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The objective of the present study is to use positron emission tomography brain imaging to investigate D3 occupancy of buspirone, an FDA-approved anxiolytic which acts as a serotonin partial agonist but has recently been identified as a D3 antagonist. It is hypothesized that clinically relevant doses of buspirone will occupy the D3 receptor.
Buspirone is used for anxiety disorder treatment, a therapeutic effect that has been thought to be mediated through its partial agonist properties at the serotonin receptor. However, since one PET study in humans has shown low occupancy of the serotonin by buspirone in clinical doses and since the DRD3 has been recently implicated in anxiety, some therapeutic effects of buspirone may be mediated through the DRD3. In human clinical studies, promising effects of buspirone have been reported for treatment of substance dependence, including tobacco, marijuana, and opiates, and clinical studies in cocaine dependent subjects are underway. However, it is unclear if buspirone is producing those effects through the DRD3 and no human study has incorporated a PET imaging component to investigate this question; it remains unclear whether buspirone significantly occupies the DRD3 at therapeutic doses in humans.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Buspirone 120 mg | Experimental | Buspirone 120 mg (encapsulated). |
|
| Buspirone 60 mg | Experimental | Buspirone 60 mg (encapsulated) |
|
| Placebo | Placebo Comparator | Placebo (encapsulated) |
|
| Buspirone 30 mg | Experimental | Buspirone 30 mg (encapsulated). |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Buspirone | Drug | The buspirone will be given once as a tablet and encapsulated for blinding. |
|
| Measure | Description | Time Frame |
|---|---|---|
| Dose-response occupancy of buspirone at DRD3 | [11C]-(+)-PHNO binding potential at three doses of buspirone and placebo. | few months |
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Inclusion Criteria:
- 19 years or older
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Isabelle Boileau, PhD | Center for Addiction and Mental Health | Principal Investigator |
| Bernard Le Foll, MD, PhD | Center for Addiction and Mental Health | Principal Investigator |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Center for Addiction and Mental Health | Toronto | Ontario | M5S 2S1 | Canada |
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| Label | URL |
|---|---|
| Information about research at the Centre for Addiction and Mental Health, Canada's largest mental health and addiction teaching | View source |
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| ID | Term |
|---|---|
| D016540 | Smoking Cessation |
| D020340 | Tobacco Use Cessation |
| ID | Term |
|---|---|
| D015438 | Health Behavior |
| D001519 | Behavior |
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| ID | Term |
|---|---|
| D002065 | Buspirone |
| D007785 | Lactose |
| ID | Term |
|---|---|
| D013141 | Spiro Compounds |
| D006844 | Hydrocarbons, Cyclic |
| D006838 | Hydrocarbons |
| D009930 | Organic Chemicals |
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|
| Placebo | Drug | Placebo will be lactose and encapsulated for blinding. A single capsule will be given. |
|
|
| D010879 |
| Piperazines |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D011743 | Pyrimidines |
| D011083 | Polycyclic Compounds |
| D004187 | Disaccharides |
| D009844 | Oligosaccharides |
| D011134 | Polysaccharides |
| D002241 | Carbohydrates |
| D000073893 | Sugars |