11C-labeling and preliminary evaluation of pimavanserin as a 5-HT2A receptor PET-radioligand

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 5, 2015, Pages 1053-1056

  Andersen, Valdemar L ^a,b   Hansen, Hanne D ^a   Herth, Matthias M ^a   Dyssegaard, Agnete ^a   Knudsen, Gitte M ^a   Kristensen, Jesper L ^a,b  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

^b UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

5 HT2A receptor; Carbon 11; N methylation; PET; Pimavanserin

Indexed keywords

KETANSERIN; PIMAVANSERIN; PIMAVANSERIN CARBON C 11; RADIOLIGAND; SEROTONIN 2A AGONIST; SEROTONIN 2A ANTAGONIST; SEROTONIN 2A RECEPTOR; UNCLASSIFIED DRUG; CARBON; LIGAND; PIPERIDINE DERIVATIVE; RADIOPHARMACEUTICAL AGENT; SEROTONIN 2 AGONIST; UREA;

ANIMAL EXPERIMENT; ARTICLE; BRAIN CORTEX; BRAIN REGION; DRUG METABOLISM; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; EVALUATION STUDY; FEMALE; ISOTOPE LABELING; LANDRACE PIG; METHYLATION; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; QUANTUM YIELD; RADIOCHEMISTRY; RAT; THALAMUS; VOLUME OF DISTRIBUTION; ANALOGS AND DERIVATIVES; ANIMAL; METABOLISM; PIG;

SUIDAE;

ANIMALS; CARBON RADIOISOTOPES; LIGANDS; METHYLATION; PIPERIDINES; POSITRON-EMISSION TOMOGRAPHY; RADIOPHARMACEUTICALS; RECEPTOR, SEROTONIN, 5-HT2A; SEROTONIN 5-HT2 RECEPTOR AGONISTS; SWINE; UREA;

EID: 84943368056     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.01.017     Document Type: Article

References (17)

1. J. Gonzalez-Maeso, N.V. Weisstaub, M.M. Zhou, P. Chan, L. Ivic, R. Ang, A. Lira, M. Bradley-Moore, Y.C. Ge, Q. Zhou, S.C. Sealfon, and J.A. Gingrich Neuron 53 2007 439
2. M.M. Herth, F. Debus, M. Piel, M. Palner, G.M. Knudsen, H. Luddens, and F. Rosch Bioorg. Med. Chem. Lett. 18 2008 1515
3. F. Debus, M.M. Herth, M. Piel, H.G. Buchholz, N. Bausbacher, V. Kramer, H. Luddens, and F. Rosch Nucl. Med. Biol. 37 2010 487
4. M.M. Herth, V. Kramer, M. Piel, M. Palner, P.J. Riss, G.M. Knudsen, and F. Rosch Bioorg. Med. Chem. 17 2009 2989
5. J.C. Baron, Y. Samson, D. Comar, C. Crouzel, P. Deniker, and Y. Agid Rev. Neurol. 141 1985 537
6. R.A. Lyon, M. Titeler, J.J. Frost, P.J. Whitehouse, D.F. Wong, H.N. Wagner, R.F. Dannals, J.M. Links, and M.J. Kuhar J. Neurosci. 6 1986 2941
7. C. Lemaire, R. Cantineau, M. Guillaume, A. Plenevaux, and L. Christiaens J. Nucl. Med. 32 1991 2266
8. C. Lundkvist, C. Halldin, N. Ginovart, S. Nyberg, C.G. Swahn, A.A. Carr, F. Brunner, and L. Farde Life Sci. 58 1996 l187
9. M.M. Herth, M. Piel, F. Debus, U. Schmitt, H. Luddens, and F. Rosch Nucl. Med. Biol. 36 2009 447
10. A. Ettrup, S. Cunha-Bang, B. McMahon, S. Lehel, A. Dyssegaard, A.W. Skibsted, L.M. Jørgensen, M. Hansen, A.O. Baandrup, S. Bache, C. Svarer, J.L. Kristensen, N. Gillings, J. Madsen, and G.M. Knudsen JCBFM 34 2014 1188
11. J.G. Goldman, and S. Holden Curr. Treat. Options Neurol. 16 2014
12. G. Fenelon, and G. Alves J. Neurol. Sci. 289 2010 12
13. K.E. Vanover, D.M. Weiner, M. Makhay, I. Veinbergs, L.R. Gardell, J. Lameh, A.L. del Tredici, F. Piu, H.H. Schiffer, T.R. Ott, E.S. Burstein, A.K. Uldam, M.B. Thygesen, N. Schlienger, C.M. Andersson, T.Y. Son, S.C. Harvey, S.B. Powell, M.A. Geyer, B.R. Tolf, M.R. Brann, and R.E. Davis J. Pharmacol. Exp. Ther. 317 2006 910
14. J.H. Friedman Expert Opin. Pharmacother. 14 2013 1969
15. J. Cummings, S. Isaacson, R. Mills, H. Williams, K. Chi-Burris, A. Corbett, R. Dhall, and C. Ballard Lancet 383 2014 533
16. A. Ettrup, B.R. Kornum, P. Weikop, and G.M. Knudsen Synapse 65 2011 136
17. H.D. Hansen, A. Ettrup, M.M. Herth, A. Dyssegaard, C. Ratner, N. Gillings, and G.M. Knudsen Synapse 67 2013 328