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Page 1
Preclinical Characterization of the Phosphodiesterase 10A PET Tracer [(11)C]MK-8193.
Hostetler ED, Fan H, Joshi AD, Zeng Z, Eng W, Gantert L, Holahan M, Meng X, Miller P, O'Malley S, Purcell M, Riffel K, Salinas C, Williams M, Ma B, Buist N, Smith SM, Coleman PJ, Cox CD, Flores BA, Raheem IT, Cook JJ, Evelhoch JL. Hostetler ED, et al. Among authors: raheem it. Mol Imaging Biol. 2016 Aug;18(4):579-87. doi: 10.1007/s11307-015-0910-0. Mol Imaging Biol. 2016. PMID: 26596571
The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey.
Smith SM, Uslaner JM, Cox CD, Huszar SL, Cannon CE, Vardigan JD, Eddins D, Toolan DM, Kandebo M, Yao L, Raheem IT, Schreier JD, Breslin MJ, Coleman PJ, Renger JJ. Smith SM, et al. Among authors: raheem it. Neuropharmacology. 2013 Jan;64:215-23. doi: 10.1016/j.neuropharm.2012.06.013. Epub 2012 Jun 27. Neuropharmacology. 2013. PMID: 22750078
Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.
Raheem IT, Breslin MJ, Bruno J, Cabalu TD, Cooke A, Cox CD, Cui D, Garson S, Gotter AL, Fox SV, Harrell CM, Kuduk SD, Lemaire W, Prueksaritanont T, Renger JJ, Stump C, Tannenbaum PL, Williams PD, Winrow CJ, Coleman PJ. Raheem IT, et al. Bioorg Med Chem Lett. 2015 Feb 1;25(3):444-50. doi: 10.1016/j.bmcl.2014.12.056. Epub 2014 Dec 23. Bioorg Med Chem Lett. 2015. PMID: 25577040
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. Cox CD, et al. Among authors: raheem it. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4893-4898. doi: 10.1016/j.bmcl.2015.05.080. Epub 2015 Jun 1. Bioorg Med Chem Lett. 2015. PMID: 26077491
Discovery of 2-Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV-1 Integrase Strand Transfer Inhibitors.
Raheem IT, Walji AM, Klein D, Sanders JM, Powell DA, Abeywickrema P, Barbe G, Bennet A, Childers K, Christensen M, Clas SD, Dubost D, Embrey M, Grobler J, Hafey MJ, Hartingh TJ, Hazuda DJ, Kuethe JT, McCabe Dunn J, Miller MD, Moore KP, Nolting A, Pajkovic N, Patel S, Peng Z, Rada V, Rearden P, Schreier JD, Sisko J, Steele TG, Truchon JF, Wai J, Xu M, Coleman PJ. Raheem IT, et al. J Med Chem. 2015 Oct 22;58(20):8154-65. doi: 10.1021/acs.jmedchem.5b01037. Epub 2015 Oct 8. J Med Chem. 2015. PMID: 26397965
Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Raheem IT, Schreier JD, Fuerst J, Gantert L, Hostetler ED, Huszar S, Joshi A, Kandebo M, Kim SH, Li J, Ma B, McGaughey G, Sharma S, Shipe WD, Uslaner J, Vandeveer GH, Yan Y, Renger JJ, Smith SM, Coleman PJ, Cox CD. Raheem IT, et al. Bioorg Med Chem Lett. 2016 Jan 1;26(1):126-32. doi: 10.1016/j.bmcl.2015.11.013. Epub 2015 Nov 10. Bioorg Med Chem Lett. 2016. PMID: 26602277
Discovery and optimization of 2-pyridinone aminal integrase strand transfer inhibitors for the treatment of HIV.
Schreier JD, Embrey MW, Raheem IT, Barbe G, Campeau LC, Dubost D, McCabe Dunn J, Grobler J, Hartingh TJ, Hazuda DJ, Klein D, Miller MD, Moore KP, Nguyen N, Pajkovic N, Powell DA, Rada V, Sanders JM, Sisko J, Steele TG, Wai J, Walji A, Xu M, Coleman PJ. Schreier JD, et al. Among authors: raheem it. Bioorg Med Chem Lett. 2017 May 1;27(9):2038-2046. doi: 10.1016/j.bmcl.2017.02.039. Epub 2017 Feb 20. Bioorg Med Chem Lett. 2017. PMID: 28285916
Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia.
Layton ME, Kern JC, Hartingh TJ, Shipe WD, Raheem I, Kandebo M, Hayes RP, Huszar S, Eddins D, Ma B, Fuerst J, Wollenberg GK, Li J, Fritzen J, McGaughey GB, Uslaner JM, Smith SM, Coleman PJ, Cox CD. Layton ME, et al. J Med Chem. 2023 Jan 26;66(2):1157-1171. doi: 10.1021/acs.jmedchem.2c01521. Epub 2023 Jan 9. J Med Chem. 2023. PMID: 36624931 Free PMC article.
38 results