Utility of small-animal positron emission tomographic imaging of rats for preclinical development of drugs acting on the serotonin transporter

International Journal of Neuropsychopharmacology

Volumn 12, Issue 8, 2009, Pages 1021-1032

  Saijo, Takeaki ^a,b,c   Maeda, Jun ^a   Okauchi, Takashi ^a   Maeda, Jun Ichi ^c   Morio, Yasunori ^c   Kuwahara, Yasuhiro ^c   Suzuki, Masayuki ^c   Goto, Nobuharu ^c   Suzuki, Kazutoshi ^a   Higuchi, Makoto ^a,b   Suhara, Tetsuya ^a,b  

^a NATIONAL INSTITUTE OF RADIOLOGICAL SCIENCES   (Japan)

^b TOHOKU UNIVERSITY SCHOOL OF MEDICINE   (Japan)

^c MITSUBISHI TANABE PHARMA CORPORATION   (Japan)

Author keywords

Fluvoxamine; Occupancy; Serotonin transporter (5 HTT); Small animal PET; Wf 516

Indexed keywords

1 [4 (3,4 DICHLOROPHENYL)PIPERIDIN 1 YL] 3 [2 (5 METHYL 1,3,4 OXADIAZOL 2 YL)BENZO[B]FURAN 4 YLOXY]PROPAN 2 OL MONOHYDROCHLORIDE; AMINO 4 (2 DIMETHYLAMINOMETHYL PHENYLSULFANYL)BENZONITRILE CARBON 11; ANTIDEPRESSANT AGENT; FLUVOXAMINE; RADIOLIGAND; SEROTONIN TRANSPORTER; UNCLASSIFIED DRUG; WF 516;

ANIMAL EXPERIMENT; ARTICLE; BLOOD LEVEL; CONTROLLED STUDY; DRUG BINDING; DRUG DOSE COMPARISON; EX VIVO STUDY; EXPERIMENTAL ANIMAL; IN VIVO STUDY; MALE; NEUROTRANSMISSION; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; QUANTITATIVE ANALYSIS; RAT; THERAPY EFFECT;

ANESTHETICS, INHALATION; ANIMALS; ANTIDEPRESSIVE AGENTS; BENZYLAMINES; BRAIN; BRAIN MAPPING; CARBON ISOTOPES; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG INTERACTIONS; FLUVOXAMINE; ISOFLURANE; MALE; OXADIAZOLES; PIPERIDINES; POSITRON-EMISSION TOMOGRAPHY; PROTEIN BINDING; RATS; RATS, WISTAR; SEROTONIN PLASMA MEMBRANE TRANSPORT PROTEINS; TIME FACTORS; WAKEFULNESS;

EID: 69849109791     PISSN: 14611457     EISSN: 14695111     Source Type: Journal    
DOI: 10.1017/S1461145709000042     Document Type: Article

References (44)

