[18F]p-MPPF: A radiolabeled antagonist for the study of 5-HT(1A) receptors with PET

Nuclear Medicine and Biology

Volumn 27, Issue 5, 2000, Pages 467-471

  Plenevaux, A ^a   Lemaire, C ^a   Aerts, J ^a   Lacan, G ^b   Rubins, D ^b   Melega, W P ^b   Brihaye, C ^a   Degueldre, C ^a   Fuchs, S ^a   Salmon, E ^a   Maquet, P ^a   Laureys, S ^a   Damhaut, P ^c   Weissmann, D ^d   Le Bars, D ^e   Pujol, J F ^e   Luxen, A ^a  

^a UNIVERSITY OF LIÈGE   (Belgium)

^b UNIVERSITY OF CALIFORNIA   (United States)

^c ERASME HOSPITAL   (Belgium)

^d UNIVERSITÉ LYON 1   (France)

^e CERMEP IMAGERIE DU VIVANT   (France)

Author keywords

5 HT(1A); Fluorine 18; MicroPET; MPPF; PET; Receptor

Indexed keywords

4 (2 METHOXYPHENYL) 1 [2 [N (2 PYRIDINYL) 4 FLUOROBENZAMIDO]ETHYL] PIPERAZINE F 18; RADIOLIGAND; SEROTONIN 1A ANTAGONIST; SEROTONIN 1A RECEPTOR; UNCLASSIFIED DRUG; 4 (2' METHOXYPHENYL) 1 (2' (N (2'' PYRIDINYL) 4 FLUOROBENZAMIDO)ETHYL)PIPERAZINE; 4-(2' METHOXYPHENYL)-1-(2'-(N-(2''-PYRIDINYL)-4-FLUOROBENZAMIDO)ETHYL)PIPERAZINE; AMINOPYRIDINE DERIVATIVE; DIAGNOSTIC AGENT; FLUORINE; LIGAND; PIPERAZINE DERIVATIVE; SEROTONIN 1 RECEPTOR; SEROTONIN ANTAGONIST; SEROTONIN RECEPTOR;

AUTORADIOGRAPHY; CHEMICAL ANALYSIS; CHEMICAL STRUCTURE; DRUG METABOLISM; HUMAN; NEUROTRANSMISSION; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; RADIOCHEMISTRY; REVIEW; SEROTONINERGIC SYSTEM; STOICHIOMETRY; STRUCTURE ACTIVITY RELATION; SYNTHESIS; ANIMAL; ARTICLE; BRAIN LEVEL; CAT; COMPUTER ASSISTED EMISSION TOMOGRAPHY; METABOLISM; RAT;

AMINOPYRIDINES; ANIMALS; AUTORADIOGRAPHY; BRAIN CHEMISTRY; CATS; FLUORINE RADIOISOTOPES; HUMANS; LIGANDS; PIPERAZINES; RATS; RECEPTORS, SEROTONIN; RECEPTORS, SEROTONIN, 5-HT1; SEROTONIN ANTAGONISTS; TOMOGRAPHY, EMISSION-COMPUTED;

EID: 0033624539     PISSN: 09698051     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0969-8051(00)00113-X     Document Type: Article

References (23)

