Maltooligosaccharide NK1 Antagonist Composition
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Solution Overview
Problem
Conventional NK1 receptor antagonists, primarily peptide-based, exhibit limited pharmacodynamic activity and cause side effects due to antigenicity and agonistic action, while non-peptide types show high selectivity for NK1 receptors but pose cardiovascular risks, leading to safety concerns and unsatisfactory therapeutic effects.
Innovation Solution
Development of an NK1 receptor antagonist composition containing maltooligosaccharides, such as maltose to maltoheptaose, which demonstrate NK1 receptor antagonistic activity, offering a safer and more effective therapeutic option.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If peptide type NK1 receptor antagonists are used, then they can block binding between substance P and NK1 receptor, but they cause side effects due to antigenicity and agonistic action
Solution Approach 1:
The patent changes the chemical structure parameter from peptide-based to non-peptide-based antagonists, specifically using compounds with quinuclidine rings. This structural parameter change eliminates antigenicity while maintaining NK1 receptor blocking activity, thereby resolving the contradiction between therapeutic effectiveness and safety from side effects.
Solution Approach 2:
The patent develops composite chemical structures combining quinuclidine rings with various substituent groups (aromatic rings, heterocyclic groups, etc.) to create non-peptide NK1 antagonists. These composite structures achieve high selectivity for NK1 receptors while avoiding the harmful effects associated with peptide-based antagonists.
2Reliability
If non-peptide type NK1 receptor antagonists with quinuclidine ring are used, then they exhibit high selectivity for NK1 receptor, but they show remarkable affinity with ionic channels particularly L type calcium channel causing cardiovascular side effects
Solution Approach 1:
The patent modifies specific local regions of the quinuclidine-based molecule by introducing bulky aromatic groups or heterocyclic groups at predetermined positions. This local structural modification reduces affinity with ionic channels while preserving NK1 receptor selectivity, thereby eliminating cardiovascular side effects.
Solution Approach 2:
The patent converts the potential harm of quinuclidine ring affinity with ionic channels by strategically placing substituent groups that redirect the molecule's interaction preferences. The modified structures maintain the beneficial NK1 selectivity while transforming the harmful ionic channel affinity into negligible interactions.
3Ease of manufacture
If peptide type NK1 receptor antagonists are used, then they can be developed from substance P structure, but they exert limited activity in living organisms
Solution Approach 1:
The patent replaces the peptide-based chemical system with a non-peptide chemical system. This substitution fundamentally changes the molecular characteristics, enabling high pharmacodynamic activity in living organisms while maintaining the therapeutic mechanism of NK1 receptor blockade.
Data Source
AI summary
An NK1 receptor antagonist composition of the present invention uses maltooligosaccharide having an NK1 receptor antagonistic activity as an active ingredient. A suitable amount of the maltooligosaccharide to be blended in the NK1 receptor antagonist composition of the present invention is 0.000001 to 70% by weight. The NK1 receptor antagonist composition of the present invention is prepared for use into various forms of external agents, internal medicines, foods and beverages by blending various materials as the ingredients other than the active ingredient. The NK1 receptor antagonist composition of the present invention has high safety for being used for pharmaceuticals and has satisfactory therapeutic effects.