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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: van hecken a, van laere k. 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: van hecken a, van laere k. 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: van laere k. 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. 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: van laere k. 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.
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: van hecken a, van laere k. J Psychopharmacol. 2011 Mar;25(3):314-28. doi: 10.1177/0269881109354927. Epub 2010 Feb 10. J Psychopharmacol. 2011. PMID: 20147571 Clinical Trial.
Quantitative PET imaging of radioligands with slow kinetics in human brain.
Sanabria-Bohórquez SM, Van Laere K. Sanabria-Bohórquez SM, et al. Among authors: van laere k. Eur J Nucl Med Mol Imaging. 2010 Aug;37(8):1613-5. doi: 10.1007/s00259-010-1518-x. Epub 2010 Jun 25. Eur J Nucl Med Mol Imaging. 2010. PMID: 20577739 No abstract available.
475 results