DMG for Endothelial NO Vasodilation Without Nitrate Side Effects

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Solution Overview

Problem

Current NO-releasing substances for vasodilation, such as nitroglycerin, molsidomine, or isosorbide dinitrate, are limited by interactions, side effects, or contraindications, necessitating new approaches for inducing endothelium-derived NO-dependent vasodilation.

Innovation Solution

The use of N,N-dimethylglycine (DMG) and/or its salts, particularly sodium dimethylglycinate, to induce endothelium-derived NO-dependent vasodilation, which can be administered topically or systemically for treating various conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional NO-releasing substances (nitroglycerin, molsidomine, isosorbide dinitrate) are used for vasodilation, then vasodilatory effect is achieved, but interactions, side effects, and contraindications occur

Engineering Contradiction:
Improvevasodilatory effectVSAvoidinteractions and side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent replaces conventional NO-releasing substances with N,N-dimethylglycine (DMG), an amino acid derivative that serves as a safer, more tolerable alternative. DMG induces endothelium-derived NO-dependent vasodilation through a different mechanism, avoiding the harmful interactions and side effects associated with nitroglycerin, molsidomine, and isosorbide dinitrate while maintaining the desired vasodilatory effect

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The patent changes the chemical parameter from conventional nitrate esters to an amino acid derivative (DMG). This parameter change fundamentally alters the mechanism of action while achieving the same therapeutic goal, thereby eliminating the harmful factors associated with the original substances

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If N,N-dimethylglycine (DMG) is used to induce endothelium-derived NO-dependent vasodilation, then vasodilation is achieved with fewer side effects, but the mechanism is less established compared to conventional NO-releasing substances

Engineering Contradiction:
Improveside effectsVSAvoidmechanism establishment
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

DMG serves as a precursor that the body converts into active metabolites through endogenous enzymatic pathways. The amino acid is metabolized to produce NO indirectly through endothelial cells, allowing the body's own systems to generate the therapeutic effect without requiring externally administered NO or unstable nitrate esters

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

DMG and its salts effectively induce endothelium-derived NO-dependent vasodilation, improving microcirculation and treating conditions like skin aging, dermatitis, and cardiovascular diseases by increasing eNOS expression and NO production, as demonstrated in vitro and in vivo studies.

Implementation Method 1

DMG can also induce or initiate endothelium-derived NO-dependent vasodilation

Methodology Applied
Scientific EffectNitric oxide release:

Implementation Method 2

Nitric oxide (NO) is known for its dilating effect on blood vessels

Methodology Applied
Scientific EffectVasodilation:

Implementation Method 3

increasing eNOS expression and NO production

Methodology Applied
Scientific EffecteNOS expression induction:

Data Source

PatentEP4599827A1Dgl for the induction of endothelial-derived no-dependent vasodilation
Publication Date: 2025.08.13 DR KURT WOLFF
  • EP4599827A1 patent drawingFigure 1a
  • EP4599827A1 patent drawingFigure 1b~1d
  • EP4599827A1 patent drawingFigure 2~2d

AI summary

The application relates to the use of a composition comprising N,N-dimethylglycine (DMG) and/or a salt thereof for inducing endothelium-derived NO-dependent vasodilation.