A method to inhibit Na V 1.8 Active cyclic peptides or their salts and their application in analgesia
By developing cyclic peptides or their salts composed of tryptophan, lysine, and arginine, NaV1.8 inhibitors were prepared, solving the problem of insufficient research on small molecule peptides targeting the NaV1.8 sodium channel in the existing technology, and achieving effective inhibition and relief of pain.
CN122103274APending Publication Date: 2026-05-29KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI
- Filing Date
- 2026-04-10
- Publication Date
- 2026-05-29
AI Technical Summary
Technical Problem
There is limited research on small molecule peptides targeting the NaV1.8 sodium channel in existing technologies, making it difficult to effectively inhibit its activity and resulting in poor pain treatment outcomes.
Method used
Develop cyclic peptides or their salts composed of tryptophan, lysine, and arginine, and prepare NaV1.8 inhibitors by cyclizing the first and last amino acids with amide bonds to block pain signal transmission.
Benefits of technology
Cyclic peptides or their salts can significantly inhibit NaV1.8 channel currents, relieve chronic inflammatory pain, neuropathic pain and thermal pain, enhance resistance to pain, and provide potential analgesic and therapeutic drug molecules.
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Figure CN122103274A_ABST
Abstract
The application belongs to the technical field of polypeptide and medicine synthesis, and particularly relates to a cyclic peptide or salt thereof inhibiting Na V 1.8 activity and application thereof in analgesia. After a series of linear peptides composed of tryptophan, lysine and arginine are obtained, the amino acids at the head and tail are cyclized by an amide bond to obtain the cyclic peptide. The cyclic peptide or salt thereof can inhibit the current of voltage-gated sodium ion channel of mammals V 1.8, and can be developed as a Na V 1.8 inhibitor. The cyclic peptide or salt thereof can act on the Na V 1.8 receptor of mammals, and can block the transmission of pain signal for a long time. The cyclic peptide or salt thereof can enhance the resistance to pain, can be developed as a potential analgesic, and is applied to relieve pain of human and other animals, and is a Na V 1.8 ion channel related disease research and a lead drug molecule for developing a drug for treating Na V 1.8 ion channel related diseases.
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