CNS Permeability Evaluation Probe

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Solution Overview

Problem

Existing methods for evaluating substance permeability through central nervous system (CNS) tissues are invasive, limited in their consideration of sophisticated biological mechanisms, and difficult to use for simultaneous screening of multiple target substances, leading to restricted information and reproducibility issues.

Innovation Solution

A novel evaluation probe, represented by a specific dye compound formula, is used to assess CNS permeability by permeating into biological specimens and serving as a substrate for transporters, allowing for functional evaluation and screening of compounds influencing transporter action in a less-invasive manner, considering in vivo metabolism mechanisms.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If invasive methods are used to evaluate CNS permeability, then measurement precision is improved, but ease of operation deteriorates and reliability worsens due to reproducibility issues

Engineering Contradiction:
ImproveCNS permeability evaluation accuracyVSAvoidOperational simplicity
Core Design Contradiction:
Measurement precisionVSEase of operation

Solution Approach 1:

The patent introduces an evaluation probe as an intermediary substance that mediates between the testing system and the CNS tissue. This probe serves as a model substrate that interacts with transporters without requiring invasive procedures, thereby maintaining measurement precision while improving ease of operation and reliability through non-invasive evaluation methods

Inventive Principle:
Principle #24Intermediary (Mediator)

2Measurement precision

If existing screening methods are used, then measurement precision is improved, but productivity deteriorates due to inability to screen multiple substances simultaneously

Engineering Contradiction:
ImproveTransporter function evaluation accuracyVSAvoidScreening throughput
Core Design Contradiction:
Measurement precisionVSProductivity

Solution Approach 1:

The evaluation probe is designed with multi-functionality to serve as a universal tool for screening multiple substances and evaluating various transporter functions simultaneously. The probe can be used across different experimental conditions and substance types, enabling high-throughput screening while maintaining measurement precision through its standardized interaction mechanism with transporters

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Reliability

If sophisticated biological mechanisms are fully considered, then reliability is improved, but device complexity worsens

Engineering Contradiction:
ImproveIn vivo metabolism mechanism considerationVSAvoidExperimental system complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The evaluation probe system utilizes the biological specimen's own sophisticated mechanisms (such as in vivo metabolism and transporter functions) to perform the evaluation automatically. The probe interacts with the specimen's endogenous transporters and metabolic pathways, allowing the biological system itself to serve the evaluation function without requiring complex external experimental apparatus, thereby improving reliability while minimizing added complexity

Inventive Principle:
Principle #25Self-service

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

The evaluation probe enables simple, high-reproducibility assessment of substance transport through CNS tissues, facilitating the evaluation and screening of compounds affecting transporters, thereby improving drug delivery efficiency and research on CNS-related diseases.

Implementation Method 1

A novel evaluation probe, represented by a specific dye compound formula, is used to assess CNS permeability by permeating into biological specimens and serving as a substrate for transporters

Methodology Applied
Scientific EffectPermeation: Permeation

Implementation Method 2

The evaluation probe enables simple, high-reproducibility assessment of substance transport through CNS tissues

Methodology Applied
Scientific EffectFluorescence: Fluorescence

Data Source

PatentEP2489665B1Evaluation probe for central nervous system permeability, evaluation method for central nervous system permeability, and screening method using an evaluation probe for central nervous system permeability
Publication Date: 2019.10.02 CANON KK
  • EP2489665B1 patent drawingFigure 1
  • EP2489665B1 patent drawingFigure 2~3
  • EP2489665B1 patent drawingFigure 4

AI summary

Provided is an evaluation probe capable of optically evaluating permeability of a substance through a central nervous system tissue. Also provided is an evaluation method for permeability of a substance through a central nervous system tissue using an evaluation probe for central nervous system permeability. Also provided is a screening method using an evaluation probe for central nervous system permeability. The evaluation probe for central nervous system permeability includes, as an active ingredient, at least one kind of compound represented by the following general formula (1). General formula (1)