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Page 1
MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans.
Atack JR, Wafford KA, Street LJ, Dawson GR, Tye S, Van Laere K, Bormans G, Sanabria-Bohórquez SM, De Lepeleire I, de Hoon JN, Van Hecken A, Burns HD, McKernan RM, Murphy MG, Hargreaves RJ. Atack JR, et al. Among authors: de lepeleire i, de hoon jn. J Psychopharmacol. 2011 Mar;25(3):314-28. doi: 10.1177/0269881109354927. Epub 2010 Feb 10. J Psychopharmacol. 2011. PMID: 20147571 Clinical Trial.
Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist.
Atack JR, Hallett DJ, Tye S, Wafford KA, Ryan C, Sanabria-Bohórquez SM, Eng WS, Gibson RE, Burns HD, Dawson GR, Carling RW, Street LJ, Pike A, De Lepeleire I, Van Laere K, Bormans G, de Hoon JN, Van Hecken A, McKernan RM, Murphy MG, Hargreaves RJ. Atack JR, et al. Among authors: de lepeleire i, de hoon jn. J Psychopharmacol. 2011 Mar;25(3):329-44. doi: 10.1177/0269881109354928. Epub 2010 Feb 15. J Psychopharmacol. 2011. PMID: 20156926 Clinical Trial.
[18F]MK-9470, a positron emission tomography (PET) tracer for in vivo human PET brain imaging of the cannabinoid-1 receptor.
Burns HD, Van Laere K, Sanabria-Bohórquez S, Hamill TG, Bormans G, Eng WS, Gibson R, Ryan C, Connolly B, Patel S, Krause S, Vanko A, Van Hecken A, Dupont P, De Lepeleire I, Rothenberg P, Stoch SA, Cote J, Hagmann WK, Jewell JP, Lin LS, Liu P, Goulet MT, Gottesdiener K, Wagner JA, de Hoon J, Mortelmans L, Fong TM, Hargreaves RJ. Burns HD, et al. Among authors: de lepeleire i, de hoon j. Proc Natl Acad Sci U S A. 2007 Jun 5;104(23):9800-5. doi: 10.1073/pnas.0703472104. Epub 2007 May 29. Proc Natl Acad Sci U S A. 2007. PMID: 17535893 Free PMC article.
The acyclic CB1R inverse agonist taranabant mediates weight loss by increasing energy expenditure and decreasing caloric intake.
Addy C, Wright H, Van Laere K, Gantz I, Erondu N, Musser BJ, Lu K, Yuan J, Sanabria-Bohórquez SM, Stoch A, Stevens C, Fong TM, De Lepeleire I, Cilissen C, Cote J, Rosko K, Gendrano IN 3rd, Nguyen AM, Gumbiner B, Rothenberg P, de Hoon J, Bormans G, Depré M, Eng WS, Ravussin E, Klein S, Blundell J, Herman GA, Burns HD, Hargreaves RJ, Wagner J, Gottesdiener K, Amatruda JM, Heymsfield SB. Addy C, et al. Among authors: de lepeleire i, de hoon j. Cell Metab. 2008 Jan;7(1):68-78. doi: 10.1016/j.cmet.2007.11.012. Cell Metab. 2008. PMID: 18177726 Free article. Clinical Trial.
In vivo characterization and dynamic receptor occupancy imaging of TPA023B, an alpha 2/alpha 3/alpha 5 subtype selective gamma-aminobutyric acid-a partial agonist.
Van Laere K, Bormans G, Sanabria-Bohórquez SM, de Groot T, Dupont P, De Lepeleire I, de Hoon J, Mortelmans L, Hargreaves RJ, Atack JR, Burns HD. Van Laere K, et al. Among authors: de lepeleire i, de groot t, de hoon j. Biol Psychiatry. 2008 Jul 15;64(2):153-61. doi: 10.1016/j.biopsych.2008.01.021. Epub 2008 Mar 14. Biol Psychiatry. 2008. PMID: 18339360 Clinical Trial.
Kinetic analysis of the cannabinoid-1 receptor PET tracer [(18)F]MK-9470 in human brain.
Sanabria-Bohórquez SM, Hamill TG, Goffin K, De Lepeleire I, Bormans G, Burns HD, Van Laere K. Sanabria-Bohórquez SM, et al. Among authors: de lepeleire i. Eur J Nucl Med Mol Imaging. 2010 May;37(5):920-33. doi: 10.1007/s00259-009-1340-5. Epub 2009 Dec 24. Eur J Nucl Med Mol Imaging. 2010. PMID: 20033684 Clinical Trial.
Evaluation of [¹⁸F]MK-0911, a positron emission tomography (PET) tracer for opioid receptor-like 1 (ORL1), in rhesus monkey and human.
Hostetler ED, Sanabria-Bohórquez S, Eng W, Joshi AD, Patel S, Gibson RE, O'Malley S, Krause SM, Ryan C, Riffel K, Bi S, Okamoto O, Kawamoto H, Ozaki S, Ohta H, de Groot T, Bormans G, Depré M, de Hoon J, De Lepeleire I, Reynders T, Cook JJ, Burns HD, Egan M, Cho W, van Laere K, Hargreaves RJ. Hostetler ED, et al. Among authors: de lepeleire i, de groot t, de hoon j. Neuroimage. 2013 Mar;68:1-10. doi: 10.1016/j.neuroimage.2012.11.053. Epub 2012 Dec 11. Neuroimage. 2013. PMID: 23238431
In vivo quantification of calcitonin gene-related peptide receptor occupancy by telcagepant in rhesus monkey and human brain using the positron emission tomography tracer [11C]MK-4232.
Hostetler ED, Joshi AD, Sanabria-Bohórquez S, Fan H, Zeng Z, Purcell M, Gantert L, Riffel K, Williams M, O'Malley S, Miller P, Selnick HG, Gallicchio SN, Bell IM, Salvatore CA, Kane SA, Li CC, Hargreaves RJ, de Groot T, Bormans G, Van Hecken A, Derdelinckx I, de Hoon J, Reynders T, Declercq R, De Lepeleire I, Kennedy WP, Blanchard R, Marcantonio EE, Sur C, Cook JJ, Van Laere K, Evelhoch JL. Hostetler ED, et al. Among authors: de lepeleire i, de groot t, de hoon j. J Pharmacol Exp Ther. 2013 Nov;347(2):478-86. doi: 10.1124/jpet.113.206458. Epub 2013 Aug 23. J Pharmacol Exp Ther. 2013. PMID: 23975906 Free article. Clinical Trial.
Characterization of the novel GlyT1 PET tracer [18F]MK-6577 in humans.
Joshi AD, Sanabria-Bohórquez SM, Bormans G, Koole M, De Hoon J, Van Hecken A, Depre M, De Lepeleire I, Van Laere K, Sur C, Hamill TG. Joshi AD, et al. Among authors: de lepeleire i, de hoon j. Synapse. 2015 Jan;69(1):33-40. doi: 10.1002/syn.21782. Epub 2014 Sep 24. Synapse. 2015. PMID: 25196464
Image-derived input function for [11C]flumazenil kinetic analysis in human brain.
Sanabria-Bohórquez SM, Maes A, Dupont P, Bormans G, de Groot T, Coimbra A, Eng W, Laethem T, De Lepeleire I, Gambale J, Vega JM, Burns HD. Sanabria-Bohórquez SM, et al. Among authors: de lepeleire i, de groot t. Mol Imaging Biol. 2003 Mar-Apr;5(2):72-8. doi: 10.1016/s1536-1632(03)00046-5. Mol Imaging Biol. 2003. PMID: 14499147
77 results