1. Arendt RM, Greenblatt DJ, Liebisch DC, Luu MD, Paul SM (1987). Determinants of benzodiazepine brain uptake: lipophilicity versus binding affinity. Psychopharmacology (Berlin) 93, 72-76.
2. Arguello PA, Gogos JA (2006). Schizophrenia: modeling a complex psychiatric disorder. Disease Models 3, 319-325.
3. 11C]flumazenil micro-positron emission tomography. Journal of Pharmacology and Experimental Therapeutics 320, 1030-1037.
4. D'Amato RJ, Blue ME, Largent BL, Lynch DR, Ledbetter DJ, Molliver ME, Snyder SH (1987). Ontogeny of the serotonergic projection to rat neocortex: transient expression of a dense innervation to primary sensory areas. Proceedings of the National Academy of Sciences USA 84, 4322-4326.
5. Deussing JM (2006). Animal models of depression. Disease Models 3, 375-383.
6. 3H-zolpidem binding in the rat and human brain. Pharmacology Biochemistry and Behavior 60, 439-448.
7. Duyk G (2003). Attrition and translation. Science 302, 603-605.
8. El Mansari M, Blier P (2008). In vivo electrophysiological assessment of the putative antidepressant Wf-516 in the rat raphe dorsalis, locus coeruleus and hippocampus. Naunyn-Schmiedeberg's Archives of Pharmacology 376, 351-361.
9. Farde L, Wiesel FA, Halldin C, Sedvall G (1998). Central D2-dopamine receptor occupancy in schizophrenic patients treated with antipsychotic drugs. Archives of General Psychiatry 45, 71-76.
10. Fowler JS, Volkow ND, Wang GJ, Ding YS, Dewey SL (1999). PET and drug research and development. Journal of Nuclear Medicine 40, 1154-1163.
11. 11C]-DASB binding to the human serotonin transporter: modeling strategies. Journal of Cerebral Blood Flow and Metabolism 21, 1342-1353.
12. 11C]-DASB, a tool for in vivo measurement of SSRI-induced occupancy of the serotonin transporter: PET characterization and evaluation in cats. Synapse 47, 123-133.
13. Herschman HR (2003). Molecular imaging: looking at problems, seeing solutions. Science 302, 605-608.
14. 1A receptors measured in vivo using small animal positron emission tomography with carbon-11 labeled WAY 100635. Synapse 36, 330-341.
15. 11C]AFM. Journal of Cerebral Blood Flow & Metabolism 22, 1377-1398.
16. Hume SP, Gunn RN, Jones T (1998). Pharmacological constraints associated with positron emission tomographic scanning of small laboratory animals. European Journal of Nuclear Medicine 25, 173-176.
17. Hurko O, Ryan JL (2005). Translational research in central nervous system drug discovery. NeuroRx 2, 671-682.
18. 11C]DASB positron emission tomography studies of the serotonin transporter in human brain. Journal of Cerebral Blood Flow & Metabolism 23, 1096-1112.
19. Jagoda EM, Vaquero JJ, Seidel J, Green MV, Eckelman WC (2004). Experiment assessment of mass effects in the rat: implications for small animal PET imaging. Nuclear Medicine and Biology 31, 771-779.
20. Johnson RF, Schenker S, Roberts RK, Desmond PV, Wilkinson GR (1979). Plasma binding of benzodiazepines in humans. Journal of Pharmaceutical Sciences 68, 1320-1322.
21. Kapur S, Zipursky R, Jones C, Remington G, Houle S (2000). Relationship between dopamine D(2) occupancy, clinical response, and side effects: a double-blind PET study of first-episode schizophrenia. American Journal of Psychiatry 157, 514-520.
22. Kung MP, Kung HF (2005). Mass effect of injected dose in small rodent imaging by SPECT and PET. Nuclear Medicine and Biology 32, 673-678.
23. 11C] raclopride studies. Journal of Cerebral Blood Flow and Metabolism 16, 42-52.
24. 123I-ADAM and the relationship to the serotonin transporter in rat and mouse brains using quantitative autoradiography. Journal of Nuclear Medicine 45, 673-681.
25. 11C]flumazenil PET to demonstrate that pagoclone is a partial agonist. Psychopharmacology 180, 789-791.
26. 11C]DASB binding after tranylcypromine-induced increase in serotonin concentration: Positron emission tomography Studies in monkeys and rats. Synapse 61, 440-449.
