Autoradiographic evaluation of [3H]CUMI-101, a novel, selective 5-HT1AR ligand in human and baboon brain

Brain Research

Volumn 1507, Issue , 2013, Pages 11-18

  Kumar, J S Dileep ^a,b   Parsey, Ramin V ^c   Kassir, Suham A ^a   Majo, Vattoly J ^b   Milak, Matthew S ^a,b   Prabhakaran, Jaya ^b   Simpson, Norman R ^a   Underwood, Mark D ^a,b   Mann, J John ^a,b   Arango, Victoria ^a,b  

^a NEW YORK STATE PSYCHIATRIC INSTITUTE   (United States)

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

^c STONY BROOK UNIVERSITY   (United States)

Author keywords

5 HT1AR; Autoradiography; Brain; Serotonin Agonist

Indexed keywords

2 DIPROPYLAMINO 8 HYDROXYTETRALIN; ALPHA 1 ADRENERGIC RECEPTOR; CUMI 101 H 3; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; PRAZOSIN; RADIOLIGAND; SEROTONIN 1A AGONIST; SEROTONIN 1A RECEPTOR; UNCLASSIFIED DRUG; (O METHYL 11C) 2 (4 (4 (3 METHOXYPHENYL)PIPERAZIN 1 YL) BUTYL) 4 METHYL 2H (1,2,4) TRIAZINE 3,5 DIONE; (O-METHYL-11C) 2-(4-(4-(3-METHOXYPHENYL)PIPERAZIN-1-YL)-BUTYL)-4-METHYL-2H-(1,2,4)-TRIAZINE-3,5-DIONE; LIGAND; PIPERAZINE DERIVATIVE; SEROTONIN 1 AGONIST; TRIAZINE DERIVATIVE; TRITIUM;

ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; BABOON; BINDING AFFINITY; BRAIN REGION; CADAVER; DRUG RECEPTOR BINDING; DRUG SCREENING; HUMAN; HUMAN TISSUE; IN VITRO STUDY; NONHUMAN; PRIORITY JOURNAL; QUANTITATIVE ANALYSIS; ANIMAL; BRAIN; HISTOLOGY; METABOLISM; PARTIAL AGONISM; POSITRON EMISSION TOMOGRAPHY; SCINTISCANNING;

PAPIO; PRIMATES;

ANIMALS; AUTORADIOGRAPHY; BRAIN; DRUG PARTIAL AGONISM; HUMANS; LIGANDS; PAPIO; PIPERAZINES; POSITRON-EMISSION TOMOGRAPHY; RECEPTOR, SEROTONIN, 5-HT1A; SEROTONIN 5-HT1 RECEPTOR AGONISTS; TRIAZINES; TRITIUM;

EID: 84875835204     PISSN: 00068993     EISSN: 18726240     Source Type: Journal    
DOI: 10.1016/j.brainres.2013.02.035     Document Type: Article

References (49)