1. Brihaye C., Lemaire C. and Luxen A. (1995) Robot-assisted synthesis of radiopharmaceuticals labeled with high activity positron emitters. International Symposium on Laboratory Automation and Robotics, Boston, MA, October, 1995.
2. Cherry S.R., Shao Y., Silverman R.W., Chatziioannou A., Meadors K., Siegel S., Boutefnouchet A., Farquhar T., Young J., Jones W.F., Newport D., Moyers C., Andreaco M., Paulus M., Binkley D., Nutt R., Phelps M.E. MicroPET A high resolution PET scanner for imaging small animals . IEEE Transactions on Nuclear Science. 44:1997;1161-1166.
3. Damhaut P., Plenevaux A., Lemaire C., Aerts J., Biver F., Monclus M., Luxen A., Goldman S. In vivo studies of [18F]p-MPPF metabolites in human. J. Labelled Compds. Radiopharm. 42:(suppl 1):1999;S661-S662.
4. Fuchs S., Plenevaux A., Degueldre C., Lemaire C., Aerts J., Laureys S., Salmon E., Maquet P., Le Bars D., Pujol J.-F., Luxen A. 5-HT1A receptor distribution in the human brain Preliminary PET data with p-[18F]MPPF . Society for Neuroscience. 25:1999;1462.
5. Gardner J.P., Fornal C.A., Jacobs B.L. Effects of sleep deprivation on serotoninergic neuronal activity in the dorsal raphe nucleus of the freely moving cat. Neuropsychopharmacology. 17:1997;72-81.
6. Ginovart N., Hassoun W., Le Bars D., Weissmann D., Leviel V. In vivo characterization of p-[18F]MPPF, a fluoro analog of WAY-100635 for visualization of 5-HT1A receptors. Synapse. 35:2000;192-200.
7. Glennon R.A. Serotonin receptors Clinical implications . Neurosci. Biobehav. Rev. 14:1990;35-47.
8. Hillver S., Bjork L., Li Y., Svensson B., Ross S., Andèn N., Hacksell U. (S)-5-Fluoro-8-hydroxy-2-(dipropylamino)tertralin A putative 5-HT1A receptor antagonist . J. Med. Chem. 33:1990;1541-1544.
9. Kostowski W., Plaznik A., Archer T. Possible implication of 5-HT1A function for the etiology and treatment of depression. New Trends Exp. Clin. Psychiatry. 5:1989;91-116.
10. Kung H.F., Stevenson D.A., Zhuang Z.P., Kung M.P., Frederick D., Hurt S.D. New 5-HT1A receptor antagonist [3H]p-MPPF . Synapse. 23:1996;344-346.
11. Le Bars D., Lemaire C., Ginovart N., Plenevaux A., Aerts J., Brihaye C., Hassoun W., Leviel V., Mekhsian P., Weissmann D., Pujol J.-F., Luxen A., Comar D. High yield radiosynthesis and preliminary in vivo evaluation of p-[18F]MPPF, a fluoro analog of WAY 100635. Nucl. Med. Biol. 25:1998;343-350.
12. Lemaire C., Plenevaux A., Aerts J., Del Fiore G., Brihaye C., Le Bars D., Comar D., Luxen A. Solid phase extraction - An alternative to the use of rotary evaporators for solvent removal in the rapid formulation of PET radiopharmaceuticals. J. Labelled Compds. Radiopharm. 42:1999;63-75.
13. Meneses A., Hong E. Role of 5-HT1A receptors in acquisition, consolidation and retrieval of learning. CNS Drug Reviews. 3:1997;68-82.
14. Passchier J., van Waarde A., Pieterman R.M., Elsinga P., Hendrikse H.N., Pruim J., Willemsen A.T., Vaalburg W. Delineation of serotonin 5-HT1A receptors in human brain with [18F]MPPF. J. Nucl. Med. 40:1999;29P.
15. Peroutka S.J. Serotonin receptor subtypes. Their evolution and clinical relevance. CNS Drugs. 4:1995;18-28.
16. Plenevaux A., Aerts J., Lemaire C., Brihaye C., Le Bars D., Mekhsian P., Weissmann D., Pujol J.-F., Comar D. and Luxen A. (1997) Evaluation of p-[F-18]MPPF, 5-HT1A antagonist, in rats: Tissue distribution, autoradiography and metabolism. The Society of Nuclear Medicine 44th Annual Meeting, San Antonio, 1-5 June. J. Nucl. Med. 38, 56P.
17. Plenevaux A., Lemaire C., Salmon E., Laureys S., Fuchs S., Maquet P., Degueldre C., Aerts J., Brihaye C., Damhaut P., Biver F., Goldman S., Le Bars D., Ginovart N., Cinotti L., Pujol J.-F., Luxen A. 5-HT1A receptors visualization with p-[18F]MPPF in healthy volunteers. J. Labelled Compds. Radiopharm. 42:(suppl 1):1999;S60-S62.
18. Saudou F., Hen R. 5-Hydroxytryptamine receptor subtypes in vertebrates and invertebrates. Neurochem. Int. 25:1994;503-532.
19. Saxena P.R. Serotonin receptors Subtypes, functional response and therapeutic relevance . Pharmacol. Ther. 66:1995;339-368.
20. Seifritz E., Stahl M.S., Gillin J.C. Human sleep EEG following the 5-HT1A antagonist pindolol Possible disinhibition of raphe neuron activity . Brain Res. 759:1997;84-91.
21. Shiue C.-Y., Shiue G.G., Mozley P.D., Kung M.-P., Zhuang Z.-P., Kim H.-J., Kung H.F. p-[18F]-MPPF A potential radioligand for PET studies of 5-HT1A receptors in humans . Synapse. 25:1997;147-154.
22. Thielen R.J., Fangon N.B., Frazer A. 4-(2′-Methoxyphenyl)-1-[2′-[N-(2′′-pyridinyl)-p- iodobenzamido]ethyl]piperazine and 4-(2′-methoxyphenyl)-1-[2′-[N-(2′′-pyridinyl)-p- fluorobenzamido] ethyl]piperazine, two new antagonists at pre- and postsynaptic serotonin-1A receptors. J. Pharmacol. Exp. Ther. 277:1996;661-670.
23. Zhuang Z.P., Kung M.P., Kung H.F. Synthesis and evaluation of 4-(2′-methoxyphenyl)-1-[2′-[N-(2′′-pyridinyl)-p- iodobenzamido]ethyl]piperazine (p-MPPI) A new iodinated 5-HT1A ligand . J. Med. Chem. 37:1994;1406-1407.