PKG-1α Binding NOP Compounds for Chronic Pain Imaging

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Solution Overview

Problem

Current methods for treating chronic pain lack objective detection and assessment tools, leading to misuse and abuse of prescription analgesics due to reliance on patient testimony and inadequate differentiation between peripheral and central pain sources, resulting in significant healthcare and societal costs.

Innovation Solution

Development of compounds that selectively bind to activated protein kinase G-1α (PKG-1α), such as NOP compounds, which can be labeled with isotopes like [18F] or [11C] for imaging and quantifying chronic pain by localizing in dorsal root ganglions, enabling accurate identification of pain sources and optimal drug dosage.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If prescription opioid analgesics are prescribed to treat chronic pain, then pain relief is provided to patients, but misuse and abuse increase leading to sedation, addiction, and overdose deaths

Engineering Contradiction:

Improvepain reliefVSAvoidmisuse and abuse

Core Design Contradiction:

Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The patent introduces an imaging agent as an intermediary diagnostic tool between the patient and the treatment decision. This agent specifically binds to activated PKG-1α in dorsal root ganglia to provide objective visualization of pain sources, enabling physicians to make informed decisions about whether opioid prescription is appropriate, thereby reducing inappropriate prescribing and subsequent misuse

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The imaging technology provides objective feedback about the actual presence and location of pain sources (peripheral vs. central) that contradicts or validates patient testimony. This feedback loop allows physicians to verify pain claims objectively before prescribing opioids, reducing addiction and abuse by preventing prescriptions to patients who do not actually have peripheral pain sources

Inventive Principle:

Principle #23Feedback

2Ease of operation

If patient testimony is used to assess chronic pain, then treatment decisions can be made quickly, but objective detection and assessment are lacking leading to inability to distinguish actual pain from simulation

Engineering Contradiction:

Improvetreatment decision speedVSAvoidpain assessment accuracy

Core Design Contradiction:

Ease of operationVSMeasurement precision

Solution Approach 1:

The patent replaces the subjective, verbal-based assessment system with an objective, visualization-based system. Instead of relying on patient testimony alone, the imaging agent provides visual evidence of pain sources through specific binding to activated PKG-1α, allowing objective detection and precise differentiation between peripheral and central pain sources while maintaining clinical workflow efficiency

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

3Adaptability or versatility

If opioid analgesics are prescribed without objective assessment, then treatment access is improved, but healthcare costs increase due to inability to match analgesic type and dose to pain intensity

Engineering Contradiction:

Improvetreatment accessibilityVSAvoidhealthcare costs

Core Design Contradiction:

Adaptability or versatilityVSQuantity of substance

Solution Approach 1:

The imaging technology enables local assessment of pain sources by visualizing specific dorsal root ganglia involved in pain transmission. This allows physicians to match the type and dose of analgesics to the specific pain source characteristics (peripheral vs. central, intensity), improving treatment precision and reducing waste from inappropriate prescribing, thereby lowering overall healthcare costs while maintaining accessibility

Inventive Principle:

Principle #3Local quality

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 use of NOP compounds allows for objective assessment of chronic pain, reducing prescription analgesic misuse and abuse, saving billions in healthcare costs and preventing thousands of lives lost to painkiller overdoses, while providing a precise method to determine optimal drug dosages.

Implementation Method 1

A family of compounds that selectively bind to a chronic pain specific, activated form of protein kinase G-1α (PKG-1α) has been identified

Methodology Applied

Scientific EffectSelective binding:

Implementation Method 2

the NOP compound is labeled with the fluorine radioisotope, [18F]

Methodology Applied

Scientific EffectRadioactive decay: Radioactive Decay

Data Source

PatentUS10098975B2Labeled pkg-1-alpha-binding compounds and their use in imaging and quantifying pain

Publication Date: 2018.10.16 THE TRUSTEES OF COLUMBIA UNIV IN THE CITY OF NEW YORK

AI summary

The present invention relates to the use of compounds that selectively bind to activated protein kinase G 1 alpha for imaging the anatomic basis for chronic pain. Such imaging may also be used to objectively quantify chronic pain.