Search of conformation-specific PET probe

2018 Fiscal Year Final Research Report

• Project/Area Number: 16K15570
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Radiation science
• Research Institution: Tohoku Medical and Pharmaceutical University
• Principal Investigator: OKAMURA Nobuyuki 東北医科薬科大学, 医学部, 教授 (40361076)
• Project Period (FY): 2016-04-01 – 2019-03-31
• Keywords: 分子イメージング / αシヌクレイン

Outline of Final Research Achievements

To develop a PET probe for in vivo monitoring of misfolded protein accumulation, we tested the binding and pharmacokinetic properties of our library compounds and found a series of novel compound that can clearly stain Lewy bodies. A candidate compound (Cpd.365) showed excellent blood-brain barrier permeability in mice. Autoradiography using postmortem human brain samples showed strong binding of 18F-labeled compound to α-synuclein rich brain sections, although the binding selectivity of this compound was insufficient for selective α-synuclein probe.

Free Research Field

薬理学

Academic Significance and Societal Importance of the Research Achievements

プローブが実用化され、パーキンソン病などのミスフォールディングの脳内蓄積を生体で非侵襲的に計測できれば、多様な神経変性疾患の早期診断のためのスクリーニング法となる。また新たな治療評価系としても活用でき新規治療薬開発と連動させるによって疾患の撲滅へ向けた第一歩となる。