Ex vivo evaluation of the serotonin 1A receptor partial agonist [3H]CUMI-101 in awake rats

Synapse

Volumn 65, Issue 8, 2011, Pages 715-723

  Palner, Mikael ^a,b,c   Underwood, Mark D ^a,b   Kumar, Dileep J S ^a,b   Arango, Victoria ^a,b   Knudsen, Gitte M ^c   John Mann, J ^a,b   Parsey, Ramin V ^a,b  

^a NEW YORK STATE PSYCHIATRIC INSTITUTE   (United States)

^b Columbia University College of Physicians and Surgeons ^*  (United States)

^c Rigshospitalet   (Denmark)

Author keywords

4 chloro DL phenylalanine; 5 HT1A; Citalopram; CUMI 101; Depletion; Ex vivo; Fenfluramine; MMP; Positron emission tomography (positronemissiontomography); Serotonin

Indexed keywords

8 HYDROXY 2 PROPYLAMINOTETRALIN; [2 [4 (4 METHYL 2 METHOXYPHENYL)PIPERAZIN 1 YL]BUTYL] 4 METHYL 1,2,4 TRIAZINE 3,5(2H,4H) DIONE; [2 [4 (4 METHYL 2 METHOXYPHENYL)PIPERAZIN 1 YL]BUTYL] 4 METHYL 1,2,4 TRIAZINE 3,5(2H,4H) DIONE H 3; CITALOPRAM; CUMI 101; FENFLURAMINE; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; PARTIAL AGONIST; RADIOLIGAND; SEROTONIN; SEROTONIN 1A AGONIST; SEROTONIN 1A RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BRAIN REGION; CEREBELLUM; CONTROLLED STUDY; CORPUS STRIATUM; DRUG BINDING SITE; DRUG UPTAKE; EVALUATION; EX VIVO STUDY; FRONTAL CORTEX; HIPPOCAMPUS; IN VITRO STUDY; MALE; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RAT; RECEPTOR DENSITY; SINGLE DRUG DOSE; SYNAPSE; WAKEFULNESS;

ANIMALS; BRAIN; CONSCIOUSNESS; MALE; RADIOPHARMACEUTICALS; RATS; RATS, SPRAGUE-DAWLEY; SEROTONIN 5-HT1 RECEPTOR AGONISTS; TRITIUM;

EID: 79957865096     PISSN: 08874476     EISSN: 10982396     Source Type: Journal    
DOI: 10.1002/syn.20888     Document Type: Article

References (36)

