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Application of biscoumarin in preparation of anti-epileptic and analgesic drugs

A dicoumarin, anti-epileptic technology, applied in the field of nervous system disease medicines, can solve the problems of changing neuronal excitability, not finding the anti-epileptic activity, analgesia, and influence of dicoumarin or any derivative thereof, Achieving the effect of small side effects and good toxicological safety

Pending Publication Date: 2021-06-11
HEBEI MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention has not found that dicoumarin or any derivative thereof has the effect of affecting Kv7 / M current and significantly changing the mechanism of neuron excitability reports and patents, nor has it been found that dicoumarin or any derivative thereof has antiepileptic activity and analgesia or use it as a raw material to prepare pharmaceutical preparations for the treatment of neuropsychiatric diseases such as epilepsy and pain

Method used

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  • Application of biscoumarin in preparation of anti-epileptic and analgesic drugs
  • Application of biscoumarin in preparation of anti-epileptic and analgesic drugs
  • Application of biscoumarin in preparation of anti-epileptic and analgesic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] electrophysiological patch clamp technique

[0024] (1) Test compound: dicoumarin

[0025] (2) Test method: Cultivation of Chinese hamster ovary cells (CHO): CHO cells stably transfected with KCNQ2 / Q3 channels were cultured in a medium containing 10% fetal bovine serum, 500ug / mL hygromycin and G418, 100U / mL penicillin and strepto Mycin B in DMEM culture solution, trypsinized and passaged. Cells were plated on 12mm round coverslips and cultured in 24-well plates.

[0026] Patch clamp technique to record cell membrane current: HEKA-EPC10 was used as patch clamp amplifier. Amphotericin B (final concentration 0.1-0.2mg / mL) was applied to the electrodes for punch-hole patch-clamp recording. After the microelectrode is polished, fill the inner liquid of the electrode, and control the resistance value at 2-4MΩ. The electrode inner solution used when recording CHO cells is (mM): KCl 160, HEPES 5, MgCl 2 3. CaCl 2 1, EGTA3, adjust pH to 7.4 with KOH; extracellular fluid ...

Embodiment 2

[0029] The pharmacodynamic experiment of embodiment 2 dicoumarins

[0030] Pentetrazole PTZ-induced seizure model:

[0031] Experimental drugs: 2% Tween 20 suspension of dicoumarolum, and 2% Tween 20 suspension of retigabine in the control group. Experimental method: Male mice in each group were injected intraperitoneally with 80 mg / kg of pentylenetetrazole to induce epilepsy, and the latency of seizures, duration of seizures, number of seizures and grades of seizures were observed within 90 minutes. Intraperitoneal injection of dicoumarin, the dosage was 12.5mg / kg, 25mg / kg, 50mg / kg respectively; the dosage of retigabine (RTG) in the control group was 15mg / kg. The experimental results are shown in Table 1, dicoumarol can significantly reduce the duration of epilepsy, the number of seizures and the grade of seizures in a dose-dependent manner. In summary, dicoumarol has significant antiepileptic effect.

[0032]Table 1: Dicoumarol significantly reduces seizure duration, seiz...

Embodiment 3

[0038] Tablets are prepared according to methods known in the art, each containing the following ingredients:

[0039] Dicoumarol 50mg, lactose 70mg, magnesium stearate 3mg, polyvinylpyrrolidone 130mg.

[0040] Capsules are prepared according to methods known in the art, and each capsule contains the following ingredients:

[0041] Dicoumarol 50mg, lactose 70mg, corn starch 25mg, magnesium stearate 1mg, polyvinylpyrrolidone 130mg.

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Abstract

The invention provides an application of biscoumarin in preparation of antiepileptic and analgesic drugs, biscoumarin or any derivative thereof, or a natural, synthetic or semi-synthetic biscoumarin-containing mixture or a biscoumarin-containing composition thereof, which has the effects of increasing Kv7 / M current, remarkably changing the action mechanism of cell excitability. The dicoumarin can be used for preventing, treating and adjunctively treating nervous system diseases and symptoms, the action mechanism of remarkably changing cell excitability by increasing the Kv7 / M current is never reported, and the action mechanism is completely different from the action mechanism of the dicoumarin in the existing medicine application.

Description

technical field [0001] The invention relates to the technical field of drugs for nervous system diseases, in particular to the use of dicoumarin in the preparation of antiepileptic and analgesic drugs. Background technique [0002] Neuropsychiatric disorders are among the diseases of greatest current and future concern, affecting more than half of the population. There is a lack of effective therapeutic drugs for neuropsychiatric diseases, and only a handful of innovative drugs have been marketed at home and abroad in recent years. At the same time, the existing drugs have relatively large adverse reactions, and repeated long-term use produces toxic and side effects such as addiction, memory impairment, movement sensitivity, and free-masking movements. In addition, the domestic market of drugs for the treatment of neuropsychiatric diseases is dominated by imported drugs, and their prices are relatively high. Long-term use has brought serious economic problems. Many neurops...

Claims

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Application Information

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IPC IPC(8): A61K31/37A61P25/08A61P29/00A61P25/00A61P25/24A61P25/22A61P9/10A61P25/20A61P25/18A61P21/02A61P25/16A61P25/28A61P25/14
CPCA61K31/37A61P25/08A61P29/00A61P25/00A61P25/24A61P25/22A61P9/10A61P25/20A61P25/18A61P21/02A61P25/16A61P25/28A61P25/14
Inventor 张凡曹鹏程子豪王玉悦耿丹丹王润萌郑荣李亚宁
Owner HEBEI MEDICAL UNIVERSITY
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