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Page 1
Discovery of a novel series of orally active nociceptin/orphanin FQ (NOP) receptor antagonists based on a dihydrospiro(piperidine-4,7'-thieno[2,3-c]pyran) scaffold.
Toledo MA, Pedregal C, Lafuente C, Diaz N, Martinez-Grau MA, Jiménez A, Benito A, Torrado A, Mateos C, Joshi EM, Kahl SD, Rash KS, Mudra DR, Barth VN, Shaw DB, McKinzie D, Witkin JM, Statnick MA. Toledo MA, et al. Among authors: joshi em. J Med Chem. 2014 Apr 24;57(8):3418-29. doi: 10.1021/jm500117r. Epub 2014 Apr 11. J Med Chem. 2014. PMID: 24678969
Development of LC-MS/MS-based receptor occupancy tracers and positron emission tomography radioligands for the nociceptin/orphanin FQ (NOP) receptor.
Pedregal C, Joshi EM, Toledo MA, Lafuente C, Diaz N, Martinez-Grau MA, Jiménez A, Benito A, Navarro A, Chen Z, Mudra DR, Kahl SD, Rash KS, Statnick MA, Barth VN. Pedregal C, et al. Among authors: joshi em. J Med Chem. 2012 Jun 14;55(11):4955-67. doi: 10.1021/jm201629q. Epub 2012 May 16. J Med Chem. 2012. PMID: 22541041
Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.
Dreyfus N, Myers JK, Badescu VO, de Frutos O, de la Puente ML, Ding C, Filla SA, Fynboe K, Gernert DL, Heinz BA, Hemrick-Luecke SK, Johnson KW, Johnson MP, López P, Love PL, Martin LJ, Masquelin T, McCoy MJ, Mendiola J, Morrow D, Muhlhauser M, Pascual G, Perun TJ, Pfeifer LA, Phebus LA, Richards SJ, Rincón JA, Seest EP, Shah J, Shaojuan J, Simmons RM, Stephenson GA, Tromiczak EG, Thompson LK, Walter MW, Weber WW, Zarrinmayeh H, Thomas CE, Joshi E, Iyengar S, Johansson AM. Dreyfus N, et al. ACS Med Chem Lett. 2013 May 7;4(6):560-4. doi: 10.1021/ml400049p. eCollection 2013 Jun 13. ACS Med Chem Lett. 2013. PMID: 24900709 Free PMC article.
Discovery of 6-(Fluoro-(18)F)-3-(1H-pyrrolo[2,3-c]pyridin-1-yl)isoquinolin-5-amine ([(18)F]-MK-6240): A Positron Emission Tomography (PET) Imaging Agent for Quantification of Neurofibrillary Tangles (NFTs).
Walji AM, Hostetler ED, Selnick H, Zeng Z, Miller P, Bennacef I, Salinas C, Connolly B, Gantert L, Holahan M, O'Malley S, Purcell M, Riffel K, Li J, Balsells J, OBrien JA, Melquist S, Soriano A, Zhang X, Ogawa A, Xu S, Joshi E, Della Rocca J, Hess FJ, Schachter J, Hesk D, Schenk D, Struyk A, Babaoglu K, Lohith TG, Wang Y, Yang K, Fu J, Evelhoch JL, Coleman PJ. Walji AM, et al. J Med Chem. 2016 May 26;59(10):4778-89. doi: 10.1021/acs.jmedchem.6b00166. Epub 2016 May 5. J Med Chem. 2016. PMID: 27088900
Informing the Selection of Screening Hit Series with in Silico Absorption, Distribution, Metabolism, Excretion, and Toxicity Profiles.
Sanders JM, Beshore DC, Culberson JC, Fells JI, Imbriglio JE, Gunaydin H, Haidle AM, Labroli M, Mattioni BE, Sciammetta N, Shipe WD, Sheridan RP, Suen LM, Verras A, Walji A, Joshi EM, Bueters T. Sanders JM, et al. Among authors: joshi em. J Med Chem. 2017 Aug 24;60(16):6771-6780. doi: 10.1021/acs.jmedchem.6b01577. Epub 2017 May 5. J Med Chem. 2017. PMID: 28418656 Review.
Evaluation in vitro and in animals of a new 11C-labeled PET radioligand for metabotropic glutamate receptors 1 in brain.
Zanotti-Fregonara P, Barth VN, Liow JS, Zoghbi SS, Clark DT, Rhoads E, Siuda E, Heinz BA, Nisenbaum E, Dressman B, Joshi E, Luffer-Atlas D, Fisher MJ, Masters JJ, Goebl N, Kuklish SL, Morse C, Tauscher J, Pike VW, Innis RB. Zanotti-Fregonara P, et al. Eur J Nucl Med Mol Imaging. 2013 Jan;40(2):245-53. doi: 10.1007/s00259-012-2269-7. Epub 2012 Nov 8. Eur J Nucl Med Mol Imaging. 2013. PMID: 23135321 Free PMC article.
The design and synthesis of novel spirocyclic heterocyclic sulfone ROMK inhibitors as diuretics.
Chobanian HR, Guo Y, Pio B, Tang H, Teumelsan N, Clements M, Frie J, Ferguson R, Guo Z, Thomas-Fowlkes BS, Felix JP, Liu J, Kohler M, Priest B, Hampton C, Pai LY, Corona A, Metzger J, Tong V, Joshi EM, Xu L, Owens K, Maloney K, Sullivan K, Pasternak A. Chobanian HR, et al. Among authors: joshi em. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1109-1114. doi: 10.1016/j.bmcl.2016.10.032. Epub 2016 Oct 13. Bioorg Med Chem Lett. 2017. PMID: 28111141
Preclinical Characterization of 18F-MK-6240, a Promising PET Tracer for In Vivo Quantification of Human Neurofibrillary Tangles.
Hostetler ED, Walji AM, Zeng Z, Miller P, Bennacef I, Salinas C, Connolly B, Gantert L, Haley H, Holahan M, Purcell M, Riffel K, Lohith TG, Coleman P, Soriano A, Ogawa A, Xu S, Zhang X, Joshi E, Della Rocca J, Hesk D, Schenk DJ, Evelhoch JL. Hostetler ED, et al. J Nucl Med. 2016 Oct;57(10):1599-1606. doi: 10.2967/jnumed.115.171678. Epub 2016 May 26. J Nucl Med. 2016. PMID: 27230925 Free article.
18 results