1. E. Akimova, R. Lanzenberger, and S. Kasper The serotonin-1A receptor in anxiety disorders Biol. Psychiatry 66 2009 627 635
2. V. Arango, P. Ernsberger, A.F. Sved, and J.J. Mann Quantitative autoradiography of alpha 1- and alpha 2-adrenergic receptors in the cerebral cortex of controls and suicide victims Brain Res. 630 1993 271 282
3. V. Arango, M.D. Underwood, A.V. Gubbi, and J.J. Mann Localized alterations in pre- and postsynaptic serotonin binding sites in the ventrolateral prefrontal cortex of suicide victims Brain Res. 688 1995 121 133
4. E. Assem-Hilger, R. Lanzenberger, M. Savli, W. Wadsak, M. Mitterhauser, L.K. Mien, E. Stogmann, C. Baumgartner, K. Kletter, and S. Asenbaum Central serotonin 1A receptor binding in temporal lobe epilepsy: a [carbonyl-(11)C]WAY- 100635 PET study Epilepsy Behav. 19 2010 467 473
5. 3H]-8-OH-DPAT binding in the rat brain raphe area: involvement of 5-HT1A and non-5-HT1A receptors Br. J. Pharmacol. 130 2000 1348 1352
6. M. Boldrini, M.D. Underwood, J.J. Mann, and V. Arango Serotonin-1A autoreceptor binding in the dorsal raphe nucleus of depressed suicides J. Psychiatr. Res. 42 2008 433 442
7. 3H]8-OH-DPAT and demonstration of increased binding in the frontal cortex in schizophrenia Neurochem. Int. 30 1997 565 574.
8. B.R. Chemel, B.L. Roth, B. Armbruster, V.J. Watts, and D.E. Nichols WAY-100635 is a potent dopamine D4 receptor agonist Psychopharmacology (Berl) 188 2006 244 251
9. A. Drago, D.D. Ronchi, and A. Serretti 5-HT1A gene variants and psychiatric disorders: a review of current literature and selection of SNPs for future studies Int. J. Neuropsychopharmacol. 11 2008 701 721
10. 3H-zolpidem binding in the rat and human brain Pharmacol. Biochem. Behav. 60 1998 439 448
11. M.S. Elliott, C.G. Ballard, R.N. Kalaria, R. Perry, T. Hortobagyi, and P.T. Francis Increased binding to 5-HT1A and 5-HT2A receptors is associated with large vessel infarction and relative preservation of cognition Brain 132 2009 1858 1865
12. G. Giovacchini, S. Conant, P. Herscovitch, and W.H. Theodore Using cerebral white matter for estimation of nondisplaceable binding of 5-HT1A receptors in temporal lobe epilepsy J. Nucl. Med. 50 2009 1794 1800
13. 3H]WAY 100635 labels both G-protein-coupled and free 5-HT1A receptors in rat brain membranes Eur. J. Pharmacol. 288 1995 173 186
14. 11C]WAY-100635 Brain Res. 745 1997 96 108
15. M. Hamon, H. Gozlan, S. el Mestikawy, M.B. Emerit, F. Bolanos, and L. Schechter The central 5-HT1A receptors: pharmacological, biochemical, functional, and regulatory properties Ann. NY Acad. Sci. 600 1990 114 131
16. P. Heusler, I. Rauly-Lestienne, A. Tourette, S. Tardif, M.C. Ailhaud, G. Croville, and D. Cussac Actions of the prototypical 5-HT1A receptor agonist 8-OH-DPAT at human alpha2-adrenoceptors: (+)8-OH-DPAT, but not (-)8-OH-DPAT is an alpha2B subtype preferential agonist Eur. J. Pharmacol. 640 2010 8 14
17. C.S. Hines, J.S. Liow, P. Zanotti-Fregonara, J. Hirvonen, C. Morse, V.W. Pike, and R.B. Innis Human biodistribution and dosimetry of (1)(1)C-CUMI-101, an agonist radioligand for serotonin-1a receptors in brain PLoS One 6 2011 e25309
18. 3H]WAY-100635, a selective 5-HT1A receptor antagonist Brain Res. 673 1995 217 225
19. J.S.D. Kumar, M.S. Milak, V.J. Majo, J. Prabhakaran, M. Pratap, L. Savenkova, J.J. Mann, and R.V. Parsey Comparison of high and low affinity serotonin 1A receptors by PET in vivo in nonhuman primates J. Pharmacol. Sci. 120 2012 254 257
20. 11C]CUMI-101 Int. J. Toxicol. 30 2011 611 618
21. 11C]2-{4-[4-(7- methoxynaphthalen-1-yl)piperazin-1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3, 5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand J. Med. Chem. 49 2006 125 134
22. J.S. Kumar, and J.J. Mann PET tracers for 5-HT(1A) receptors and uses thereof Drug Discovery Today 12 2007 748 756
23. 11C]2-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-4-methyl-1,2, 4-triazine-3,5(2H,4H)dio ne one in nonhuman primates Eur. J. Nucl. Med. Mol. Imaging 34 2007 1050 1060
