Imaging of [11C]-labelled RO 15-1788 binding to benzodiazepine receptors in the human brain by positron emission tomography

Persson, A.; Ehrin, E.; Eriksson, Lars; Farde, Lars; Hedström, Carl-Göran; Litton, Jan-Eric; Mindus, Per; Sedvall, Göran

doi:10.1016/0022-3956(85)90080-9

Cited by 167 publications

(62 citation statements)

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Section: Proof-of-concept In Humansmentioning

confidence: 99%

“…For example, in the case of the α4β2 nAChR radiotracer (-)-[ 18 F]flubatine, the time between the first report on radiosynthesis [164] and the fi rst report on human use [16] years [210,272] , and for [ 18 F]FEOBV [126] , a radiotracer for the VAChT, it has been almost 20 years [273] . At the beginning of neuroreceptor imaging with PET this transition time was much shorter, in the range of 1-2 years as exemplifi ed by [ 11 C]raclopride [225,274] , 3-N-[ 11 C]methylspiperone [224] , and [ 11 C]fl umazenil [49,275] .However, even if a radiotracer is not further developed into a radiopharmaceutical for imaging in human subjects it may fi nd widespread use in preclinical studies with special animal PET devices [276] to investigate animal models of diseases [7] or new drugs [8,252] . The foremost importance of this approach is the diagnosis and therapeutic monitoring of brain diseases.…”

mentioning

confidence: 99%

“…Acetylcholine receptor: muscarinic [N-11 C-methyl]-benztropine Xie et al 2004 [10] Histamine receptor: H3 [ 11 C]GSK189254 Ashworth et al 2010 [48] GABA-benzodiazepine receptor: α1 [ 11 C]fl umazenil Persson et al 1985 [49] GABA-benzodiazepine receptor: α1 [ 18 F]fl uoroethyl-fl umazenil Leveque et al 2003 [50] GABA-benzodiazepine receptor: α1 [ 18 F]fl uorofl umazenil Lee et al 2007 [51] GABA-benzodiazepine receptor: α1 [ 18 F]fl umazenil Massaweh et al 2009 [52] GABA-benzodiazepine receptor: α5 [ 11 C]Ro15-4513 Lingford-Hughes e al. 2002 [53] Opioid receptor: μ [ 11 C]carfentanil Frost et al 1990 [54] Opioid receptor: δ [ 11 C]methylnaltrindol Madar et al 1997 [55] Opioid receptor: κ [ 11 C]GR103545 Tomasi et al 2010 [56] Opioid receptor: unselective [ 11 C]diprenorphine Frost et al 1990 [54] Opioid receptor: unselective…”

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Development of 18F-labeled radiotracers for neuroreceptor imaging with positron emission tomography

2014

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Positron emission tomography (PET) is an in vivo molecular imaging tool which is widely used in nuclear medicine for early diagnosis and treatment follow-up of many brain diseases. PET uses biomolecules as probes which are labeled with radionuclides of short half-lives, synthesized prior to the imaging studies. These probes are called radiotracers. Fluorine-18 is a radionuclide routinely used in the radiolabeling of neuroreceptor ligands for PET because of its favorable half-life of 109.8 min. The delivery of such radiotracers into the brain provides images of transport, metabolic, and neurotransmission processes on the molecular level. After a short introduction into the principles of PET, this review mainly focuses on the strategy of radiotracer development bridging from basic science to biomedical application. Successful radiotracer design as described here provides molecular probes which not only are useful for imaging of human brain diseases, but also allow molecular neuroreceptor imaging studies in various small-animal models of disease, including geneticallyengineered animals. Furthermore, they provide a powerful tool for in vivo pharmacology during the process of pre-clinical drug development to identify new drug targets, to investigate pathophysiology, to discover potential drug candidates, and to evaluate the pharmacokinetics and pharmacodynamics of drugs in vivo.Keywords: Alzheimer's disease; autoradiography; blood-brain barrier; brain tumor; cholinergic system; kinetic modeling; metabolism; molecular imaging; neurodegeneration; positron emission tomography; precursor; psychiatric disorder; radiotracer; sigma receptor ·Review· IntroductionPositron emission tomography (PET) is an in vivo molecular imaging tool widely used in nuclear medicine for early diagnosis and treatment follow-up of many brain diseases. Positron-emitting radionuclide-labeled substances allow the visualization, characterization, and measurement of biological processes at the molecular and cellular levels in humans and other living systems by highly sensitive coincidence-detection [1] . This is based on 511 keV photons (gamma radiation) originating from positronelectron annihilation. PET differs in that aspect from other modalities such as single-photon emission computed tomography (SPECT), magnetic resonance imaging (MRI), optical imaging, and ultrasound. Because of their high sensitivity (~10 -9 to 10 -12 M) PET and SPECT offer advantages over the other methods. Therefore, in the past, they were the only modalities that allowed noninvasive imaging of biochemical receptor sites. Nowadays, the other imaging modalities compete in that aspect although precise absolute quantitation in terms of biochemical parameters has not been achieved yet. fusion accuracy, provides an advanced diagnostic tool and research platform [2,3] .PET and SPECT use biomolecules as probes, labeled with radionuclides of short half-lives, synthesized prior to the imaging studies. These probes are called radiotracers. According to the concept developed by George ...

