Evaluation of potential PET imaging probes for the orexin 2 receptors

Nuclear Medicine and Biology

Volumn 40, Issue 8, 2013, Pages 1000-1005

  Wang, Changning ^a   Wilson, Colin M ^a   Moseley, Christian K ^a   Carlin, Stephen M ^a   Hsu, Shirley ^a   Arabasz, Grae ^a   Schroeder, Frederick A ^a   Sander, Christin Y ^a,b   Hooker, Jacob M ^a  

^a MASSACHUSETTS GENERAL HOSPITAL   (United States)

^b Massachusetts Institute of Technology   (United States)

Author keywords

Carbon 11; Hypocretin; Imaging; Orexin; PET radiotracers

Indexed keywords

CARBON 11; CARBON CW3 C 11; CARBON CW4 C 11; CARBON CW6 C 11; OREXIN 2 RECEPTOR; RADIOPHARMACEUTICAL AGENT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; BIOACCUMULATION; BLOOD BRAIN BARRIER; COMPLEX FORMATION; CONTROLLED STUDY; DRUG ACCUMULATION; DRUG DETERMINATION; DRUG IDENTIFICATION; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG UPTAKE; FEMALE; ISOTOPE LABELING; MALE; MOLECULAR PROBE; NONHUMAN; NUCLEAR MAGNETIC RESONANCE IMAGING; PAPIO ANUBIS; PHYSICAL CHEMISTRY; POSITRON EMISSION TOMOGRAPHY; RADIOASSAY; RADIOISOTOPE DECAY; RADIOISOTOPE DISTRIBUTION; RAT; RECEPTOR DENSITY; SCINTILLATION PROBE;

CARBON-11; HYPOCRETIN; IMAGING; OREXIN; PET RADIOTRACERS;

ANIMALS; AZEPINES; BLOOD-BRAIN BARRIER; DRUG DESIGN; MALE; OREXIN RECEPTORS; PAPIO; POSITRON-EMISSION TOMOGRAPHY; RADIOCHEMISTRY; RATS; TOMOGRAPHY, X-RAY COMPUTED;

EID: 84886254913     PISSN: 09698051     EISSN: 18729614     Source Type: Journal    
DOI: 10.1016/j.nucmedbio.2013.07.001     Document Type: Article

References (17)

1. de Lecea L., et al. The hypocretins: hypothalamus-specific peptides with neuroexcitatory activity. Proc Natl Acad Sci U S A 1998, 95(1):322-327.
2. Alexander S.P., Mathie A., Peters J.A. Guide to Receptors and Channels (GRAC), 3rd edition. Br J Pharmacol 2008, 153(Suppl 2):S1-S209.
3. Siegel J.M. Hypocretin (orexin): role in normal behavior and neuropathology. Annu Rev Psychol 2004, 55:125-148.
4. Marcus J.N., et al. Differential expression of orexin receptors 1 and 2 in the rat brain. J Comp Neurol 2001, 435(1):6-25.
5. Nishino S. The hypocretin/orexin receptor: therapeutic prospective in sleep disorders. Expert Opin Investig Drugs 2007, 16(11):1785-1797.
6. Hirose M., et al. N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist. Bioorg Med Chem Lett 2003, 13(24):4497-4499.
7. Brisbare-Roch C., et al. Promotion of sleep by targeting the orexin system in rats, dogs and humans. Nat Med 2007, 13(2):150-155.
8. Winrow C.J., et al. Promotion of sleep by suvorexant-a novel dual orexin receptor antagonist. J Neurogenet 2011, 25(1-2):52-61.
9. Herring W.J., et al. Orexin receptor antagonism for treatment of insomnia: A randomized clinical trial of suvorexant. Neurology 2012, 79(23):2265-2274.
10. Bettica P., et al. The orexin antagonist SB-649868 promotes and maintains sleep in men with primary insomnia. Sleep 2012, 35(8):1097-1104.
11. Bettica P., et al. Differential effects of a dual orexin receptor antagonist (SB-649868) and zolpidem on sleep initiation and consolidation, SWS, REM sleep, and EEG power spectra in a model of situational insomnia. Neuropsychopharmacology 2012, 37(5):1224-1233.
12. Bettica P., et al. Phase I studies on the safety, tolerability, pharmacokinetics and pharmacodynamics of SB-649868, a novel dual orexin receptor antagonist. J Psychopharmacol 2012, 26(8):1058-1070.
13. Malherbe P., et al. Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor. Br J Pharmacol 2009, 156(8):1326-1341.
14. Liu F., et al. Radiosynthesis of [11C]BBAC and [11C]BBPC as potential PET tracers for orexin2 receptors. Bioorg Med Chem Lett 2012, 22(6):2172-2174.
15. Ghose A.K., et al. Knowledge-based, central nervous system (CNS) lead selection and lead optimization for CNS drug discovery. ACS Chem Neurosci 2012, 3(1):50-68.
16. Whitman D.B., et al. Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n, n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats. ChemMedChem 2009, 4(7):1069-1074.
17. Constantinescu C.C., et al. Striatal and extrastriatal microPET imaging of D2/D3 dopamine receptors in rat brain with [(1)(8)F]fallypride and [(1)(8)F]desmethoxyfallypride. Synapse 2011, 65(8):778-787.