Pindolol binding to 5-HT1A receptors in the human brain confirmed with positron emission tomography
| Autor: | Bengt Andrée, Lars Farde, Christer Halldin, Seth-Olov Thorberg |
|---|---|
| Rok vydání: | 1999 |
| Předmět: |
Adult
Male medicine.medical_specialty Radioligand Assay Dorsal raphe nucleus Internal medicine polycyclic compounds medicine Radioligand Humans Carbon Radioisotopes Pindolol Pharmacology Temporal cortex business.industry Chemistry musculoskeletal neural and ocular physiology organic chemicals Brain Human brain medicine.anatomical_structure Endocrinology Cerebellar cortex Receptors Serotonin Serotonin Serotonin Antagonists Radiopharmaceuticals Raphe nuclei Nuclear medicine business Receptors Serotonin 5-HT1 medicine.drug Tomography Emission-Computed |
| Zdroj: | Psychopharmacology. 144(3) |
| ISSN: | 0033-3158 |
| Popis: | The augmentation effect of (-)pindolol as used in combination with SSRI to treat major depression has been ascribed to blocking of dorsal raphe nucleus cell body 5-HT autoreceptors. In this study, the radioligand [carbonyl-11C]WAY-100635 and positron emission tomography were used to establish whether pindolol at a clinical dose level (10 mg s.o.d.) occupies 5-HT1A receptors in the human brain in vivo. Three healthy males were recruited and each subject was used as his own control. The 5-HT1A receptor occupancy was calculated for the frontal and temporal cortex and the raphe nuclei, using and a ratio analysis with the cerebellar cortex as the reference region. Maximal pindolol plasma concentration was reached within 3 h after drug administration. Two hours after pindolol administration, the regional 5-HT1A receptor occupancy was within the range 7-21% in the three subjects. The study confirms that the 5-HT1A-receptor may be a clinically significant target for pindolol. |
| Databáze: | OpenAIRE |
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