Evaluation of 11C-BU99008, a PET Ligand for the Imidazoline 2 Binding Sites in Rhesus Brain

Journal of Nuclear Medicine

Volumn 55, Issue 5, 2014, Pages 838-844

  Parker, Christine A ^a,b   Nabulsi, Nabeel ^c   Holden, Daniel ^c   Lin, Shu Fei ^c   Cass, Tara ^c   Labaree, David ^c   Kealey, Steven ^d   Gee, Antony D ^e   Husbands, Stephen M ^f   Quelch, Darren ^a   Carson, Richard E ^c   Nutt, David J ^a   Huang, Yiyun ^c   Tyacke, Robin J ^a  

^a HAMMERSMITH HOSPITAL   (United Kingdom)

^b GLAXOSMITHKLINE   (United Kingdom)

^c YALE UNIVERSITY   (United States)

^d KING'S COLLEGE LONDON   (United Kingdom)

^e ST THOMAS HOSPITAL   (United Kingdom)

^f University of Bath   (United Kingdom)

Author keywords

BU99008; I2BS; PET; Positron emission tomography

Indexed keywords

2 (2 IMIDAZOLIN 2 YL)QUINOLINE; AMINE OXIDASE (FLAVIN CONTAINING) ISOENZYME A; AMINE OXIDASE (FLAVIN CONTAINING) ISOENZYME B; CARBON 2 (4,5 DIHYDRO 1H IMIDAZOL 2 YL) 1 METHYL 1H INDOLE C 11; CARRIER PROTEINS AND BINDING PROTEINS; IMIDAZOLINE 2 BINDING SITE; RADIOLIGAND; UNCLASSIFIED DRUG; 2 (4,5 DIHYDRO 1H IMIDAZOL 2 YL) 1 METHYL 1H INDOLE; 2-(4,5-DIHYDRO-1H-IMIDAZOL-2-YL)-1-METHYL-1H-INDOLE; CARBON; DIAGNOSTIC AGENT; IMIDAZOLE DERIVATIVE; IMIDAZOLINE DERIVATIVE; INDOLE DERIVATIVE; LIGAND;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BINDING COMPETITION; BINDING SITE; CEREBELLUM; CONTROLLED STUDY; DRUG BINDING; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG PENETRATION; DRUG SCREENING; DRUG SYNTHESIS; ENZYME INHIBITION; FEMALE; FRONTAL CORTEX; GLOBUS PALLIDUS; HUMAN; HUMAN TISSUE; IC 50; IN VITRO STUDY; IN VIVO STUDY; ISOTOPE LABELING; MACACA FASCICULARIS; NEUROIMAGING; NONHUMAN; NUCLEAR MAGNETIC RESONANCE IMAGING; NUCLEAR MAGNETIC RESONANCE SCANNER; PET SCANNER; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN EXPRESSION; PROTEIN LOCALIZATION; RADIATION DETECTION; RADIOCHEMISTRY; RAT; RHESUS MONKEY; ANIMAL; BRAIN; BU99008; CELL MEMBRANE; CHEMISTRY; EVALUATION STUDY; I2BS; IMIDAZOLINE2 BINDING SITE; METABOLISM; METHYLATION; PET; SCINTISCANNING; TISSUE DISTRIBUTION;

BU99008; I2BS; IMIDAZOLINE2 BINDING SITE; PET; POSITRON EMISSION TOMOGRAPHY;

ANIMALS; BINDING SITES; BINDING, COMPETITIVE; BRAIN; CARBON RADIOISOTOPES; CELL MEMBRANE; FEMALE; IMIDAZOLES; IMIDAZOLINES; INDOLES; LIGANDS; MACACA MULATTA; MAGNETIC RESONANCE IMAGING; METHYLATION; POSITRON-EMISSION TOMOGRAPHY; RATS; TISSUE DISTRIBUTION;

EID: 84901361656     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: 10.2967/jnumed.113.131854     Document Type: Article

References (20)

