Bupropion occupancy of the dopamine transporter is low during clinical treatment
| Autor: | Jeffrey H. Meyer, Doug Hussey, Verdell S. Goulding, Alan A. Wilson, Sylvain Houle, Bruce K. Christensen |
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| Rok vydání: | 2002 |
| Předmět: |
Adult
Male Adolescent Dopamine Plasma Membrane Transport Proteins Pharmacology toxicology Nerve Tissue Proteins Pharmacology Cocaine Dopamine Uptake Inhibitors Dopamine health services administration mental disorders medicine Humans Bupropion Clinical treatment Dopamine transporter Depressive Disorder Membrane Glycoproteins biology business.industry Membrane Transport Proteins Middle Aged Magnetic Resonance Imaging nervous system Mechanism of action behavior and behavior mechanisms biology.protein Catecholamine Antidepressive Agents Second-Generation Female Radiopharmaceuticals medicine.symptom business psychological phenomena and processes Protein Binding Tomography Emission-Computed medicine.drug |
| Zdroj: | Psychopharmacology. 163:102-105 |
| ISSN: | 1432-2072 0033-3158 |
| DOI: | 10.1007/s00213-002-1166-3 |
| Popis: | Bupropion is thought to treat major depression by blocking the dopamine transporter (DAT) because bupropion appears to have a selective affinity for the DAT. The validity of this mechanism has been questioned because the affinity of bupropion for the DAT is quite low.To determine the occupancy of bupropion for the DAT during clinical treatment of patients with depression.Positron emission tomography with [(11)C]-RTI32 was used to determine the striatal DAT binding potential (BP) of eight depressed patients before and during treatment with bupropion. BP is proportional to available receptor density (receptors not blocked by drug). Occupancy is the percent change in BP. Eight healthy subjects were similarly studied in a test-retest design.No significant difference in DAT BP was found after bupropion treatment in comparison to the test-retest data. The occupancy after bupropion treatment was 14% (confidence interval 6-22%) as compared to 7% in the test-retest condition.Bupropion treatment occupies less than 22% of DAT sites. This raises the question as to whether a DAT occupancy of less than 22% is therapeutic or whether there is another mechanism involved during treatment with bupropion. |
| Databáze: | OpenAIRE |
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