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Pharmaceutical composition for treating cerebral apoplexy and acute cerebral infarction

A composition and cerebral apoplexy technology, applied in the field of biomedicine, can solve the problems of undetectable Apelin prototype drug, short half-life, hindering the development of Apelin clinical therapeutic drugs, etc., and achieve the effect of reducing the volume of cerebral infarction and reducing neurological dysfunction.

Active Publication Date: 2021-03-26
温州医科大学慈溪生物医药研究院 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The inventive medicine described by this patented product helps prevent damage from strokes caused by lacking oxygen or blood flow during surgery while also improving brain function after it's done with drugs that block reactive molecules called nitric oxide (NO).

Problems solved by technology

This patented technical problem addressed in this patents relates to finding new therapies for prevention or recovery from strokes due to blockages in blood flow resulting from narrowings called occluders. Current methods like surgery may lead to complications including bleeding, heart attacks, and even worse outcomes. There needs further researches towards developing novel medicines capable of effectively blocking these conditions without causing side effects.

Method used

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  • Pharmaceutical composition for treating cerebral apoplexy and acute cerebral infarction
  • Pharmaceutical composition for treating cerebral apoplexy and acute cerebral infarction
  • Pharmaceutical composition for treating cerebral apoplexy and acute cerebral infarction

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: The solid-phase synthesis of 2-(4-chlorophenyl)-2,2-difluoroacetic acid-QRPRLSHKGPMPF

[0023] (1) Weigh 1mmol of 2-cl-Trt resin in a solid-phase synthesizer, add 15mL of anhydrous dichloromethane (hereinafter referred to as DCM), place on a shaker and shake for 5min to fully swell the 2-Cl-Trt resin ;

[0024] (2) DCM is removed from the solid-phase synthesizer equipped with 2-Cl-Trt resin with ear washing ball;

[0025] (3) Dissolve 0.75 mmol of Fmoc-Phe in 10 mL of anhydrous DCM, add 0.75 mmol of DIPEA, then transfer to the above-mentioned solid-phase synthesizer, add 0.75 mmol of DIPEA, and react at room temperature for 1 h;

[0026] (4) Sealing: remove the reaction liquid in the solid-phase synthesizer with ear washing balls, then wash with 10 mL of anhydrous DCM, each time for 1 min, and wash 5 times in total, add the prepared volume ratio of anhydrous DCM: DIPEA: methanol =17:1:2 solution 20mL, react at room temperature for 10min;

[0027] (5) Re...

Embodiment 2

[0032] Embodiment 2: Experiment of the biological half-life of the target active peptide in rats

[0033] (1) Experimental animal information

[0034] SPF grade SD rats, 16 males, weighing 190g to 210g, were provided by the Experimental Animal Center of Wenzhou Medical University.

[0035] (2) Dosing regimen and plasma sample collection and processing

[0036] Intravenous injection, the dosage was 10mg / kg, the rats were randomly divided into positive control [Pyr1]-Apelin-13 solution group, experimental group 2-(4-chlorophenyl)-2,2-di Fluoroacetic acid-QRPRLSHKGPMPF solution group, a total of 2 groups (n=8), fixed rats, administered through the tail vein. At different time points after administration, 0.2 mL of whole blood was collected through the jugular vein cannula and placed in a 1.5 mL LEDTA-2K anticoagulant centrifuge tube. ) to seal the tube for smooth collection at the next time point. The blood sample was centrifuged at 4000g for 5 minutes at 4°C, the plasma was ...

Embodiment 3

[0042] Example 3: The treatment of 2-(4-chlorophenyl)-2,2-difluoroacetic acid-QRPRLSHKGMPPF for cerebral apoplexy and cerebral infarction

[0043] 3.1 Experimental materials

[0044] Experimental Animals and Breeding

[0045] 2-3 months old, male C57BL / 6J mice, 24-28g, provided by Experimental Animal Center of Wenzhou Medical University. Raising conditions: the room temperature is between 22-24° C., the humidity is between 40-70%, the lighting time is 12 hours alternately between light and dark, and free to drink and eat.

[0046] 3.2 Modeling of tMCAo mice: Mice were fasted for 8-10 hours before surgery and had free access to water. Mice were anesthetized by intraperitoneal injection of chloral hydrate (350 mg / kg). According to the Longa method, the right middle cerebral artery occlusion (middle cerebral artery occlusion) in the monofilament lumen was prepared with 6-0 silica gel-coated nylon monofilament suture (Doccol Corp). , MCAO) model. After 60 minutes of ischemia, ...

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Abstract

The invention relates to a pharmaceutical composition for treating cerebral apoplexy and acute cerebral infarction. The pharmaceutical composition takes active peptide Apelin as an active ingredient,and the structure of the active peptide Apelin is 2-(4-chlorphenyl)-2, 2-difluoroacetic acid-QRPRLSHKGPMPF. The pharmaceutical composition disclosed by the invention has a bidirectional treatment effect on cerebral arterial thrombosis, and can relieve neurological dysfunction of the cerebral arterial thrombosis and reduces the cerebral infarction volume.

Description

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Claims

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Application Information

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Owner 温州医科大学慈溪生物医药研究院
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