1. Borg J. 2008. Molecular imaging of the 5-HT(1A) receptor in relation to human cognition. Behav Brain Res 195: 103-111.
2. Brunelli SA, Aviles JA, Gannon KS, Branscomb A, Shacham S. 2009. PRX-00023, a selective serotonin 1A receptor agonist, reduces ultrasonic vocalizations in infant rats bred for high infantile anxiety. Pharmacol Biochem Behav 94: 8-15.
3. Ceglia I, Acconcia S, Fracasso C, Colovic M, Caccia S, Invernizzi RW. 2004. Effects of chronic treatment with escitalopram or citalopram on extracellular 5-HT in the prefrontal cortex of rats: Role of 5-HT1A receptors. Br J Pharmacol 142: 469-478.
4. Clawges HM, Depree KM, Parker EM, Graber SG. 1997. Human 5-HT1 receptor subtypes exhibit distinct G protein coupling behaviors in membranes from Sf9 cells. Biochemistry 36: 12930-12938.
5. Cumming P, Wong DF, Gillings N, Hilton J, Scheffel U, Gjedde A. 2002. Specific binding of [(11)C]raclopride and N-[(3)H]propyl-norapomorphine to dopamine receptors in living mouse striatum: Occupancy by endogenous dopamine and guanosine triphosphate-free G protein. J Cereb Blood Flow Metab 22: 596-604.
6. Datla KP, Curzon G. 1996. Effect of p-chlorophenylalanine at moderate dosage on 5-HT and 5-HIAA concentrations in brain regions of control and p-chloroamphetamine treated rats. Neuropharmacology 35: 315-320.
7. Ebenezer IS, Arkle MJ, Tite RM. 2007a. 8-Hydroxy-2-(di-n-propylamino)-tetralin inhibits food intake in fasted rats by an action at 5-HT1A receptors. Methods Find Exp Clin Pharmacol 29: 269-272.
8. Ebenezer IS, Surujbally A. 2007b. The effects of 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) on food intake in non-deprived C57BL6 mice. Eur J Pharmacol 559: 184-188.
9. Elfving B, Bjørnholm B, Knudsen GM. 2003. Interference of anaesthetics with radioligand binding in neuroreceptor studies. Eur J Nucl Med Mol Imag 30: 912-915.
10. Elsinga PH, Hendrikse NH, Bart J, van Waarde A, Vaalburg W. 2005. Positron emission tomography studies on binding of central nervous system drugs and p-glycoprotein function in the rodent brain. Mol Imaging Biol 7: 37-44.
11. Fitzgerald LW, Conklin DS, Krause CM, Marshall AP, Patterson JP, Tran DP, Iyer G, Kostich WA, Largent BL, Hartig PR. 1999. High-affinity agonist binding correlates with efficacy (intrinsic activity) at the human serotonin 5-HT2A and 5-HT2C receptors. Evidence favoring the ternary complex and two-state models of agonist action. J Neurochem 72: 2127-2134.
12. Gozlan H, Thibault S, Laporte AM, Lima L, Hamon M. 1995. The selective 5-HT1A antagonist radioligand [3H]WAY 100635 labels both G-protein-coupled and free 5-HT1A receptors in rat brain membranes. Eur J Pharmacol 288: 173-186.
13. Günther L, Liebscher S, Jähkel M, Oehler J. 2008. Effects of chronic citalopram treatment on 5-HT1A and 5-HT2A receptors in group- and isolation-housed mice. Eur J Pharm 593: 49-61.
14. Huang M, Ichiwaka J, Li Z, Dai J, Meltzer HY. 2006. Augmentation by citalopram of risperidone-induced monoamine release in rat prefrontal cortex. Psychopharmacology 185: 274-281.
15. Hume SP, Ashworth S, Opacka-Juffry J, Ahier RG, Lammertsma AA, Pike VW, Cliffe IA, Fletcher A, White AC. 1994. Evaluation of [O-methyl-3H]WAY-100635 as an in vivo radioligand for 5-HT1A receptors in rat brain. Eur J Pharmacol 271: 515-523.
16. Hume SP, Hirani E, Opacka-Juffry J, Myers R, Townsend C, Pike VW, Grasby P. 2001. Effect of 5-HT on Binding of WAY 100635 toreceptors in rat brain, assessed using in vivo microdialysis. Synapse 41: 150-159.
17. Kornum BR, Licht CL, Weikop P, Knudsen GM, Aznar S. 2006. Central serotonin depletion affects rat brain areas differently: A qualitative and quantitative comparison between different treatment schemes. Neurosci Lett 392: 129-134.
18. Kumar JS, Prabhakaran J, Majo VJ, Milak MS, Hsiung SC, Tamir H, Simpson NR, Van Heertum RL, Mann JJ, Parsey RV. 2007. Synthesis and in vivo evaluation of a novel 5-HT1A receptor agonist radioligand [O-methyl-11C]2-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-4-methyl-1, 2, 4-triazine-3, 5(2H, 4H)dione in nonhuman primates. Eur J Nucl Med Mol Imag 34: 1050-1060.
