Dopamine D2 and Serotonin 5-HT2 Receptor Antagonists for Retinal Degeneration

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Solution Overview

Problem

Current treatments for retinal degeneration, such as retinitis pigmentosa and age-related macular degeneration, are limited and primarily focus on slowing disease progression rather than effectively addressing vision loss, with a need for pharmaceutical products that can improve visual function.

Innovation Solution

Administration of compounds that block or diminish stimulation of dopamine D2-like receptors or serotonin 5-HT2 receptors, including antagonists, partial agonists, or inverse agonists, to enhance light responses in retinal neurons, potentially improving vision in subjects with retinal degeneration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for retinal degeneration are used, then disease progression is slowed, but visual function is not effectively improved

Engineering Contradiction:
Improvedisease progression controlVSAvoidvisual function improvement
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent changes the pharmacological parameter by using dopamine D2-like receptor and serotonin 5-HT2 receptor antagonists instead of conventional treatments. This parameter change targets the underlying neural signaling pathways to improve visual function while also controlling disease progression, resolving the contradiction between reliability and productivity.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If retinal prostheses are used, then vision is restored in advanced stages, but device complexity increases

Engineering Contradiction:
Improvevision restorationVSAvoidprosthesis system complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent replaces the mechanical/electrical prosthesis system with a pharmacological system using receptor antagonists. This substitution achieves vision improvement through biochemical modulation of retinal neurons rather than through complex mechanical devices, thereby reducing device complexity while maintaining productivity.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

3Reliability

If sunlight protection and vitamin therapy are used, then degenerative process is slowed, but treatment effectiveness is limited

Engineering Contradiction:
Improvedegeneration slowingVSAvoidtherapeutic effectiveness
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent introduces a new pharmacological parameter (receptor antagonism) that enhances therapeutic effectiveness beyond the limited effects of sunlight protection and vitamin therapy. This parameter change allows for more potent intervention while maintaining the protective effects against degeneration.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS12102640B2Use of dopamine and serotonin receptor antagonists for treatment in a subject with retinal degeneration
Publication Date: 2024.10.01 THE UNITED STATES OF AMERICA AS REPRESENTED BY THE DEPT OF VETERANS AFFAIRS
  • US12102640B2 patent drawing
  • US12102640B2 patent drawing
  • US12102640B2 patent drawing

AI summary

Disclosed herein are methods of treating disorders of the retina (e.g., macular degeneration, retinitis pigmentosa, etc.) comprising administering to a subject in need of such treatment a therapeutically effective amount of a compound (for example, an antipsychotic drug) that blocks or diminishes agonist-mediated responses upon binding to either dopamine D2-like receptors or serotonin 5-HT2 receptors.