Enkephalin-Modulating Composition for Pain Relief

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Solution Overview

Problem

Current pain management methods, particularly for chronic pain, are inadequate in effectively modulating the body's natural pain relief mechanisms, such as enkephalins, and do not fully leverage the synergistic potential of cannabinoids like THC and CBC.

Innovation Solution

A composition comprising phenylalanine, serine, GABA, and optionally THC, designed to enhance enkephalin activity by allosterically modulating opioid receptors and stimulating descending pathways of antinociception, potentially combined with other cannabinoids, to increase pain relief and inflammation reduction.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current pain management methods are used, then pain relief is provided to some extent, but the body's natural pain relief mechanisms (enkephalins) are not effectively modulated

Engineering Contradiction:
Improvepain relief effectivenessVSAvoidmodulation of natural pain relief mechanisms
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent changes the chemical parameters by introducing specific amino acids (phenylalanine, serine, glutamine) and neurotransmitters (GABA) that modify the biochemical environment to enhance enkephalin activity and opioid receptor modulation, thereby improving both pain relief effectiveness and natural mechanism modulation

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite biochemical formulation combining multiple amino acids, neurotransmitters, and optionally cannabinoids (THC, CBC) to work synergistically, where each component contributes to different aspects of pain modulation and enkephalin enhancement

Inventive Principle:
Principle #40Composite materials

2Device complexity

If single-component pain treatments are used, then the treatment is simple, but the synergistic potential of multiple cannabinoids and amino acids is not leveraged

Engineering Contradiction:
Improvetreatment composition simplicityVSAvoidpain management effectiveness
Core Design Contradiction:
Device complexityVSReliability

Solution Approach 1:

The patent merges multiple bioactive components (phenylalanine, serine, GABA, glutamine, and optionally THC/CBC) into a single integrated composition that works synergistically to enhance pain relief, leveraging the combined effects rather than isolated actions of each component

Inventive Principle:
Principle #5Merging (Combining)

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 composition effectively increases enkephalin activity, enhancing pain relief and reducing inflammation by biochemically synergizing its components, leading to increased analgesia and antinociception, with the option to include THC for enhanced effects.

Implementation Method 1

Phenylalanine's role as an analgesic is best postulated by its blockage of enkephalin degradation

Methodology Applied
Scientific EffectEnzyme inhibition: Enzyme

Implementation Method 2

THC is a chemical which binds to the specific receptor site; cannabinoid receptor CB1 and CB2

Methodology Applied
Scientific EffectReceptor binding: Adsorption

Implementation Method 3

Enkephalins are the endogenous ligands which bind to the mentioned opiate receptors described herein

Methodology Applied
Scientific EffectLigand-receptor binding: Adsorption

Implementation Method 4

Serine's role participates in the phosphorylation of serine containing analogs and has been recognized to potentiate the blood brain barrier permeability and CNS bioavailability of peptides

Methodology Applied
Scientific EffectPhosphorylation: Chemical Bonding

Implementation Method 5

Glutamine is one of the few amino acids capable of penetrating the blood brain barrier

Methodology Applied
Scientific EffectBlood brain barrier penetration: Permeation

Implementation Method 6

GABA (γ-aminobutyric acid) plays a chief role in reducing neuronal excitability in the nervous system

Methodology Applied
Scientific EffectNeurotransmission inhibition:

Implementation Method 7

The role of dopaminergic neurotransmission is recognized as a natural analgesic within the supraspinal regions and the role of dopamines descending inhibition of pain

Methodology Applied
Scientific EffectDopaminergic neurotransmission:

Data Source

PatentUS10413523B2Enkephalin-influencing composition and method
Publication Date: 2019.09.17 YELLOWSTONE NATURALS LLC

AI summary

A composition which includes Phenylalanine, Serine, Glutamine and GABA (γ-aminobutyric acid). The composition contains the essential amino acids Phenylalanine; Glutamine; the non-essential amino acid Serine; and GABA (γ-aminobutyric acid) in concentrations effective to influence or modulate the neurotransmitter pentapeptide enkephalin. The composition may further comprise tetrahydrocannabinol (THC).