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Nuclear Medicine and Biology
Volume 34, Issue 5
, Pages 559-570
, July 2007
Radiosynthesis and biological evaluation of an 18F-labeled derivative of the novel pyrazolopyrimidine sedative–hypnotic agent indiplon
References
- . Consequences of the evolution of the GABAA receptor gene family. Cell Mol Neurobiol. 2005;25:607–624
- . GABAA receptor channel pharmacology. Curr Pharm Des. 2005;11:1867–1885
- . Sleep, epilepsy and thalamic reticular inhibitory neurons. Trends Neurosci. 2005;28:317–324
- . Selective GABAergic treatment for panic? Investigations in experimental panic induction and panic disorder. J Psychiatry Neurosci. 2005;30:167–175
- Gamma-aminobutyric acid type A receptors and alcoholism: intoxication, dependence, vulnerability, and treatment. Arch Gen Psychiatry. 2006;63:957–968
- . Alcohol, GABA receptors, and neurodevelopmentaldisorders. Int Rev Neurobiol. 2005;71:217–237
- . GABAA-receptor subtypes: a new pharmacology. Curr Opin Pharmacol. 2001;1:22–25
- . Development of effective therapeutics targeting the GABAA receptor: naturally occurring alternatives. Curr Pharm Des. 2004;10:1035–1044
- . Variations on an inhibitory theme: phasic and tonic activation of GABAA receptors. Nat Rev Neurosci. 2005;6:215–229
- . The distribution of 13 GABAA receptor subunit mRNAs in the rat brain. I. Telencephalon, diencephalon, mesencephalon. J Neurosci. 1992;12:1040–1062
- . Ion channels and epilepsy. Curr Pharm Des. 2005;11:1975–2003
- . Synthesis of ethyl 8-fluoro-5,6-dihydro-5-[11C]methyl-6-oxo-4H-imidazo [1,5-a] [1,4]benzodiazepine-3-carboxylate (RO 15.1788-11C): a specific radioligand for the in vivo study of central benzodiazepine receptors by positron emission tomography. Int J Appl Radiat Isot. 1984;35:973–976
- . Is central benzodiazepine receptor imaging useful for the identification of epileptogenic foci in localization-related epilepsies?. Eur J Nucl Med Mol Imaging. 2003;30:325–328
- . PET in neuroscience: dopaminergic. GABA/benzodiazepine, and opiate system. Nuklearmedizin. 2004;43:33–42
- . Development of radioligands for in vivo imaging of GABAA-benzodiazepine receptors. Mini Rev Med Chem. 2004;4:909–921
- Radiosynthesis of 3-(2′-[18F]fluoro)-flumazenil ([18F]FFMZ). J Label Compd Radiopharm. 2003;46:1229–1240
- Novel one-pot one-step synthesis of 2′-[18F]fluoroflumazenil (FFMZ) for benzodiazepine receptor imaging. Nucl Med Biol. 2003;30:521–527
- . Binding of 5-(2′-[18F]fluoroethyl)flumazenil to central benzodiazepine receptors measured in living baboon by positron emission tomography. Eur J Pharmacol. 1992;218:109–115
- [18F]Fluoroethylflumazenil: a novel tracer for PET imaging of human benzodiazepine receptors. Eur J Nucl Med. 2001;28:1463–1470
- Preparation of highly specific radioactivity [18F]flumazenil and its evaluation in cynomolgus monkey by positron emission tomography. Nucl Med Biol. 2005;32:109–116
- Biological properties of 2′-[18F]fluoroflumazenil for central benzodiazepine receptor imaging. Nucl Med Biol. 2005;32:263–268
- Biological evaluation of 2′-[18F]fluoroflumazenil ([18F]FFMZ), a potential GABA receptor ligand for PET. Nucl Med Biol. 2004;31:291–295
- . Characterization of the interaction of indiplon, a novel pyrazolopyrimidine sedative-hypnotic, with the GABAA receptor. J Pharmacol Exp Ther. 2004;311:537–546
- Indiplon is a high-affinity positive allosteric modulator with selectivity for α1 subunit containing GABAA receptors. J Pharmacol Exp Ther. 2006;317:369–377
- Thiele WJ, O'Donnell PB. Polymorphs of N-methyl-N-(3-(3-[2-thienylcarbonyl]-pyrazol-[1,5-a]-pyrimidin-7-yl) phenyl)acetamide and compositions and methods related thereto. Neurocrine Biosciences, Inc., US Patent 6,384,221, 2002.
- . Substitution–reduction: an alternative process for the [18F]N-(2-fluoroethylation) of anilines. J Label Compd Radiopharm. 2004;47:217–232
- . GABAA receptor subtypes: autoradiographic comparison of GABA, benzodiazepine, and convulsant binding sites in the rat central nervous system. J Chem Neuroanat. 1990;3:59–76
- . Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (IC50) of an enzymatic reaction. Biochem Pharmacol. 1973;22:3099–3108
- CambridgeSoft Corporation. CS ChemDraw Ultra chemical structure drawing standard. www.camsoft.com, 1998.
