Exploring Occupancy of Dopamine D3 Receptor by Buspirone in Humans Using PET
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 6
- 试验地点
- 1
- 主要终点
- Dose-response occupancy of buspirone at DRD3
研究概览
简要总结
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.
详细描述
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.
研究设计
- 研究类型
- Interventional
- 分配方式
- Non Randomized
- 干预模型
- Crossover
- 主要目的
- Basic Science
- 盲法
- None
入排标准
- 年龄范围
- 19 Years 至 65 Years（Adult, Older Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •19 years or older
排除标准
- •Medical condition including cardiovascular, renal, hepatic or cerebrovascular diseases
- •History of or current neurological illnesses including seizure disorders, migraine, multiple sclerosis, movement disorders, head trauma, CVA or CNS tumor, - Present or past psychiatric condition including mood, anxiety, psychotic disorders and substance abuse and/or dependence.
- •Condition that precludes use of buspirone or that will interfere with participation in the present study (such as hypersensitive to buspirone hydrochloride).
- •Pregnancy or breastfeeding.
- •Presence of metal objects in the body or implanted electronic devices, that preclude safe MR scanning.
- •Claustrophobia.
- •Current use or use during the previous month of medication that may affect the CNS, including monoamine oxidase inhibitor (MAOI) or positive during drug screening for drugs of abuse or any medication that could increase the risk of buspirone administration.
- •Exposure to radiation in the last 12 month exceeding permissible limit for subjects participating in research.
研究组 & 干预措施
Buspirone 120 mg
Buspirone 120 mg (encapsulated).
干预措施: Buspirone (Drug)
Buspirone 60 mg
Buspirone 60 mg (encapsulated)
干预措施: Buspirone (Drug)
Placebo
Placebo (encapsulated)
干预措施: Placebo (Drug)
Buspirone 30 mg
Buspirone 30 mg (encapsulated).
干预措施: Buspirone (Drug)
结局指标
主要结局
Dose-response occupancy of buspirone at DRD3
时间窗: few months
\[11C\]-(+)-PHNO binding potential at three doses of buspirone and placebo.
次要结局
未报告次要终点
研究者
Bernard Le Foll
PI
Centre for Addiction and Mental Health