Central serotonergic S2 binding in Papio anubis measured in vivo with and PET

作者: Stephen M. Moerlein , Joel S. Perlmutter

DOI: 10.1016/0304-3940(91)90149-N

关键词:

摘要: Abstract N-ω-[ 18 F]fluoroethylketanserin ([18F]FEK), an 18F-labeled analogue of the serotonin S2 antagonist ketanserin, was evaluated for use with positron emission tomography (PET). PET imaging a baboon brain following injection [18F]FEK indicated that fluorinated ligand rapidly localized in vivo within receptor-rich tissues ( frontal cortex cerebellum radioactivity ratio = 2.5 after 15 min), and selective localization retained as long 3 h post injection. Pretreatment unlabeled ketanserin (15 mg/kg, i.v.) 1 prior to completely abolished radiotracer, whereas regional cerebral blood flow, volume, free fraction arterial were unaltered. has several advantages compared previously used radiopharmaceuticals, may be excellent radioligand non-invasive evaluation binding vivo.

参考文章(18)
HeinzH. Coenen, Klaus Wienhard, Gerhard St�cklin, Peter Laufer, Ira Hebold, G�nter Pawlik, Wolf-Dieter Heiss, PET measurement of D2 and S2 receptor binding of 3-N-[( 2'-18F]fluoroethyl)spiperone in baboon brain. European Journal of Nuclear Medicine and Molecular Imaging. ,vol. 14, pp. 80- 87 ,(1988) , 10.1007/BF00253446
J.E. Leysen, F. Awouters, L. Kennis, P.M. Laduron, J. Vandenberk, P.A.J. Janssen, Receptor binding profile of R 41 468, A novel antagonist at 5-HT2 receptors Life Sciences. ,vol. 28, pp. 1015- 1022 ,(1981) , 10.1016/0024-3205(81)90747-5
Dean F Wong, Henry N Wagner Jr, Robert F Dannals, Jonathan M Links, J James Frost, Hayden T Ravert, Alan A Wilson, Arthur E Rosenbaum, Albert Gjedde, Kenneth H Douglass, John D Petronis, Marshal F Folstein, JK Thomas Toung, Michael J Kuhar, Effects of age on dopamine and serotonin receptors measured by positron tomography in the living human brain Science. ,vol. 226, pp. 1393- 1396 ,(1984) , 10.1126/SCIENCE.6334363
Dean F. Wong, John R. Lever, Paul R. Hartig, Robert F. Dannals, Victor Villemagne, Beth J. Hoffman, Alan A. Wilson, Hayden T. Ravert, Jonathan M. Links, Ursula Scheffel, Henry N. Wagner, Localization of serotonin 5‐HT2 receptors in living human brain by positron emission tomography using N1‐([11C]‐methyl)‐2‐BR‐LSD Synapse. ,vol. 1, pp. 393- 398 ,(1987) , 10.1002/SYN.890010502
Tatsuo Mita, Susumu Hanada, Naoki Nishino, Takayoshi Kuno, Hisao Nakai, Takashi Yamadori, Yasuhiko Mizoi, Chikako Tanaka, Decreased serotonin S2 and increased dopamine D2 receptors in chronic schizophrenics Biological Psychiatry. ,vol. 21, pp. 1407- 1414 ,(1986) , 10.1016/0006-3223(86)90332-X
A. Schotte, J.M. Maloteaux, P.M. Laduron, Characterization and regional distribution of serotonin S2-receptors in human brain. Brain Research. ,vol. 276, pp. 231- 235 ,(1983) , 10.1016/0006-8993(83)90729-1
Michel M. Ter-Pogossian, David C. Ficke, John T. Hood, Mikio Yamamoto, Nizar A. Mullani, PETT VI: a positron emission tomograph utilizing cesium fluoride scintillation detectors. Journal of Computer Assisted Tomography. ,vol. 6, pp. 125- 133 ,(1982) , 10.1097/00004728-198202000-00021
A. J. Cross, T. J. Crow, I. N. Ferrier, J. A. Johnson, S. R. Bloom, J. A. N. Corsellis, Serotonin receptor changes in dementia of the Alzheimer type. Journal of Neurochemistry. ,vol. 43, pp. 1574- 1581 ,(1984) , 10.1111/J.1471-4159.1984.TB06081.X
Tom O. Videen, Joel S. Perlmutter, Peter Herscovitch, Marcus E. Raichle, Brain blood volume, flow, and oxygen utilization measured with 15O radiotracers and positron emission tomography: revised metabolic computations. Journal of Cerebral Blood Flow and Metabolism. ,vol. 7, pp. 513- 516 ,(1987) , 10.1038/JCBFM.1987.97
Richard A. Glennon, Central serotonin receptors as targets for drug research. Journal of Medicinal Chemistry. ,vol. 30, pp. 1- 12 ,(1987) , 10.1021/JM00384A001