Pain Relief Peptide Targeting N-Type Calcium Channels
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Solution Overview
Problem
Current pain management technologies face challenges in effectively addressing pain without causing significant side effects or requiring high doses, particularly for conditions like neuropathic pain and pain associated with injuries or diseases such as stroke and epilepsy.
Innovation Solution
The use of a peptide with the sequence YGRKKRRQRRRKLSSIESDV, specifically designed to bind to N-type calcium channels rather than PSD-95 interactions with NMDAR, providing pain relief at lower doses and without entering the CNS in detectable amounts.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional analgesic drugs (NSAIDs, narcotics) are used to treat pain, then pain relief is achieved, but significant side effects occur and high doses are required
Solution Approach 1:
The patent changes the molecular target parameter from traditional analgesic targets to N-type calcium channels, achieving pain relief through a different mechanism that reduces side effects and allows lower effective doses
Solution Approach 2:
The peptide acts as an intermediary substance that binds to N-type calcium channels and prevents calcium influx, thereby indirectly reducing pain transmission without directly acting on the pain pathway itself
2Reliability
If high doses of analgesic drugs are used to achieve effective pain relief, then pain control improves, but the risk of side effects and toxicity increases
Solution Approach 1:
The patent identifies a new target parameter (N-type calcium channels) that provides higher efficacy at lower doses, changing the dose-response relationship to achieve effective pain control with reduced quantity of substance required
3Reliability
If peptides enter the CNS to provide pain relief, then central pain modulation is achieved, but detectable amounts in CNS may cause unwanted effects
Solution Approach 1:
The peptide serves as an intermediary that acts on peripheral N-type calcium channels, providing pain relief without requiring significant penetration into the CNS, thus avoiding unwanted central effects
Solution Approach 2:
The patent segments the pain management function into peripheral action (N-type calcium channel inhibition) rather than requiring central CNS penetration, separating the therapeutic effect from potential harmful central effects
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
This peptide effectively alleviates pain in a dose-dependent manner, specifically targeting N-type calcium channels to reduce pain hypersensitivity, as demonstrated in animal models, with minimal side effects and lower therapeutic doses compared to traditional methods.
Implementation Method 1
specifically designed to bind to N-type calcium channels rather than PSD-95 interactions with NMDAR
Data Source
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AI summary
The invention provides agents useful for treating pain. An exemplary agent comprises or consists of the a portion of a retroviral Tat protein. One such agent is the peptide Tat-NR2B9c. This peptide has previously been described as an agent for inhibiting damaging effects of stroke and similar conditions via inhibition of PSD95 interactions with NMDA receptors and/or NOS. The present application provides data showing that the Tat- NR2B9c peptides is effective in alleviation of pain. The alleviation of pain can be obtained at a dose of the peptide below the dose required to inhibit PSD-95 interactions with NMDAR or NOS.