Preparation method and application of novel high-selectivity KV7.2 opener

By designing binding pockets based on KV7.2 specific residues, highly selective KV7.2 openers were synthesized, solving the problem of insufficient selectivity of existing drugs in KV7.2 potassium channel activation. This resulted in highly efficient antiepileptic activity and no cardiotoxic side effects in epilepsy models.

CN121800760APending Publication Date: 2026-04-07HEBEI MEDICAL UNIVERSITY
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Patent Information

Application Number
CN202610177344.2
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-02-07
Publication Date
2026-04-07

AI Technical Summary

Technical Problem

Existing drugs are unable to achieve highly selective activation of the KV7.2 potassium channel, leading to toxic side effects caused by non-selective activation, especially posing risks to the cardiovascular and nervous systems.

Method used

By identifying KV7.2 specific residues and designing binding pockets, combined with virtual screening and optimization, a series of highly selective KV7.2 openers were synthesized to enhance the current of the potassium ion channel KV7.2 and accelerate the channel activation and inactivation process.

Benefits of technology

It exhibits highly effective antiepileptic activity in a simulated human epilepsy model, significantly superior to the positive control, and has no motor dysfunction side effects, providing a new strategy for precise targeting of KV7 drugs.

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Abstract

The invention belongs to the technical field of biological medicine, and particularly relates to preparation of a novel high-selectivity KV7.2 opener and application of the novel high-selectivity KV7.2 opener in antiepileptic drugs. A series of KV7.2-targeted small-molecule inhibitors are designed and synthesized, and the small-molecule inhibitors can enhance the current of a potassium ion channel KV7.2, accelerate channel activation and delay the inactivation process of the channel. The small molecule has a remarkable potential for treating epilepsy, shows efficient anti-epileptic activity in three classic epilepsy models for simulating human comprehensive attack and drug-refractory focal attack, is remarkably superior to positive control RTG, can be used for preparing anti-epileptic drugs and has a wide application prospect.
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