Application of bulleyaconitine A used as state-independent sodium ion channel blocker to analgesia

A kind of clathrin, dependence technology, applied in non-central analgesics, medical preparations containing active ingredients, anti-inflammatory agents, etc., can solve the mechanism of analgesic action, biopharmaceutical properties and pharmacokinetic characteristics not clear, etc.

Inactive Publication Date: 2012-07-11
YUNNAN HAOPY PHARM LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] What the present invention is to solve is the problem that the deep analgesic mechanism, biopharmaceutical properties and pharmacokinetic characteristics of aconitin are not clear at present, further explore the analgesic principle of aconitin, and establish The animal model of rational pain investigates the analgesic effect of aconitin, and explores the analgesic mechanism of aconitin through the study of sodium ion channels and TNF-a, thus discovering the effect of aconitin on neuropathic pain model animals. Therapeutic effect and its duration

Method used

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  • Application of bulleyaconitine A used as state-independent sodium ion channel blocker to analgesia
  • Application of bulleyaconitine A used as state-independent sodium ion channel blocker to analgesia
  • Application of bulleyaconitine A used as state-independent sodium ion channel blocker to analgesia

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Embodiment 1

[0012] Embodiment 1: the application of aconitin in analgesia as a state-dependent sodium ion blocker, through the accompanying drawings and three experimental groups, resting state experimental group, inactivated state group and activated state group to the present invention for further clarification.

[0013] figure 1 A is the current trajectory of sodium ions in the resting state before and after 10 μM of aconitin for 5 minutes. Control the potential at -140mV, keep the sodium ion channel in a resting state, use a single pulse voltage of +50 mV, last for 3ms, insert, and stimulate once every 30s. The figure shows that after the action of BLA, the sodium ion current does not decrease, therefore, BLA has no blocking effect on the Na channel in the resting state.

[0014] figure 1 B is the current trajectory of sodium ions in the inactivated state before and after 10 μM of aconitin for 5 minutes. Control the potential at -70mV for 10s to depolarize (intercalate) the sodiu...

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Abstract

The invention discloses application of bulleyaconitine A (BLA) used as a state-independent sodium ion channel blocker to the analgesia, and relates to application of a medicine, in particular to application of aconitine alkaloids to the analgesia. The application of the bulleyaconitine A used as the state-independent sodium ion channel blocker to the analgesia is characterized in that the BLA only blocks a neuron sodium ion channel in an open state in a state dependence way, and does not interact with a neuron sodium ion channel in a resting state or an inactivation state. Compared with other analgesic medicines, the medicine in which the bulleyaconitine A is taken as an active ingredient has the advantage that the analgesic side effect is relatively small.

Description

technical field [0001] The invention relates to a drug application, in particular to an application of aconitine alkaloids in analgesia. Background technique [0002] For hundreds of years, the roots of the Aconitum plant have been used extensively in Chinese and Japanese medicine for anesthetic, rheumatic, and nervous effects. There are as many as 10 alkaloids isolated from plants of the genus Aconitum, including various "aconitine" and "hoconitine" diterpenoids. These two diterpene alkaloids have strong anesthetic activity in vivo. In addition, aconitine can irreversibly block the Na ion current, while aconitine can not only reduce the Na ion current, but also activate the voltage-dependent Na ion channel under hyperpolarized conditions, causing the Na ion valve current to increase. Appears as an "activator" of sodium ion channels. As a result of the voltage shift during this activation, aconitine can cause repetitive firing of nerve cells, hyperesthesia, and cardiac ar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/439A61P29/00A61P25/00
Inventor 李彪
Owner YUNNAN HAOPY PHARM LTD
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