Multi-Target Receptor Modulator for Inflammatory Disease Treatment
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Solution Overview
Problem
Current treatments for inflammatory, autoimmune, gastrointestinal, and respiratory diseases lack effective drugs that simultaneously activate opioid receptors and inhibit tachykinin receptors and TRPV1 and TRPM8 ion channels, leading to inadequate symptom management and side effects from opioid therapy.
Innovation Solution
A novel 2-phenylethylamide N-(p-hydroxyphenylacetyl)phenylalanine compound acts as an agonist of opioid receptors, antagonist of tachykinin receptors, and blocker of TRPV1 and TRPM8 ion channels, offering a therapeutic approach for these conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional treatments are used for inflammatory and autoimmune diseases, gastrointestinal diseases, and respiratory diseases, then symptom management is provided, but side effects occur and symptom relief is inadequate
Solution Approach 1:
The patent combines multiple pharmacological actions into a single compound that simultaneously activates opioid receptors (for pain relief) and blocks tachykinin receptors and TRPV1/TRPM8 ion channels (to reduce side effects and enhance therapeutic effect). This multi-target approach merges the benefits of opioid analgesia with the protective effects of tachykinin and ion channel modulation, providing reliable symptom management while minimizing harmful side effects.
Solution Approach 2:
The compound exhibits multi-functionality by acting on multiple receptor types and ion channels simultaneously. It serves as an opioid receptor agonist for pain management, while also functioning as a tachykinin receptor antagonist and TRPV1/TRPM8 ion channel blocker, thereby providing broad-spectrum therapeutic effects for inflammatory, gastrointestinal, and respiratory conditions with a single agent.
2Object-affected harmful factors
If opioid therapy is used for pain management, then nociception is reduced, but harmful side effects are generated
Solution Approach 1:
The patent converts the potential harm of opioid therapy into a benefit by combining opioid receptor activation with tachykinin receptor and ion channel blockade. The tachykinin and ion channel blocking actions counterbalance the side effects of opioid therapy (such as respiratory depression, constipation, and dependence), while the opioid agonist activity provides effective pain relief. This transforms the harmful profile of opioid therapy into a beneficial multi-target therapeutic approach.
3Device complexity
If single-target therapies are used, then treatment simplicity is maintained, but symptom relief is inadequate for complex conditions
Solution Approach 1:
The patent merges multiple therapeutic actions into a single compound, eliminating the need for complex combination therapies. The compound simultaneously targets opioid receptors, tachykinin receptors, and TRPV1/TRPM8 ion channels, providing comprehensive symptom relief for complex inflammatory, gastrointestinal, and respiratory conditions while maintaining treatment simplicity with a single agent.
Data Source
AI summary
The invention relates to organic chemistry, pharmacology and medicine and is concerned with the treatment of inflammatory and autoimmune diseases, such as psoriasis, atopic dermatitis, prurigo, Crohn's disease, colitis, gastrointestinal diseases such as diarrhoea and irritable bowel syndrome, respiratory diseases such as asthma, COPD, bronchitis, rhinitis, and also cough and a series of other diseases associated with the activity of opioid and tachykinin receptors and of TRPV1 and TRPM8 ion channels using a 2-phenylethylamine N-(p-hydroxyphenylacetyl)phenylalanine compoundThe invention, and also pharmaceutically acceptable adducts, hydrates, solvates are agonists of opioid receptors, antagonists of tachykinin receptors and of TRPV1 and TRPM8 ion channels. The invention also relates to pharmaceutical compositions comprising a therapeutically effective amount of the compound according to the invention.