Varenicline-Induced Elevation of Dopamine in Smokers: A Preliminary [(11)C]-(+)-PHNO PET Study
Autor: | Dina Lagzdins, Mihail Guranda, Islam Gamaleddin, Isabelle Boileau, Peter Selby, Bernard Le Foll, Rachel F. Tyndale, Patricia Di Ciano |
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Rok vydání: | 2015 |
Předmět: |
Adult
Male Dopamine Craving Neuroimaging Pharmacology Partial agonist 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine medicine Humans 030212 general & internal medicine Varenicline Brain Chemistry Receptors Dopamine D2 Dopaminergic Smoking Receptors Dopamine D3 Brain medicine.disease Magnetic Resonance Imaging Tobacco Use Cessation Devices Psychiatry and Mental health Nicotinic agonist chemistry Schizophrenia Positron-Emission Tomography Female Original Article Psychopharmacology medicine.symptom Psychology 030217 neurology & neurosurgery medicine.drug |
Zdroj: | Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 41(6) |
ISSN: | 1740-634X |
Popis: | Varenicline, a nicotinic partial agonist, is the most effective treatment for tobacco use disorder. However, its mechanism of action is still unclear and may involve stimulating dopaminergic transmission. Here we used PET imaging with [(11)C]-(+)-PHNO to explore for the first time the impact of varenicline on dopamine transmission in the D2-rich striatum and D3-rich extra-striatal regions and its relationship with craving, withdrawal and smoking. Eleven treatment-seeking smokers underwent two PET scans with [(11)C]-(+)-PHNO, each following 12-h overnight smoking abstinence both prior to receiving varenicline and following 10-11 days of varenicline treatment (ie, at steady-state drug levels). Subjective measures of craving and urges to smoke were also assessed on the days of the PET scans. Varenicline treatment significantly reduced [(11)C]-(+)-PHNO binding in the dorsal caudate (p=0.008) and reduced some craving measures. These findings provide the first evidence that varenicline is able to increase DA levels in the human brain, a factor that may contribute to its therapeutic efficacy. |
Databáze: | OpenAIRE |
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