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Application of 4-PBA (sodium 4-phenylbutanoate)

An action and drug technology, applied in the field of medicine, can solve the problems of shortened duration, hyperalgesia, weakened analgesic effect, etc., and achieve the effects of improving morphine tolerance, avoiding adverse reactions, and improving analgesic effect.

Inactive Publication Date: 2018-05-15
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Morphine tolerance is mainly manifested as weakened analgesic effect, shortened duration, increased pain after drug withdrawal, and hyperalgesia. In clinical application, a larger dose is required to achieve the ideal analgesic effect, and large doses of morphine will aggravate the adverse reactions of the drug.

Method used

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  • Application of 4-PBA (sodium 4-phenylbutanoate)
  • Application of 4-PBA (sodium 4-phenylbutanoate)
  • Application of 4-PBA (sodium 4-phenylbutanoate)

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: Effect of 4-PBA on the analgesic effect of morphine

[0027] SD rats were injected with 4-PBA and morphine (10ug) intrathecally. After 30 minutes, they flicked their tails in a 55-degree water bath to measure pain. The pain was measured every 30 minutes. The maximum time for each flick was 10s. The experiment was divided into five groups : Normal saline group, morphine group, 4-PBA (5, 15, 50 μg)+morphine group, 7 rats in each group.

[0028] see results figure 1 ,Depend on figure 1 It can be clearly seen that compared with the single injection of morphine, intrathecal injection of 4-PBA and morphine, the tail-flick latency of SD rats is longer, and the greater the dose of 4-PBA, the longer the latency, and can form a significant difference, indicating that the sheath Intra-injection of 4-PBA can improve the analgesic effect of morphine.

Embodiment 2

[0029] Example 2: Effect of 4-PBA on Morphine Tolerance

[0030] SD rats were intrathecally injected with 4-PBA and morphine (10 μg), and 30 minutes later, they flicked their tails in a water bath at 55 degrees to measure pain. Each flick lasted 10 seconds for 7 consecutive days. The experiments were divided into five groups: normal saline group, morphine group, 4-PBA (5, 15, 50 μg) + morphine group, with 7 rats in each group.

[0031] see results figure 2 ,Depend on figure 2 It can be clearly seen that compared with the single injection of morphine, intrathecal injection of 4-PBA and morphine, the tail-flick latency of SD rats is longer, and the greater the dose of 4-PBA, the longer the latency, and can form a significant difference, indicating that the sheath Intra-injection of 4-PBA can improve the analgesic effect of morphine.

Embodiment 3

[0032] Example 3: Effect of 4-PBA on Morphine Dose-Response Curve

[0033] Sham normal saline group, Morphine morphine tolerance group and Morphine+4-PBA injection morphine and 4-PBA group were set up. The morphine tolerance group and the morphine and 4-PBA injection group were injected with intrathecal injection of morphine every half an hour, and the dose of morphine was From low to high (0.5μg, 1μg, 3μg, 6μg, 9μg, 15μg, 48μg, 96μg) measure tail flick to calculate %MPE, that is, (experimental value-basic value) / (10-basic value)*100%, if flick The injection was stopped when the tail time reached 10s, and the experiment was completed within one day.

[0034] see results image 3 , the curve of the morphine tolerance group shifted to the right, indicating that the analgesic effect decreased after morphine tolerance, and the analgesic effect gradually weakened or even disappeared after continuous administration of morphine, and the dose of morphine needed to be increased to obtai...

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Abstract

The invention relates to the technical field of medicines and discloses application of 4-PBA (sodium 4-phenylbutanoate). The invention provides a plurality of application of the 4-PBA in the aspects of improving a morphine pain alleviating effect, improving morphine tolerance and improving caused hyperalgesia, so that effective guarantee is provided for safe drug utilization of morphine in a clinical pain treatment process; the morphine can reach an ideal pain alleviating effect under the same dosage and adverse effects caused by the fact that a large dosage of the morphine is used are avoided.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of 4-PBA. Background technique [0002] Morphine, as a classic opioid, is widely used in the clinical treatment of acute and chronic pain, neuropathic pain and cancer pain. Tolerance to morphine after long-term use limits the clinical application of the drug and becomes a difficult problem in pain diagnosis and treatment. This issue has attracted extensive attention from scholars, and a large number of studies have been conducted from different levels, but the mechanism of morphine tolerance has not yet been fully elucidated. Morphine tolerance is mainly manifested as weakened analgesic effect, shortened duration, intensified pain after drug withdrawal, and hyperalgesia. In clinical application, a larger dose is required to achieve the ideal analgesic effect, and large doses of morphine will aggravate adverse drug reactions. [0003] The main mechanisms involve...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/192A61K31/485A61P25/00A61P35/00A61P29/00
CPCA61K31/192A61K31/485A61K2300/00
Inventor 刘通王兵郭然冯雨陈丽华黄娅
Owner SUZHOU UNIV
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