Central benzodiazepine receptor occupancy by zolpidem in the human brain as assessed by positron emission tomography
| Autor: | Zarifian E, Pascale Abadie, Jean-Claude Baron, Bernard Scatton, Louisa Barré, Patrice Rioux, Alain Patat |
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| Rok vydání: | 1996 |
| Předmět: |
Adult
Flumazenil Male Zolpidem medicine.medical_specialty Time Factors Pyridines medicine.drug_class Hypnotic Radioligand Assay Internal medicine medicine Humans Middle frontal gyrus Tissue Distribution Pharmacology Benzodiazepine Neocortex Chemistry Brain Human brain Receptors GABA-A medicine.anatomical_structure Endocrinology Cerebellar cortex Tomography Emission-Computed medicine.drug |
| Zdroj: | European Journal of Pharmacology. 295:35-44 |
| ISSN: | 0014-2999 |
| Popis: | The central benzodiazepine receptor occupancy by zolpidem in man is unknown. The present study used positron emission tomography (PET) and [11C]flumazenil to assess in five healthy volunteers, central benzodiazepine receptor occupancy in brain regions with high receptor densities 1 h following an acute oral administration of twice the usual hypnotic dose of zolpidem (20 mg). Receptor occupancy was measured in five discrete structures (middle frontal gyrus, middle temporal gyrus, posterior occipital cortex, lateral parietal cortex, and cerebellar cortex) and in a large neocortical area as the fractional change in the [11C]flumazenil bound/free ratio for the interval 15-40 min post-administration of the radiotracer. The free-radioligand concentration was estimated from the pons, a reference structure virtually devoid of central benzodiazepine receptor. With individual pons values, mean occupancy was about 21% but with spurious inter-subject variability. With pons values averaged across the five subjects and separately for control and treated condition, the occupancy was (mean +/- S.D.) 27 +/- 11% for the whole neocortex, and ranged from 26 to 29% in the five discrete structures (P < 0.01). By showing hypnotic effect at moderate occupancies, this study directly provides evidence for the full-agonist properties of zolpidem in human. |
| Databáze: | OpenAIRE |
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