24. 11C-CUMI-101, an agonist radioligand for serotonin 5-HT1A receptors J. Nucl. Med. 51 2010 164
25. M.C. Michel, G. Hanft, and G. Grob Radioligand binding studies of α1-adrenoceptor subtypes in rat heart Br. J. Pharmacol. 111 1994 533 538
26. 11C-CUMI-101, an agonist radiotracer for imaging serotonin 1A receptor in vivo with PET J. Nucl. Med. 49 2008 587 596
27. 11C-CUMI-101, an agonist PET radiotracer J. Nucl. Med. 51 2010 1892 1900
28. 11C]CUMI-101: a serotonin 1A receptor agonist positron emission tomography radiotracer J. Cereb. Blood Flow Metab. 31 2011 243 249
29. M.J. Millan Improving the treatment of schizophrenia: focus on serotonin (5-HT)(1A) receptors J. Pharmacol. Exp. Ther. 295 2000 853 861
30. A. Munoz, T. Carlsson, E. Tronci, D. Kirik, A. Bjorklund, and M. Carta Serotonin neuron-dependent and -independent reduction of dyskinesia by 5-HT1A and 5-HT1B receptor agonists in the rat parkinson model Exp. Neurol. 219 2009 298 307
31. T. Nagai, R. Murai, K. Matsui, H. Kamei, Y. Noda, H. Furukawa, and T. Nabeshima Aripiprazole ameliorates phencyclidine-induced impairment of recognition memory through dopamine D1 and serotonin 5-HT1A receptors Psychopharmacology (Berl.) 202 2009 315 328
32. 11C]-raclopride Synapse 52 2004 188 208
33. 3H]hydroxydipropylaminotetralin J. Neurochem. 62 1994 1822 1834
34. H. Ohira, M. Matsunaga, K. Kimura, H. Murakami, T. Osumi, T. Isowa, S. Fukuyama, J. Shinoda, and J. Yamada Chronic stress modulates neural and cardiovascular responses during reversal learning Neuroscience 193 2011 193 204
35. 11C]WAY-100635 in humans: comparison of arterial and reference tissue input functions J. Cereb. Blood Flow Metab. 20 2000 1111 1133
36. J.M. Palacios, D. Hoyer, and R. Cortés Alpha 1-adrenoceptors in the mammalian brain: similar pharmacology but different distribution in rodents and primates Brain Res. 419 1987 65 75
37. V.W. Pike, C. Halldin, and H.V. Wikstrom Radioligands for the study of brain 5-HT1A receptors in vivo Prog. Med. Chem. 38 2001 189 247
38. L.H. Pinborg, L. Feng, M. Haahr, N. Gillings, A. Ettrup, H.D. Hansen, S. Yndgaard, C. Svarer, and G.M. Knudsen No change in [(11) C]CUMI-101 binding to 5-HT(1A) receptors after intravenous citalopram in human Synapse 66 2012 880 884
39. J.W. Richardson-Jones, C.P. Craige, B.P. Guiard, A. Stephen, K.L. Metzger, H.F. Kung, A.M. Gardier, A. Dranovsky, D.J. David, S.G. Beck, R. Hen, and E.D. Leonardo 5-HT1A autoreceptor levels determine vulnerability to stress and response to antidepressants Neuron 65 2010 40 52
40. 11C]WAY 100635 Int. J. Neuropsychopharmacol. 13 2010 785 791
41. P.A. Sargent, E.A. Rabiner, Z. Bhagwagar, L. Clark, P. Cowen, G.M. Goodwin, and P.M. Grasby 5-HT(1A) receptor binding in euthymic bipolar patients using positron emission tomography with [carbonyl-(11)C]WAY-100635 J. Affect. Disord. 123 2010 77 80
42. C.W. Schindler, S.R. Tella, and S.R. Goldberg Adrenoceptor mechanisms in the cardiovascular effects of cocaine in conscious squirrel monkeys Life Sci. 51 1992 653 660
43. 3H]8-OH-DPAT labels the serotonin transporter in the rat striatum Eur. J. Pharmacol. 124 1986 371 373
44. 11C]CUMI-101 PET challenge study Mol. Psychiatry 12 2012 1 7
45. 3H]8-OH-DPAT reveals increases in 5-HT(1A) receptors in ventral prefrontal cortex in schizophrenia Biol. Psychiatry 39 1996 919 928
46. J. Sprouse, L. Reynolds, X. Li, J. Braselton, and A. Schmidt 8-OH-DPAT as a 5-HT7 agonist: phase shifts of the circadian biological clock through increases in cAMP production Neuropharmacology 46 2004 52 62
47. 11C]WAY-100635 Eur. J. Nucl. Med. Mol. Imaging 35 2008 2159 2168
48. P. Szot, S.S. White, J.L. Greenup, J.B. Leverenz, E.R. Peskind, and M.A. Raskind A1-adrenoreceptor in human hippocampus: Binding and receptor subtype mRNA expression Mol. Brain Res. 139 2005 367 371
49. A.C. Trillat, I. Malagie, M. Mathe-Allainmat, M.C. Anmela, C. Jacquot, M. Langlois, and A.M. Gardier Effects of WAY 100635 and (-)-5-Me-8-OH-DPAT, a novel 5-HT1A receptor antagonist, on 8-OH-DPAT responses Eur. J. Pharmacol. 347 1998 41 49