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Drug depropment in neuropsycguatric disorders : from bench to bed
https://repo.qst.go.jp/records/65029
https://repo.qst.go.jp/records/650294c3fb541-aa76-4d43-9dfb-a85e178c98fa
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2013-06-07 | |||||
| タイトル | ||||||
| タイトル | Drug depropment in neuropsycguatric disorders : from bench to bed | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_c94f | |||||
| 資源タイプ | conference object | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Suhara, Tetsuya
× Suhara, Tetsuya× 須原 哲也 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Session Type: BrainPET Educational Course 1 \nDrug Development in Neuropsychiatric Disorders: From Bench to Bed \nTetsuya Suhara, MD, PhD \nMolecular Neuroimaging Program, Molecular Imaging Center, National Institute of Radiological Sciences, Chiba, Japan. \nPositron emission tomography (PET) techniques have enabled the visualization of target molecules of various psychotropic drugs, such as receptors and transporters in the living human brain. The concept of occupancy has been used as a reliable index for therapeutic drug monitoring at specific binding sites. Previous PET studies on antipsychotics have suggested that 70%–80% of central dopamine D2 receptor occupancy provides the desired therapeutic effects without any extrapyramidal symptom. Regarding the antidepressant therapy, serotonin transporter occupancy is also used as one of the indices for the evaluation of antidepressants such as selective serotonin reuptake inhibitors. Clinical doses of clomipramine and fluvoxamine occupied about 80% of serotonin transporter, and dose escalation would have minimal effect on serotonin transporter blockade. Norepinephrine transporter (NET) is another target of antidepressants. The mean NET occupancies by nortriptyline doses were 16.4 % at 10 mg, 33.2 % at 25 mg, and 41.1% at 75 mg, respectively. The application of PET method on drug evaluation can provide us useful information about the characteristics of psychotropics, including an optimal clinical dose and the kinetic profile at the sites of action as well as their ability to penetrate into the brain. However, in psychiatric disorders, reliable diagnostic biomarkers are still awaited. Nonetheless, in the case of Alzheimer disease (AD), distinctive pathological changes such as deposition of B-amyloid (AB) and tau protein have been identified. Several amyloid ligands, such as [11C]PIB and [11C]BF227, have been developed for imaging AB deposition. On the other hand, tau pathology is considered to be closely related with neural dysfunction in AD and non-AD tauopathy, and could accordingly be an important target for both therapeutic intervention and diagnostic imaging. [11C]PBB3 has been recently developed as a tau imaging PET ligand, and showed high affinity and selectivity for tau deposits in our preclinical studies. [11C]PBB3-PET demonstrated high accumulation in the medial temporal cortex of all AD patients, in which binding of [11C]PIB was minimal. Distribution of [11C]PBB3 accumulation observed in AD patients extended to the entire limbic system and subsequently to the neocortex as a function of the disease severity. |
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| 会議概要（会議名, 開催地, 会期, 主催者等） | ||||||
| 内容記述タイプ | Other | |||||
| 内容記述 | Shanghai BRAIN 2013 | |||||
| 発表年月日 | ||||||
| 日付 | 2013-05-23 | |||||
| 日付タイプ | Issued | |||||
