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Oligopeptide capable of relieving analgesic tolerance of morphine in neuropathic pain and application of oligopeptide

A technology for neuropathy and tolerance, applied in the direction of neurological diseases, medical preparations containing active ingredients, peptides, etc., can solve problems such as limiting the clinical application of morphine, increasing pain, and contradictions

Pending Publication Date: 2021-05-28
XUZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, morphine is one of the most effective clinical drugs for quickly relieving various types of pain, but due to the severe drug tolerance caused by its long-term use, it is often necessary to increase the dose, but at the same time it will lead to increased morphine dose and increased pain "Contradictory" phenomenon, limiting the clinical application of morphine

Method used

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  • Oligopeptide capable of relieving analgesic tolerance of morphine in neuropathic pain and application of oligopeptide
  • Oligopeptide capable of relieving analgesic tolerance of morphine in neuropathic pain and application of oligopeptide
  • Oligopeptide capable of relieving analgesic tolerance of morphine in neuropathic pain and application of oligopeptide

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Experimental program
Comparison scheme
Effect test

preparation example Construction

[0033] Preparation of rat neuropathic pain model of the present invention:

[0034] Neuropathic pain model: Prepare the CCI neuropathic pain model according to the method described in the literature (Bennett GJ, et al.Pain, 1988): rats are anesthetized by intraperitoneal injection of 10% chloral hydrate (300mg / kg), and placed in ultra- In the clean bench, the surgical area is prepared for skin iodophor disinfection. Make an oblique incision along the muscle texture on the dorsal limb of the left lower limb, and bluntly separate the biceps femoris muscle to expose the middle and upper part of the sciatic nerve trunk. Use 4-0 silk suture soaked in sterile water for 15 minutes at the bifurcation of the sciatic nerve 4 lanes of ligation (the distance between each lane is 1mm).

[0035] The tightness of the ligature should be suitable for causing slight twitching of the leg on the side of the operation without affecting the blood supply of the epineurium. Then the wound was suture...

Embodiment 1

[0037] Detection of mechanical hyperalgesia: Determination of the analgesic effect and analgesic tolerance of synthetic peptide P10581 and morphine on neuropathic pain in rats.

[0038] (1) Select 180g-220g healthy adult male SD rats and put them into the same cage after numbering their tails (15 rats in total).

[0039] (2) Adapt to the measurement room for 2 hours. After the rats are quiet, use the tapered tip of the 38500-PAM pressure application measurement system (UgoBasile Biological Research Apparatus, Comerio–Varese, Italy) to align the center of the left hind foot of the rat. The rat's mechanical paw withdrawal threshold was measured at a constant force rate (30gf / s), and the maximum measurement time was set at 15s (when the measured value is greater than 450gf, it will cause damage to the rat).

[0040] (3) Record the mechanical paw withdrawal threshold of the left hind paw of the rat. If the paw withdrawal reflex does not appear in the rat after 15 seconds, stop the...

Embodiment 2

[0047] The comparison of the dose dependence of synthetic peptide P10581 on neuropathic pain in rats before and after repeated administration for 9 days (twice a day) was determined.

[0048] The experimental steps of this embodiment are similar to those in Example 1, with some differences:

[0049] (1) In experiment 2, a total of 30 healthy adult male SD rats of 180g-220g were selected. On the 8th day after CCI modeling, the successful modeling rats were randomly divided into 6 groups. Group A was injected with 0.45μg / kg P10581, and group B was injected with 0.9 μg / kg P10581, group C was injected with 1.8 μg / kg P10581, group D was injected with 3.6 μg / kg P10581, group E was injected with 7.2 μg / kg P10581, group F was injected with 8.5 μg / kg P10581, and the mechanical contraction of rats in each group was recorded 1.5 hours later. foot threshold.

[0050] (2) Rats in each group were injected with 7.2 mg / kg P10581 at 5:30 p.m. on the 8th day after modeling, and then continuous...

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Abstract

The invention discloses an oligopeptide capable of relieving analgesic tolerance of morphine in neuropathic pain and application of the oligopeptide. The oligopeptide is polypeptide with an amino acid sequence as shown in SEQ ID NO: 1, and is named as polypeptide P10581. The synthetic peptide P10581 is a polypeptide with an amino acid sequence as shown in SEQ ID NO: 1, not only has certain analgesic effect, but also does not generate tolerance after being used for multiple times, and a low dosage of P10581 can also improve / eliminate morphine tolerance, so that a new thought is provided for clinical treatment of morphine tolerance and development of new drugs in future.

Description

technical field [0001] The invention belongs to the technical field of analgesic drugs, and in particular relates to a short peptide capable of alleviating the analgesic tolerance of morphine in neuropathic pain and its application. Background technique [0002] Opioids such as morphine are an important choice in clinical pain treatment, but repeated use can lead to physiological tolerance and dependence. Its clinical manifestation is mainly analgesic tolerance, which is manifested in that the analgesic effect gradually weakens or even disappears after continuous administration of opioids, and it is necessary to increase the dose of opioids to obtain the same analgesic effect. [0003] At present, morphine is one of the most effective clinical drugs for quickly relieving various types of pain, but due to the severe drug tolerance caused by its long-term use, it is often necessary to increase the dose, but at the same time it will lead to increased morphine dose and increased...

Claims

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Application Information

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IPC IPC(8): C07K14/435A61K38/17A61P25/04
CPCC07K14/43518A61P25/04A61K38/1767
Inventor 唐琼瑶张赭唐明希陈晨滕月王小慧肖燕妹
Owner XUZHOU MEDICAL UNIV
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