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Medicinal use of securinine

The technology of a drug, haginine, applied in the field of pharmacy, can solve the problems of poor treatment effect and no treatment of obstructive sleep apnea hypopnea syndrome, etc., and achieve the effect of significant technological progress, high cost performance and clear effect

Inactive Publication Date: 2017-12-01
ZHONGSHAN HOSPITAL FUDAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Aiming at the above-mentioned technical problems in the prior art, the present invention provides the application of chogonine in the preparation of drugs for the treatment of obstructive sleep apnea hypopnea syndrome. Appropriate drugs for sleep apnea-hypopnea syndrome and technical issues with poor response to other treatments

Method used

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  • Medicinal use of securinine
  • Medicinal use of securinine
  • Medicinal use of securinine

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Experimental program
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Effect test

Embodiment 1

[0019] After the juvenile rats were anesthetized, the medullary brain slices with a thickness of 10 μm were quickly isolated, and the living hypoglossal motor neurons were located through the structural characteristics and electrophysiological characteristics under the microscope. Single hypoglossal motor neuron firing was continuously recorded by whole-cell patch-clamp technique. Such as figure 1 , which significantly increased the firing of hypoglossal motoneurons when administered with abagiline, this effect had a dose-escalation effect and was successfully eluted (attached figure 1 ). It shows that abapine can significantly excite hypoglossal motor neurons.

Embodiment 2

[0021] Accurately locate the motor nucleus of the hypoglossal nerve (such as figure 2 A, left picture), through the way of drug administration, infusion of ababaine into the hypoglossal nerve motor nucleus of living rats, and finally each animal was sacrificed, and the correct position of the drug nucleus was verified by immunohistochemical method , erroneous data removal (such as figure 2 A right picture). We found that microperfusion of bavinine in the motor nucleus of the hypoglossal nerve can significantly increase the myoelectricity of the genioglossus muscle, and this effect has a dose-escalation effect (eg figure 2 Figure B). By statistical method, we further verified that genioglossine significantly increased the firing of the genioglossus muscle (e.g. figure 2 Figure C). It shows that the centrally administered genioglossine can cause the contraction of the genioglossus muscle and promote the opening of the upper airway by activating the motor neurons of the h...

Embodiment 3

[0023] In the living situation, the genioglossus myoelectricity of rats was recorded, and the genioglossine solution was directly injected into the abdominal cavity of rats. We found that the genioglossus muscle myoelectricity increased significantly, and this effect had an obvious dose-escalation effect (such as image 3 Panels A and B). By statistical method, we further verified that the intraperitoneal administration of genioglossine significantly increased the discharge of the genioglossus muscle, and did not affect the respiratory activity (attached image 3 Figure C). It shows that the genioglossus administered peripherally can also excite the genioglossus muscle, causing the increase of its muscle tone and further opening the upper airway. The decline of genioglossus myoelectricity is an important reason for the pathogenesis of OSAHS. Based on the above data, we have reason to believe that genioglossine has great application value in the prevention and treatment of OSA...

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Abstract

The invention provides use of securinine in preparing medicines for treating OSAHS (obstructive sleep apnea hypopnea syndrome). Peripherally administered securinine reaches hypoglossal nerve motor nuclei through a blood-brain barrier, directly activates the hypoglossal nerve motor neclei by inhibiting GABAA current in the postsynaptic membrane, and further activates the genioglossus muscle through the hypoglossal nerve to enable the genioglossus muscle to contract, so that the collapsed upper airway is reopened to achieve the purpose of treatment of OSAHS. Compared with continuous positive airway pressure ventilation, the securinine has the advantages of high acceptability of patients, no need of being applied continuously throughout the sleep period, cheap price and cost-effective effect. Compared with other drugs, the securinine has the advantages of definite effects, high safety, small side effects, and peripheral administration.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to the use of ababaine, in particular to the application of a kind of ababaine in the preparation of medicines for treating obstructive sleep apnea-hypopnea syndrome. Background technique: [0002] Obstructive sleep apnea-hypopnea-hypopnea syndrome (OSAHS) is a disease with a high incidence and great harm. However, the current treatment methods for OSAHS are limited, and the main treatment method is continuous positive airway pressure. The operation of continuous positive airway pressure is cumbersome, patients have many adverse reactions, and the current treatment compliance is extremely low. Scholars have proposed that drug treatment is the way out to solve the plight of OSAHS treatment. However, as a medical disease, OSAHS is still blank in drug treatment. [0003] The direct cause of OSAHS is the collapse of the soft tissues of the upper airway, mainly the genioglossus muscle, during sle...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/55A61P11/00A61P25/00
CPCA61K31/55
Inventor 刘子龙吴旭符翠萍陆欢曲卫敏黄志力李善群
Owner ZHONGSHAN HOSPITAL FUDAN UNIV
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