJ, Smith SM, Coleman PJ.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4893-8. doi: 10.1016/j.bmcl.2015.05.080. Epub 2015 Jun 1.

PMID:
26077491
16.

Brain PET measurement of PDE10A occupancy by TAK-063, a new PDE10A inhibitor, using [11 C]T-773 in nonhuman primates.

Takano A, Stepanov V, Nakao R, Amini N, Gulyás B, Kimura H, Halldin C.

Synapse. 2016 Jun;70(6):253-63. doi: 10.1002/syn.21896. Epub 2016 Mar 4.

PMID:
26878349
17.

Synthesis, in vivo occupancy, and radiolabeling of potent phosphodiesterase subtype-10 inhibitors as candidates for positron emission tomography imaging.

Andrés JI, De Angelis M, Alcázar J, Iturrino L, Langlois X, Dedeurwaerdere S, Lenaerts I, Vanhoof G, Celen S, Bormans G.

J Med Chem. 2011 Aug 25;54(16):5820-35. doi: 10.1021/jm200536d. Epub 2011 Aug 2.

PMID:
21777010
18.

Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).

Hu E, Kunz RK, Chen N, Rumfelt S, Siegmund A, Andrews K, Chmait S, Zhao S, Davis C, Chen H, Lester-Zeiner D, Ma J, Biorn C, Shi J, Porter A, Treanor J, Allen JR.

J Med Chem. 2013 Nov 14;56(21):8781-92. doi: 10.1021/jm401234w. Epub 2013 Oct 25.

PMID:
24102193
19.

Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).

Hu E, Chen N, Bourbeau MP, Harrington PE, Biswas K, Kunz RK, Andrews KL, Chmait S, Zhao X, Davis C, Ma J, Shi J, Lester-Zeiner D, Danao J, Able J, Cueva M, Talreja S, Kornecook T, Chen H, Porter A, Hungate R, Treanor J, Allen JR.

J Med Chem. 2014 Aug 14;57(15):6632-41. doi: 10.1021/jm500713j. Epub 2014 Aug 4.

PMID:
25062128
20.

Characterization of [11C]Lu AE92686 as a PET radioligand for phosphodiesterase 10A in the nonhuman primate brain.

Yang KC, Stepanov V, Amini N, Martinsson S, Takano A, Nielsen J, Bundgaard C, Bang-Andersen B, Grimwood S, Halldin C, Farde L, Finnema SJ.

Eur J Nucl Med Mol Imaging. 2017 Feb;44(2):308-320. doi: 10.1007/s00259-016-3544-9. Epub 2016 Nov 5.

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