Small Molecule Tracer for Non-Invasive Alpha-Synuclein Imaging
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Solution Overview
Problem
Current methods for detecting α-synuclein aggregates in neurodegenerative diseases are invasive and unable to provide non-invasive, real-time diagnostic information in vivo.
Innovation Solution
Development of small molecule tracers, specifically compounds represented by Formula I, that can bind to α-synuclein aggregates and cross the blood-brain barrier, allowing for imaging using PET, SPECT, and fluorescence techniques.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If histological analysis of autopsy materials is used to detect α-synuclein aggregates, then detection accuracy is achieved, but the method is invasive and cannot provide non-invasive detection in vivo
Solution Approach 1:
The patent uses small molecule tracers as intermediaries that can bind specifically to α-synuclein aggregates and cross the blood-brain barrier. These tracers serve as a mediator between the detection system and the target protein, enabling non-invasive in vivo detection while maintaining high detection accuracy through specific binding interactions
Solution Approach 2:
The patent replaces the mechanical/invasive histological analysis system with a molecular imaging system using PET, SPECT, or fluorescence techniques. This substitution allows detection to occur non-invasively in living subjects by detecting radiation or light signals from the tracer-bound aggregates
2Ease of operation
If small molecule tracers are developed to bind to α-synuclein aggregates, then non-invasive in vivo imaging is enabled, but the tracers must have high selectivity among co-deposited proteins (Aβ, Tau) to achieve specific imaging
Solution Approach 1:
The patent applies local quality by designing tracers with specific molecular structures (Formula I with specific Ring A, Ring B, and substituent combinations) that have high affinity and selectivity for α-synuclein aggregates while showing weak binding to Aβ and Tau proteins. The local chemical structure is optimized to recognize specific features of α-synuclein aggregates
Solution Approach 2:
The patent uses parameter changes by systematically varying the chemical parameters of the tracer molecules (different Ring A, Ring B, and R1, R2 substituents) to optimize the balance between blood-brain barrier permeability, binding affinity, and selectivity for α-synuclein aggregates versus other proteins
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
Enables non-invasive visualization of α-synuclein aggregates in the brain, facilitating early diagnosis, disease monitoring, and drug efficacy evaluation for neurodegenerative diseases such as Parkinson's disease and dementia with Lewy body.
Implementation Method 1
the specific binding of molecular tracer (e.g., radioactive tracer, fluorescent tracer, etc.) to biomarkers (e.g., receptors, enzymes, ion channels, misfolded proteins)
Implementation Method 2
after radio-labelled the tracer can be used by PET and SPECT to realize the non-invasive visual detection of α-synuclein in vivo
Implementation Method 3
The compound exhibits self-fluorescence and can be used as a tracer for fluorescence imaging
Data Source
AI summary
The invention discloses a type of compound that can specifically bind to α-synuclein aggregates represented by Formula I, a radio-labelled compound thereof, a preparation method, and its use. The compound can be used as a tracer for optical imaging of α-synuclein aggregates in biological samples or in vivo (such as the brain). After radio-labelled, the compound of the invention can be used as a radio imaging tracer for PET, SPECT, and other imaging techniques to realize the detection of α-synuclein lesions by non-invasive visualization in vivo (such as the brain).