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Application of aminoadamantane mononitrate compound in preparation of drugs for preventing and treating diseases

A technology of aminoadamantane and compounds, applied in sensory diseases, drug combinations, respiratory diseases, etc.

Active Publication Date: 2017-01-25
GUANGZHOU MAGPIE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

NO has a strong reaction ability with various free radicals and can effectively reduce the number of free radicals, but its synthesis in the body requires the participation of nitric oxide synthase (NOS)

Method used

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  • Application of aminoadamantane mononitrate compound in preparation of drugs for preventing and treating diseases
  • Application of aminoadamantane mononitrate compound in preparation of drugs for preventing and treating diseases
  • Application of aminoadamantane mononitrate compound in preparation of drugs for preventing and treating diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0091] Example 1. The protective effect of aminoadamantane nitrate compounds on cerebellar granule cells.

[0092] Primary isolated neonatal rat cerebellar granule cells were divided into 1.2×10 5 Each well was seeded in a 96-well plate and cultured in BME medium containing 10% FBS+25mM KCl+2mM Glutamine+1% double antibody. After 24 hours, cytarabine at a final concentration of 10 μM was added to inhibit the proliferation of glial cells. From the 4th day, add glucose with a final concentration of 5mM every 4 days to supplement the energy metabolism and water evaporation of the cells, and place them in a cell culture incubator (37°C, 5% CO 2 ) for 10 days. Primary cerebellar granule cells were divided into normal control group, glutamate group, different aminoadamantane nitrate compound pretreatment group and memantine pretreatment control group induced by 200 μM glutamate. Add different concentrations of compounds MN-04, MN-05, MN-06, MN-07, MN-08, MN-09 and memantine (mema...

Embodiment 2

[0093] Example 2. Inhibition of NMDA receptors by aminoadamantane nitrate compounds.

[0094] The inhibitory activity of aminoadamantane nitrate compounds on NMDA receptors in HEK293 cells stably transfected with human NR1 and NR2A was studied by patch clamp technique. We recorded changes in NMDA receptor channel currents using the whole-cell patch clamp technique. The clamping voltage of HEK293 cells was set to -70mV, adding various concentrations of test compounds and L-glutamate solution to stimulate the opening of NMDA channels, and measuring the inhibitory effect of each compound on the increase of L-glutamate-induced current, and then calculating the effect of each compound on NMDA channel The half inhibitory concentration constant IC 50 .

Embodiment 3

[0095] Example 3. Time-concentration curve of nitric oxide in plasma after intravenous administration of MN-08 to rats.

[0096] Eight SD rats weighing 250±20 g were used and randomly divided into two groups, with 4 rats in each group. MN-08 (25 mg / kg) or ISDN (3 mg / kg) was injected into the tail vein, and about 400 μL of blood (using EDTA- K2 anticoagulant), and centrifuged at 3000r / min for 10min to get the supernatant, and stored the plasma sample at -20°C for testing. The NO content in plasma was determined according to the instructions of Beyontien's total nitric oxide detection kit.

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Abstract

The invention provides application of an aminoadamantane mononitrate compound in preparation of drugs for preventing and treating diseases such as glaucoma, vascular dementia, subarachnoid hemorrhage and pulmonary arterial hypertension. Discovered by experiments, the aminoadamantane mononitrate compound can be combined with an NMDA receptor and release nitric oxide (NO), excitatory toxicity of nerve cells induced by glutamic acid can be lowered, the compound plays a role in dilating cerebral blood vessels, cerebral blood flow can be improved, but peripheral blood pressure is not lowered; retinal ganglion cell injury induced by high intraocular pressure can be reduced, and the intraocular pressure is lowered through releasing the NO; in a vascular dementia model, the cerebral blood flow can be improved, motor behavior disorder is relieved, and learning cognitive ability is improved; behavioral abnormality and cerebrovascular spasm induced by subarachnoid hemorrhage can be relieved; discovered by researches on tissue distribution of the drugs, MN-08 can be gathered in pulmonary tissue, in a pulmonary arterial hypertension model, pulmonary blood vessels can be dilated, right ventricular pressure can be lowered, and plumpness of right ventricle can be reduced.

Description

technical field [0001] The invention belongs to the technical field of medicines and relates to new uses of medicines, in particular to the application of aminoadamantane mononitrate compounds in the prevention and treatment of glaucoma, vascular dementia, subarachnoid hemorrhage and pulmonary hypertension. Background technique [0002] (1) Glaucoma and its drug treatment [0003] Glaucoma is an eye disease in which intraocular pressure is intermittently or continuously elevated. Sustained high intraocular pressure can cause damage to various parts of the eyeball and visual function. If it is not treated in time, the visual field can be completely lost and even blind. Glaucoma is one of the three major blindness diseases that cause blindness in humans, with an incidence rate of 1% in the general population and 2% after the age of 45. [0004] Elevated intraocular pressure is considered to be one of the important risk factors for the development of glaucoma disease, and it ...

Claims

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Application Information

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IPC IPC(8): A61K31/21A61P27/06A61P25/28A61P27/02A61P9/12A61P11/00
CPCA61K31/21A61P9/12A61P11/00A61P25/28A61P27/02A61P27/06
Inventor 王玉强孙业伟张在军于沛张高小易鹏
Owner GUANGZHOU MAGPIE PHARMA
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