Quaternary ammonium salt compound and preparation method and application thereof

Abstract

The invention discloses a quaternary ammonium salt compound and a preparation method and application thereof. The invention provides a compound shown in a formula I with a novel structure, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, or a solvate thereof, or a prodrug thereof, or a metabolite thereof. The compound has the advantages of rapid onset of action, long-termlocal anesthesia effect after single administration, sensory nerve block time greater than motor nerve block time, and both long-term local anesthesia effect and selective local anesthesia effect, remarkably reduces side effects of QX314 and QX314 compositions and quaternary ammonium salt compounds with surfactant structural characteristics, and has better safety. Namely, the compound of formula Iand the pharmaceutically acceptable salt thereof can be used for preparing safe drugs with long-term local anesthesia and selective local anesthesia effects, and have the advantages of long-term local anesthesia, good local anesthesia selectivity, less nerve damage and high safety.

Description

technical field [0001] The invention relates to a quaternary ammonium salt compound and a preparation method and use thereof. Background technique [0002] Local anesthetics (local anesthetics) are a class of drugs that can reversibly block the generation and transmission of sensory nerve impulses locally, referred to as "local anesthetics". A class of drugs that reversibly blocks the generation and signal conduction of sensory nerve impulses locally, causing temporary sensory loss in the innervated parts of animals or humans, thereby reversibly causing pain loss in local tissues. Typically, the effect of local anesthetics is localized at the site of administration and disappears rapidly as the drug diffuses from the site of administration. Local anesthetics directly inhibit the relevant ion channels on nerve cells and fiber membranes, block the generation of action potentials and the conduction of nerve impulses, thereby producing local anesthesia. The currently recognize...

AI Technical Summary

Problems solved by technology

Although this type of compound can obtain a long-term local anesthetic effect to a certain extent, because this type of compound has a structure similar to a surfactant, although it can obtain a long-acting effect to a certain extent, it will also cause severe muscle and muscle pain at the local injection site. Nerve damage, poor safety

At the same time, similar compounds that have been reported so far do not have selective local anesthetic effect and cannot meet the clinical needs.

Therefore, whether QX314 is used alone, QX314 is used in combination with other active drugs, or the QX314 long-chain compound with surfactant structure features has the defects of poor safety and poor local anesthesia selectivity

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