27. MaedaJ, Ji B, Irie T, Tomiyama T, Maruyama M, Okauchi T, Staufenbiel M, Iwata N, Ono M, Saido TC, Suzuki K, Mori H, Higuchi M, Suhara T (2007). Longitudinal, quantitative assessment of amyloid, neuroinflammation, and anti-amyloid treatment in a living mouse model of Alzheimer's disease enabled by positron emission tomography. Journal of Neuroscience 27, 10957-10968.
28. Maeda J, Morio Y, Oohashi Y, Katayama J, Nishiyama A, Yamagami K, Saito K (2006a). Wf-516, a novel antidepressant with dual serotonergic activity: l. Receptorial and pharmacological profiles in comparison with reference antidepressants. European Neuropsychopharmacology 16, S333.
29. Maeda J, Morio Y, Katayama J, Horie S, Inaba K, Nishiyama A, Eguchi J, Saito K (2006b). Wf-516, a novel antidepressant with dual serotonergic activity: II. Pharmacological profiles ex vivo and in vivo to monoamine transporters in comparison with standard antidepressant. European Neuropsychopharmacology 16, S333-S334.
30. McArthur R, Borsini F (2006). Animal models of depression in drug discovery: a historical perspective. Pharmacology Biochemistry & Behavior 84, 436-452.
31. 11C]DASB positron emission tomography study. American Journal of Psychiatry 161, 826-835.
32. Rupniak NM (2003). Animal models of depression: challenges from a drug development perspective. Behavioural Pharmacology 14, 385-390.
33. Sato N, Takata H, Tsukui M, Tatebayashi T, Fuji K, Hiranuma T, Aizawa K, Nakayoshi T (1995). Studies on the pharmacokinetics of fluvoxamine maleate. (3) Plasma concentration profile and brain distribution in rats. Japanese Pharmacology and Therapeutics 23, 637-643.
34. Stehouwer JS, Jarkas N, Zeng F, Voll RJ, Williams L, Camp VM, Malveaux EJ, Votaw JR, Howell L, Owens MJ, Goodman MM (2008). Synthesis, radiosynthesis, and biological evaluation of fluorine-18-labeled 2beta-carbo(fluoroalkoxy)- 3beta-(3'-((Z)-2-haloethenyl)phenyl)nortropanes: candidate radioligands for in vivo imaging of the serotonin transporter with positron emission tomography. Journal of Medicinal Chemistry 51, 7788-7799.
35. Suhara T, Takano A, Sudo Y, Ichimiya T, Inoue M, Yasuno F, Ikoma Y, Okubo Y (2003). High levels of serotonin transporter occupancy with low-dose clomipramine in comparative occupancy study with fluvoxamine using positron emission tomography. Archives of General Psychiatry 60, 386-391.
36. Tai YC, Ruangma A, Rowland D, Siegel S, Newport DF, Chow PL, Laforest R (2005). Performance evaluation of the microPET focus: a third-generation microPET scanner dedicated to animal imaging. Journal of Nuclear Medicine 46, 455-463.
37. Takano A, Suhara T, Ichimiya T, Yasuno F, Suzuki K (2006). Time course of in vivo 5-HTT transporter occupancy by fluvoxamine. Journal of Clinical Psychopharmacology 26, 188-191.
38. Takano A, Suhara T, Ikoma Y, Yasuno F, Maeda J, Ichimiya T, Sudo Y, Inoue M, Okubo Y (2004). Estimation of the time-course of dopamine D2 receptor occupancy in living human brain from plasma pharmacokinetics of antipsychotics. International Journal of Neuropsychopharmacology 7, 19-26.
39. van Harten J (1995). Overview of the pharmacokinetics of fluvoxamine. Clinical Pharmacokinetics 29 (Suppl. 1), 1-9.
40. Wang J, Maurer L (2005). Positron emission tomography: applications in drug discovery and drug development. Current Topics in Medicinal Chemistry 5, 1053-1075. (Pubitemid 41582120)
41. Wilde MI, Plosker GL, Benfield P (1993). Fluvoxamine: an updated review of its pharmacology, and therapeutic use in depressive illness. Drugs 46, 895-924.
42. 11C]-DASB: a probe for in vivo measurements of the serotonin transporter by positron emission tomography. Nuclear Medicine and Biology 29, 509-515.
43. 11C-labeled 2-(phenylthio) araalkylamines. Journal of Medicinal Chemistry 43, 3103-3110.
44. Yang Y, Tai YC, Siegel S, Newport DF, Bai B, Li Q, Leahy RM, Cherry SR (2004). Optimization and performance evaluation of the microPET II scanner for in vivo small-animal imaging. Physics in Medicine & Biology 49, 2527-2545.