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Novel use of protein kinase B inhibitor

A technology of protein kinase and inhibitor, applied in the field of protein kinase B inhibitor

Inactive Publication Date: 2015-07-22
SHANGHAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Pfizer, Merck and other companies have reported that they have launched preclinical experiments on Akt inhibitors as therapeutic drugs. Although such drugs have not yet been marketed, they are already the focus of drug development.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Observation of different doses of Akt IV alleviating spontaneous pain-related responses in rats

[0020] Put a 75 cm high bracket on the table covered with a glass mirror, and place a 20×20×30cm 3 Transparent plexiglass box, from the mirror on the table to observe the reaction of rat feet after administration. Before the drug injection, the rats were placed in the box 30 minutes in advance to adapt to the experimental environment. After the plantar injection of BmK I, the animals were put back into the detection box, and the spontaneous pain behavior was continuously observed. The nociceptive spontaneous pain response was evaluated by the number of spontaneous foot lifting every 5 minutes, the number of pain attacks (such as screaming, etc.), the total number of foot lifting, and the time of licking and biting the foot. The way of Akt IV administration is to inject 10 μl drug system with doses of 1 μg, 5 μg and 10 μg in the intrathecal L5-L6 space of rats...

Embodiment 2

[0022] Example 2: Observation of Different Doses of Akt IV Relieving Bilateral Mechanical Pain in Rats

example 1

[0023] After the spontaneous pain disappeared substantially in Example 1, the rats were placed on a steel wire grid (1cm 2 ) on a plexiglass box (20×20×30 cm 3 )middle. A series of Von Frey fibers (58011, Stoelting Co., USA) (from 0.6 to 26 g) were used to measure the mechanical withdrawal reflex threshold. It can be measured when the rat's injected hind foot touches the ground and bears normal weight. Stimulate the skin of the plantar center of the hindlimb of the animal on the injection side from under the grid, bend each fiber to an appropriate degree and stay for 2-3 seconds, and the interval between two measurements is 10 seconds. The stimulation intensity of Von Frey fibers ranged from small to large. If there is no withdrawal reflex, continue with a larger grammage of fiber, up to a maximum of 26 g. The minimum gram value that can cause 50% paw withdrawal response was taken as the mechanical paw withdrawal reflex threshold. The mechanical pain threshold was collect...

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Abstract

The invention relates to an application of a protein kinase B inhibitor in preparation of a medicine for relieving inflammatory pain. By intrathecally injecting three dosages of Akt IV into L5-L6 sacrum gap 30 min before injecting the BmK 1, the relieving effects of different dosages of Akt IV in the phenomenon such as experimental spontaneous pain, paroxysmal pain sense grand mal, bilateral mechanical pain sensitive and unilateral heat pain sensitive are researched. The protein kinase B inhibitor is built on an experimental animal inflammatory pain model and a basis for researching the Akt signal pathway related analgesic molecular mechanism and developing a novel analgesic medicine is provided.

Description

technical field [0001] The present invention relates to novel uses of protein kinase B inhibitors. Background technique [0002] Pain is divided into physiological pain and pathological pain. The former is a protective mechanism of the body, while pathological pain usually has a complex pathogenesis, long course of disease, slow recovery, and often persists for a long time. Therefore, it can also be called chronic pain, which can be caused by various etiologies such as trauma, infection, inflammation, and tumors. Dysfunction, difficulty in rehabilitation, and mental depression have become important causes that endanger people's health and affect people's quality of life. Its clinical symptoms include spontaneous pain (Spontaneous pain), hyperalgesia (Hyperalgesia) and abnormal pain (Allodynia). Spontaneous pain refers to pain that occurs spontaneously without external stimuli; hyperalgesia refers to the exaggerated pain response of the body to noxious stimuli; and allodyni...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61P29/00
Inventor 叶品焦云露陈孝明王子逸姜南朱红艳
Owner SHANGHAI UNIV
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