19. Laferrere B, Wurtman RJ. 1989. Effect of D-fenfluramine on serotonin release in brains of anaesthetized rats. Brain Res 504: 258-263.
20. Liow J, Lu S, Zoghbi S, Shrestha S, Gladding R, Morse C, Hirvonen J, Parsey RV, Pike V, Innis R. 2010. Selectivity in rodents and monkeys of 11C-CUMI-101, an agonist radioligand for serotonin 5-HT1A receptors. Soc Nucl Med Annu Meet Abstr 51: 164.
21. Maeda J, Suhara T, Ogawa M, Okauchi T, Kawabe K, Zhang MR, Semba J, Suzuki K. 2001. In vivo binding properties of [carbonyl-11C]WAY-100635: Effect of endogenous serotonin. Synapse 40: 122-129.
22. Milak MS, Kumar JS, Prabhakaran J, Majo VJ, Mann JJ, Parsey RV. 2008a. [C-11]CUMI-101 an agonist 5-HT1A positron emission tomography (PET) tracer in human: Preliminary test-retest data. Neuroreceptor Mapp 49: 587-596.
23. Milak MS, Severance AJ, Ogden RT, Prabhakaran J, Kumar JS, Majo VJ, Mann JJ, Parsey RV. 2008b. Modeling considerations for 11C-CUMI-101, an agonist radiotracer for imaging serotonin 1A receptor in vivo with PET. J Nucl Med 49: 587-596.
24. Mongeau R, Welner SA, Quirion R, Suranyi-Cadotte BE. 1992. Further evidence for differential affinity states of the serotonin1A receptor in rat hippocampus. Brain Res 590: 229-238.
25. Mørk A, Kreilgaard M, Sánchez C. 2003. The R-enantiomer of citalopram counteracts escitalopram-induced increase in extracellular 5-HT in the frontal cortex of freely moving rats. Neuropharmacology 45: 167-173.
26. Narendran R, Hwang D, Slifstein M, Hwang Y, Huang Y, Ekelund J, Guillin O, Scher E, Martinez D, Laruelle M. 2005. Measurement of the proportion of D2 receptors configured in state of high affinity for agonists in vivo: A positron emission tomography study using [11C]N-propyl-norapomorphine and [11C]raclopride in baboons. J Pharm Exp Therapeut 315: 80-90.
27. Paterson LM, Tyacke RJ, Nutt DJ, Knudsen GM. 2010. Measuring endogenous 5-HT release by emission tomography: Promises and pitfalls. J Cereb Blood Flow Metab 30: 1682-1706.
28. Plenevaux A, Lemaire C, Aerts J, Lacan G, Rubins D, Melega WP, Brihaye C, Degueldre C, Fuchs S, Salmon E, Maquet P, Laureys S, Damhaut P, Weissmann D, Le Bars D, Pujol JF, Luxen A. 2000. [(18)F]p-MPPF: A radiolabeled antagonist for the study of 5-HT(1A) receptors with PET. Nucl Med Biol 27: 467-471.
29. Rice OV, Gatley SJ, Shen J, Huemmer CL, Rogoz R, DeJesus OT, Volkow ND, Gifford AN. 2001. Effects of endogenous neurotransmitters on the in vivo binding of dopamine and 5-HT radiotracers in mice. Neuropsychopharmacology 25: 679-689.
30. Richfield EK, Penney JB, Young AB. 1989. Anatomical and affinity state comparisons between dopamine D1 and D2 receptors in the rat central nervous system. Neuroscience 30: 767-777.
31. Rocher C, Gardier AM. 2001. Effects of repeated systemic administration of d-fenfluramine on serotonin and glutamate release in rat ventral hippocampus: Comparison with methamphetamine using in vivo microdialysis. Naunyn-Schmiedeberg's Arch Pharmacol 363: 422-428.
32. Sumiyoshi T, Bubenikova-Valesova V, Horacek J, Bert B. 2008. Serotonin1A receptors in the pathophysiology of schizophrenia: Development of novel cognition-enhancing therapeutics. Adv Ther 25: 1037-1056.
33. Udo De Haes JI, Cremers TI, Bosker F, Postema F, Tiemersma-Wegman TD, den Boer JA. 2005. Effect of increased serotonin levels on [18F]MPPF binding in rat brain: Fenfluramine vs the combination of Citalopram and ketanserin. Neuropsychopharmacology 30: 1624-1631.
34. Wilson SJ, Bailey JE, Rich AS, Nash J, Adrover M, Tournoux A, Nutt DJ. 2005. The use of sleep measures to compare a new 5HT1A agonist with buspirone in humans. J Psychopharmacol 19: 609-613.
35. Zimmer L, Le Bars D, Mauger G, Luxen A, Bonmarchand G, Pujol J. 2002. Effect of endogenous serotonin on the binding of the 5-hT1A PET ligand 18F-MPPF in the rat hippocampus: Kinetic beta measurements combined with microdialysis. J Neurochem 80: 278-286.
36. Zimmer L, Rbah L, Giacomelli F, Le Bars D, Renaud B. 2003. A reduced extracellular serotonin level increases the 5-HT1A PET ligand 18F-MPPF binding in the rat hippocampus. J Nucl Med 44: 1495.