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Section: Proof-of-concept In Humansmentioning

confidence: 99%

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confidence: 99%

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Development of 18F-labeled radiotracers for neuroreceptor imaging with positron emission tomography

2014

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“…Benzodiazepines act at specific receptor sites on the gamma-aminobutyric acid (GABA) A receptor complex by facilitating the action of GABA, the primary inhibitory neurotransmitter in the central nervous system (CNS) (Mohler and Okada 1977;Squires and Braestrup 1977). Benzodiazepine receptors are distributed widely throughout the brain, and, therefore, the initial sites of benzodiazepine action in the brain are known (Fernandez-Lopez et al 1997;Frey et al 1996;Millet et al 2000;Persson et al 1985). Nonetheless, little is known about the brain circuitry affected by benzodiazepine administration during episodic memory encoding, because the distribution of such effects likely goes beyond the sites of initial receptor interactions.…”

Section: It Is Well Documented That Acute Administration Of the Benzomentioning

confidence: 99%

“…Benzodiazepine receptors are distributed widely throughout the brain, and, therefore, the initial sites of benzodiazepine action in the brain are known (Fernandez-Lopez et al 1997;Frey et al 1996;Millet et al 2000;Persson et al 1985). Nonetheless, little is known about the brain circuitry affected by benzodiazepine administration during episodic memory encoding, because the distribution of such effects likely goes beyond the sites of initial receptor interactions.…”

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Effects of Triazolam on Brain Activity During Episodic Memory Encoding: A PET Study

Mintzer

Griffiths

Contoreggi

et al. 2001

Neuropsychopharmacology

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It is well documented that acute administration of the benzodiazepine hypnotic drug triazolam (Halcion®) impairs episodic memory encoding. We examined the neuroanatomical substrates of this effect in healthy adult volunteers using a double-blind, within-subject design. Following oral capsule administration (0.25 mg/70 kg triazolam or placebo), regional cerebral blood flow (rCBF) was measured using positron emission tomography (PET) withBenzodiazepine anxiolytic/hypnotic drugs, such as diazepam (Valium®), alprazolam (Xanax®), lorazepam (Ativan®), and triazolam (Halcion®), are among the most widely prescribed psychotropic medications. In addition to their anxiolytic and sedative properties, benzodiazepines also have memory-and cognitiveimpairing effects (for reviews see Curran 1991;Duka et al. 1996;Polster 1993). Acute benzodiazepine administration produces dose-related decrements in episodic memory encoding, while leaving retrieval of previously encoded material intact. Episodic memory refers to conscious long-term memory for a personally experienced event that is associated with a specific spatial and temporal context (Tulving 1972(Tulving , 1983. Encoding refers to the cognitive processes engaged (either intentionally or unintentionally) during the initial event that lead to the creation of a representation or trace of the event in epi- N EUROPSYCHOPHARMACOLOGY 2001 -VOL . 25 , NO . 5 Triazolam and PET 745 sodic memory. Thus, if information is presented for study while a participant is under the influence of a benzodiazepine, subsequent memory for that information is impaired, even when memory testing occurs while the drug is no longer in the system; however, if information presented before drug administration is tested under the influence of a benzodiazepine, no impairment is observed. Benzodiazepines act at specific receptor sites on the gamma-aminobutyric acid (GABA) A receptor complex by facilitating the action of GABA, the primary inhibitory neurotransmitter in the central nervous system (CNS) (Mohler and Okada 1977;Squires and Braestrup 1977). Benzodiazepine receptors are distributed widely throughout the brain, and, therefore, the initial sites of benzodiazepine action in the brain are known (Fernandez-Lopez et al. 1997;Frey et al. 1996;Millet et al. 2000;Persson et al. 1985). Nonetheless, little is known about the brain circuitry affected by benzodiazepine administration during episodic memory encoding, because the distribution of such effects likely goes beyond the sites of initial receptor interactions.Over the past decade, considerable progress has been made in identifying the brain regions involved in episodic memory encoding under nonpharmacological conditions using noninvasive functional neuroimaging techniques, such as positron emission tomography (PET) and functional magnetic resonance imaging (fMRI), which enable measurement of brain activity in vivo while a human subject performs specific tasks. Encoding has been investigated most commonly by comparing brain activity associated with a cond...

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Positron Emission Tomography Measures of Benzodiazepine Binding in Alzheimer's Disease

Meyer¹,

Koeppe²,

Frey³

et al. 1995

Archives of Neurology

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Imaging of [11C]-labelled RO 15-1788 binding to benzodiazepine receptors in the human brain by positron emission tomography

Cited by 167 publications

References 18 publications

Development of 18F-labeled radiotracers for neuroreceptor imaging with positron emission tomography

Development of 18F-labeled radiotracers for neuroreceptor imaging with positron emission tomography

Effects of Triazolam on Brain Activity During Episodic Memory Encoding: A PET Study

Positron Emission Tomography Measures of Benzodiazepine Binding in Alzheimer's Disease

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