Multifunctional Neuroprotective Compound for Glutamate and Calcium Blockade

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Solution Overview

Problem

Current treatments for neurotoxicity in neuron cells, such as those caused by glutamate toxicity and ischemia, are limited in effectiveness and require early intervention, extending treatment periods and not fully addressing multifactorial neurodegenerative disease mechanisms.

Innovation Solution

A compound, N3,N5-bis(2-(5-methoxy-1H-indole-3-yl)ethyl)-2,6-dimethyl-4-(2-nitrophenyl)pyridine-3,5-dicarboxamide, synthesized from Nifedipine and Melatonin, functions as a glutamate blocker, T-type Ca channel blocker, and antioxidant, effectively reducing neurotoxicity by inhibiting calcium ion entry and providing cellular protection.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If glutamate receptor antagonists are used to prevent ischemia-related neuronal damage, then neuroprotection is achieved in stroke and head trauma, but treatment must be administered early and treatment period is extended

Engineering Contradiction:
Improveneuroprotection effectivenessVSAvoidtreatment period
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent combines multiple neuroprotective mechanisms into a single compound structure. The compound integrates calcium channel blocking activity (from nifedipine moiety) with antioxidant properties (from melatonin moiety), creating a multi-functional neuroprotective agent that addresses multiple pathological pathways simultaneously, thereby extending effective treatment window

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The compound serves multiple functions: it blocks glutamate receptors, blocks calcium channels, and provides antioxidant protection. This multi-functionality allows a single agent to address multiple aspects of neurotoxicity pathology, reducing the need for multiple separate treatments and extending the effective treatment period

Inventive Principle:
Principle #6Universality (Multi-functionality)

2Adaptability or versatility

If calcium channel blockers and antioxidants are used separately to address neurotoxicity, then specific mechanisms are targeted, but treatment mechanisms are limited and do not fully address multifactorial disease processes

Engineering Contradiction:
Improvetreatment mechanism coverageVSAvoidtreatment regimen complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent merges calcium channel blocking and antioxidant functions into a single molecular structure. The nifedipine portion provides calcium channel blocking while the melatonin portion provides antioxidant protection, creating a unified compound that addresses multiple pathological mechanisms without requiring multiple separate medications

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The compound is designed to be universally effective against multiple neurotoxicity mechanisms including glutamate excitotoxicity, calcium overload, and oxidative stress. This multi-functionality increases adaptability to different neurodegenerative conditions while simplifying the treatment regimen to a single agent

Inventive Principle:
Principle #6Universality (Multi-functionality)

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 compound effectively blocks glutamate receptors and calcium channels, offering neuroprotection and antioxidant properties, potentially delaying or reversing neuron cell death, thereby improving treatment outcomes for neurodegenerative diseases.

Implementation Method 1

The compound effectively blocks glutamate receptors and calcium channels, offering neuroprotection

Methodology Applied
Scientific EffectIon Repulsion/Attraction: Ion Repulsion/Attraction

Implementation Method 2

Melatonin reduces oxidative neurotoxicity due to quinolinic acid: in vitro and in vivo findings

Methodology Applied
Scientific EffectOxidation: Oxidation

Data Source

PatentEP3408266B1N3,n6-bis(2-(5-methoxy-1h-indole-3-yl)ethyl)-2,6-dimethyl-4-(2-nitrophenyl)pyridine-3,5-dicarboxamide and use thereof in the field of neurotoxicity
Publication Date: 2020.11.18 ATARTURK UNIVERSITY BILIMSEL ARASTIRMA PROJELLERI BIRIMI
  • EP3408266B1 patent drawing
  • EP3408266B1 patent drawing
  • EP3408266B1 patent drawing

AI summary

The invention relates to a molecule enabling removal of neurotoxicity observed in neuron cells due to various reasons.