- . Interconversion of lipophilicities from hydrocarbon–water systems into octanol–water system. Eur J Med Chem. 1974;9:473–479
- Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists. J Med Chem. 1988;31:656–671
- Status epilepticus induced by pentylenetetrazole modulates in vivo [11C]Ro 15-1788 binding to benzodiazepine receptors. Effects of ligands acting at the supramolecular receptor complex. Eur J Pharmacol. 1988;146:207–214
- . In vivo demonstration of reduced benzodiazepine receptor binding in human epileptic foci. Lancet. 1988;2:863–866
- . Brain imaging in idiopathic generalized epilepsies. Epilepsia. 2005;46(Suppl 9):108–111
- Positron emission tomography measures of benzodiazepine receptors in Huntington's disease. Ann Neurol. 1993;34:76–81
- Benzodiazepine receptor binding in Huntington's disease: [11C]flumazenil uptake measured using positron emission tomography. Ann Neurol. 2000;47:644–648
- . Positron emission tomography measures of benzodiazepine binding in Alzheimer's disease. Arch Neurol. 1995;52:314–317
- PET imaging of neuroreceptors in schizophrenia. Eur Neuropsychopharmacol. 1995;5:25–30
- . Relationships between trait and state anxiety and the central benzodiazepine receptor: a PET study in process citation. Eur J Neurosci. 1999;11:1470–1478
- Yohimbine increases the binding potential for [11C]flumazenil in the monkey brain. J Neural Transm. 2001;108:1375–1382
- Measurement of brain concentration of FK960 for development of a novel antidementia drug: a PET study in conscious rhesus monkeys. J Nucl Med. 2003;44:105–108
- . Decreased brain GABAA-benzodiazepine receptor binding in panic disorder: preliminary results from a quantitative PET study. Arch Gen Psychiatry. 1998;55:715–720
- . Positron emission tomography receptor studies. In: Delgado-Escueta AV, Wilson WA, Olsen RW, Porter RJ editor. Jasper's basic mechanisms of the epilepsies. Third edition: advances in neurology. vol 79:Philadelphia: Lippincott Williams & Wilkins; 1999;p. 893–899
- . Abnormalities of gyration, heterotopias, tuberous sclerosis, focal cortical dysplasia, microdysgenesis, dysembryoplastic neuroepithelial tumour and dysgenesis of the archicortex in epilepsy. Clinical, EEG and neuroimaging features in 100 adult patients. Brain. 1995;118:629–660
- . The distribution of thirteen GABAA receptor subunit mRNAs in the rat brain. III. Embryonic and postnatal development. J Neurosci. 1992;12:4151–4172
- . Developmental changes in the expression of GABAA receptor alpha 1 and gamma 2 subunits in human temporal lobe, hippocampus and basal ganglia: an implication for consideration on age-related epilepsy. Epilepsy Res. 2006;71:47–53
- . Increased GABAA-receptor α1-subunit expression in hippocampal dentate gyrus after early-life status epilepticus. Epilepsia. 2006;47:1665–1673
- Enhancing GABAA receptor α1 subunit levels in hippocampal dentate gyrus inhibits epilepsy development in an animal model of temporal lobe epilepsy. J Neurosci. 2006;26:11342–11346
- . Changes of [3H]muscimol, [3H]flunitrazepam and [3H]MK-801 binding in rat brain by prolonged ventricular infusion of 7-nitroindazole. Neurochem Res. 2004;29:2221–2229
- . Learning deficits induced by sleep deprivation and recovery are not associated with altered [3H]muscimol and [3H]flunitrazepam binding. Brain Res. 2005;1037:157–163
- . The neurotoxic effects of 3,4-methylenedioxymethamphetamine (MDMA) and methamphetamine on serotonin, dopamine, and GABA-ergic terminals: an in vitro autoradiographic study in rats. Neurotoxicology. 2004;25:905–914
- . Postnatal maturation of human GABAA receptors measured with positron emission tomography. Ann Neurol. 2001;49:618–626
- GABAA receptor abnormalities in Prader–Willi syndrome assessed with positron emission tomography and [11C]flumazenil. Neuroimage. 2004;22:22–28
- Decrease in cortical benzodiazepine receptors in symptomatic patients with leukoaraiosis: a positron emission tomography study. Stroke. 2004;35:942–947
- GABA-benzodiazepine receptor function in alcohol dependence: a combined 11C-flumazenil PET and pharmacodynamic study. Psychopharmacology (Berl). 2005;180:595–606
- . The heterogeneity of central benzodiazepine receptor subtypes in the human hippocampal formation, frontal cortex and cerebellum using [3H]flumazenil and zolpidem. Mol Brain Res. 2002;104:203–209
- . A PET radiotracer for studying serotonin uptake sites: carbon-11-McN-5652Z. J Nucl Med. 1993;34:121–127
- . Neuroimaging of the serotonin transporter — possibilities and pitfalls. Curr Psychiat Rev. 2006;2:111–149
- Synthesis and in vivo evaluation of [11C]zolpidem, an imidazopyridine with agonist properties at central benzodiazepine receptors. Nucl Med Biol. 2003;30:435–439
- In vivo pharmacological characterization of indiplon, a novel pyrazolopyrimidine sedative–hypnotic. J Pharmacol Exp Ther. 2004;311:547–559
- . Indiplon: the development of a new hypnotic. Expert Opin Investig Drugs. 2005;14:1269–1276
- . Preferential labeling of glial and meningial brain tumors with [2-14C]acetate. J Nucl Med. 2001;42:1243–1250
- . Evaluation of radiolabeled acetate and fluoroacetate as potential tracers of cerebral oxidative metabolism. Metab Brain Dis. 1990;5:45–56
PII: S0969-8051(07)00093-5
doi: 10.1016/j.nucmedbio.2007.03.011
« Previous
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Nuclear Medicine and Biology
Volume 34, Issue 5
, Pages 559-570
, July 2007