1. Eglen RM, Hudson AL, Kendall DA, et al. 'Seeing through a glass darkly': casting light on imidazoline 'I' sites. Trends Pharmacol Sci. 1998;19:381-390.
2. Regunathan S, Feinstein DL, Reis DJ. Expression of non-adrenergic imidazoline sites in rat cerebral cortical astrocytes. J Neurosci Res. 1993;34:681-688.
3. García-Sevilla JA, Escriba PV, Guimon J. Imidazoline receptors and human brain disorders. Ann N Y Acad Sci. 1999;881:392-409.
4. Ruiz-Durántez E, Torrecilla M, Pineda J, Ugedo L. Attenuation of acute and chronic effects of morphine by the imidazoline receptor ligand 2-(2-benzofuranyl)-2-imidazoline in rat locus coeruleus neurons. Br J Pharmacol. 2003;138:494-500.
5. Hudson AL, Gough R, Tyacke R, et al. Novel selective compounds for the investigation of imidazoline receptors. Ann N Y Acad Sci. 1999;881:81-91.
6. Hudson AL, Nutt DJ, Husbands SM. Imidazoline receptors and their role in depression. Pharm News. 2001;8:26-32.
7. Olmos G, Alemany R, Escriba PV, Garcia-Sevilla JA. The effects of chronic imidazoline drug treatment on glial fibrillary acidic protein concentrations in rat brain. Br J Pharmacol. 1994;111:997-1002.
8. Martín-Gómez JI, Ruiz J, Callado LF, et al. Increased density of I2-imidazoline receptors in human glioblastomas. Neuroreport. 1996;7:1393-1396.
9. Martín-Gómez JI, Ruiz J, Barrondo S, Callado LF, Meana JJ. Opposite changes in imidazoline I2 receptors and alpha2-adrenoceptors density in rat frontal cortex after induced gliosis. Life Sci. 2005;78:205-209.
10. Callado LF, Martin-Gomez JI, Ruiz J, Garibi JM, Meana JJ. Imidazoline I2 receptor density increases with the malignancy of human gliomas. J Neurol Neurosurg Psychiatry. 2004;75:785-787.
11. Roeda D, Hinnen F, Dolle F. Radiosynthesis of a 2-substituted 4,5-dihydro-1H-[2-C-11] imidazole: the I-2 imidazoline receptor ligand [Cl-11 benazoline. J Labelled Compd Rad. 2003;46:1141-1149.
12. Kawamura K, Maeda J, Hatori A, et al. In vivo and in vitro imaging of I2 imidazoline receptors in the monkey brain. Synapse. 2011;65:452-455.
13. Tyacke RJ, Fisher A, Robinson ES, et al. Evaluation and initial in vitro and ex vivo characterization of the potential positron emission tomography ligand, BU99008 (2-(4,5-dihydro-1H-imidazol-2-yl)-1-methyl-1H-indole), for the imidazoline (2) binding site. Synapse. 2012;66:542-551.
14. Kealey S, Turner EM, Husbands SM, et al. Imaging imidazoline-I2 binding sites in porcine brain using 11C-BU99008. J Nucl Med. 2013;54:139-144.
15. Sandiego CM, Weinzimmer D, Carson RE. Optimization of PET-MR registrations for nonhuman primates using mutual information measures: a multi-transform method (MTM). Neuroimage. 2013;64:571-581.
16. Ichise M, Toyama H, Innis RB, Carson RE. Strategies to improve neuroreceptor parameter estimation by linear regression analysis. J Cereb Blood Flow Metab. 2002;22:1271-1281.
17. Cunningham VJ, Rabiner EA, Slifstein M, Laruelle M, Gunn RN. Measuring drug occupancy in the absence of a reference region: the Lassen plot re-visited. J Cereb Blood Flow Metab. 2010;30:46-50.
18. De Vos H, Convents A, De Keyser J, et al. Autoradiographic distribution of alpha 2 adrenoceptors, NAIBS, and 5-HT1A receptors in human brain using [3H]idazoxan and [3H]rauwolscine. Brain Res. 1991;566:13-20.
19. Paterson LM, Tyacke RJ, Robinson ES, Nutt DJ, Hudson AL. In vitro and in vivo effect of BU99006 (5-isothiocyanato-2-benzofuranyl-2-imidazoline) on I2 binding in relation to MAO: evidence for two distinct I2 binding sites. Neuropharmacology. 2007;52:395-404.
20. Bonivento D, Milczek EM, McDonald GR, et al. Potentiation of ligand binding through cooperative effects in monoamine oxidase B. J Biol Chem. 2010;285: 36849-36856.