Central type benzodiazepine binding sites: A positron emission tomography study in the baboon's brain

Hantraye, Philippe; Kaijima, Mitsunobu; Prenant, C.; Guibert, Bernard; Sastre, J.; Crouzel, M.; Naquet, R; Comar, D.; Mazière, M.

doi:10.1016/0304-3940(84)90005-3

Cited by 92 publications

(25 citation statements)

References 15 publications

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“…In all the patients FMZ distribution within the first 2 minutes after bolus injection showed the perfusion pattern to be in excellent agreement with the flow maps obtained after H 2 15 O injection (Figs 1 to 3). The usefulness of FMZ as a tracer of perfusion was further tested by comparing the regional FMZ uptake within the first 2 minutes to the absolute flow values.…”

Section: Compromised Cortical Regions In Individual Patientssupporting

confidence: 74%

“…17 After completion of the 15 O studies, 20 mCi (740 MBq) FMZ was injected intravenously, and the distribution and accumulation of this tracer were followed for 60 minutes by serial scanning. The initial tracer distribution reached within 2 minutes after injection served as an indicator of the perfusion pattern in comparison to the flow values determined by H 2 15 O. BZR density was estimated from the distribution of FMZ 30 to 60 minutes after the bolus injection. 18 In a few cases in which blood samples were available, a two-compartment, two-parameter model could be applied to estimate regional receptor distribution.…”

Section: Radiological Investigationsmentioning

confidence: 99%

“…For both studies arterial blood activity was measured with a commercially available automated blood sampling system. 15 From the multiple brain activity frames accumulated after H 2 15 O injection and 15 O 2 inhalation and the time-activity curves of the blood, the computer (SUN SPARC, Sun Microsystems Inc) after decay correction calculated regional values of CBF, CMRO 2 , and OEF pixel by pixel with the use of the operational equation of Mintun et al 16 Details of these procedures have been described previously. 17 After completion of the 15 O studies, 20 mCi (740 MBq) FMZ was injected intravenously, and the distribution and accumulation of this tracer were followed for 60 minutes by serial scanning.…”

Section: Radiological Investigationsmentioning

confidence: 99%

“…In this article we report the first application of the central BZR ligand FMZ to patients with acute ischemic stroke. The findings are compared with acute changes in rCBF and in rCMRO 2 , with persistent alterations of rCMR glc , and with morphological damage assessed on MRI or CT 2 to 3 weeks after the stroke.…”

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confidence: 99%

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Permanent Cortical Damage Detected by Flumazenil Positron Emission Tomography in Acute Stroke

Heiss¹,

Grond²,

Thiel³

et al. 1998

Stroke

103

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Background and Purpose-Therapy of acute ischemic stroke can only be effective as long as neurons are viable and tissue is not infarcted. Since ␥-aminobutyric acid receptors are abundant in the cortex and sensitive to ischemic damage, specific radioligands to their subunits, the central benzodiazepine receptors (BZR), may be useful as indicators of neuronal integrity and as markers of irreversible damage. To test this hypothesis we studied the binding of the BZR ligand [ 11 C]flumazenil (FMZ) early after ischemic stroke in comparison to the extent of final infarcts and hypometabolic cortical areas. Methods-In 10 patients cerebral blood flow, cerebral metabolic rate for oxygen (CMRO 2 ), oxygen extraction fraction (OEF), and FMZ binding were studied by positron emission tomography 3.5 to 16 hours after onset of their first hemispheric stroke. Early changes in flow, oxygen metabolism, and FMZ binding were compared with permanent disturbances in glucose metabolism, and the size of the final infarcts was determined on MRI or CT 12 to 22 days after the stroke. Results-In all patients except one cerebral blood flow was disturbed, with marked decreases in eight and a hyperperfusion in one patient corresponding to the location of neurological deficits. In these areas CMRO 2 was also reduced but to a variable degree, inducing highly variable OEF. Areas with markedly decreased CMRO 2 (Ͻ60 mol/100 g per minute) corresponded to regions with decreased FMZ binding (Ͻ4.0 times the mean value in the white matter). In all patients the final cortical infarcts were visible on the early FMZ images. Infarcts could be discriminated from noninfarcted cortex by decreased FMZ binding despite a wide range of OEF. In finally hypometabolic cortex FMZ binding was initially decreased or normal, with OEF covering a wide range; this suggested neuronal loss and/or deactivation as the cause of metabolic disturbance. Additionally, a highly significant correlation was found between FMZ distribution within the first 2 minutes after injection and regional cerebral blood flow. Conclusions-These results demonstrate that permanently and irreversibly damaged cortex can be detected by reduced FMZ binding early after stroke. Since FMZ distribution additionally images regional cerebral perfusion, BZR radioligands have a potential as clinically useful tracers in patients with acute ischemic stroke. The evidence of tissue damage furnished by these tracers might be of relevance for the selection of individual therapeutic strategies. (Stroke. 1998;29:454-461.)

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Section: Compromised Cortical Regions In Individual Patientssupporting

confidence: 74%

Section: Radiological Investigationsmentioning

confidence: 99%

Section: Radiological Investigationsmentioning

confidence: 99%

mentioning

confidence: 99%

See 2 more Smart Citations

Permanent Cortical Damage Detected by Flumazenil Positron Emission Tomography in Acute Stroke

Heiss¹,

Grond²,

Thiel³

et al. 1998

Stroke

103

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“…It has been widely used for mapping the central benzodiazepine receptor, in vivo, using Positron emission tomography (PET) [7,8,10,14,[17][18][19]. Nevertheless, due to its binding kinetics, mathematical modeling is required to obtain relevant quantitative parameters such as Bmax or affinity constant.…”

Section: Introductionmentioning

confidence: 99%

Biodistribution, binding specificity and metabolism of [ 18 F]fluoroethylflumazenil in rodents

Levêque

Labar

Gallez

2001

Nuclear Medicine and Biology

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Pre-clinical studies were carried out in order to characterize in rodents the biodistribution, the binding specificity and the metabolism of hydrophylic metabolites which cannot cross the blood brain barrier, and are rapidly eliminated in the urine. Inhibition of the metabolism by acetaminophen (chemically induced hepatitis) led to a significant increase of the radioactivity found in the circulating blood and in the brain, while these results were not observed using classical inhibitors of the cytochrome CYP450, cimetidine and ketoconazole.

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Syntheses and Uses of Isotopically Labelled Organic Halides

Zieliński

Kańska

2009

Patai's Chemistry of Functional Groups

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Introduction Syntheses and Uses of Organic Halides Labelled with Fluorine‐18 and Carbon‐11 Syntheses and Uses of Isotopically Labelled Organic Chlorides Syntheses and Applications of Bromine Isotopes Syntheses and Uses of Organic Compounds Labelled with Iodine Isotopes Syntheses of Organic Compounds Labelled with Astatine‐211 Isotope Effect Studies with Organic Halides Acknowledgements

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Central type benzodiazepine binding sites: A positron emission tomography study in the baboon's brain

Cited by 92 publications

References 15 publications

Permanent Cortical Damage Detected by Flumazenil Positron Emission Tomography in Acute Stroke

Permanent Cortical Damage Detected by Flumazenil Positron Emission Tomography in Acute Stroke

Biodistribution, binding specificity and metabolism of [ 18 F]fluoroethylflumazenil in rodents

Syntheses and Uses of Isotopically Labelled Organic Halides

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