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A chimeric peptide based on cannabinoid (r)vd-hpα and neuropeptide ff and its preparation method and application

A technology of chimeric peptides and cannabinoid peptides, applied in the field of biochemistry, can solve problems such as unsatisfactory analgesic effect and obvious analgesic tolerance, and achieve effective analgesic effect and enhanced analgesic activity

Active Publication Date: 2021-07-27
LANZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the analgesic effect of (m)VD-Hpα is still unsatisfactory, and there will be obvious analgesic tolerance during long-term administration

Method used

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  • A chimeric peptide based on cannabinoid (r)vd-hpα and neuropeptide ff and its preparation method and application
  • A chimeric peptide based on cannabinoid (r)vd-hpα and neuropeptide ff and its preparation method and application
  • A chimeric peptide based on cannabinoid (r)vd-hpα and neuropeptide ff and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1VF-11

[0049] The synthesis of embodiment 1VF-11

[0050] (1) Resin pretreatment: Weigh 500 mg of Rink-Amide-MBHA resin, stir and swell in 5 mL of dichloromethane at 80 rpm, the reaction time is 30 min, and drain for 30 min after the reaction. Then add DMF to wash 3 times, each 3min.

[0051] (2) Removal of Fmoc group protection: Add a mixed solution of piperidine with a volume fraction ratio of 1:1:98: DBU:DMF to the swollen resin, and the volume-to-mass ratio of the mixed solution to the swollen resin is 10 mL / g; according to 80rpm stirring 5min, repeat 2 times. After draining, the above mixed solution was added again, and stirred at 80 rpm for 10 min. After that, it was washed 4 times with DMF, each time for 3 min, to remove residual piperidine. Obtain the resin that removes Fmoc protecting group;

[0052] (3) Indene detection: pick a small amount of resin into a colorless transparent glass tube, add indene detection reagent, and place it in boiling water for 3 minutes. If t...

Embodiment 2V

[0057] The synthesis of embodiment 2VF-13

[0058] (1) Resin pretreatment: Weigh 600 mg of Rink-Amide-MBHA resin, stir and swell in 6 mL of dichloromethane at 80 rpm, the reaction time is 30 min, and drain for 30 min after the reaction. Then add DMF to wash 3 times, each 3min.

[0059](2) Removal of Fmoc group protection: Add a mixed solution of piperidine with a volume ratio of 1:1:98: DBU: DMF to the swollen resin, and the volume mass of the mixed solution and the swollen resin is 10mL / g ; According to 80rpm stirring 5min, repeat 2 times. After draining, the above mixed solution was added again, and stirred at 80 rpm for 10 min. After that, it was washed 4 times with DMF, each time for 3 min, to remove residual piperidine. Obtain the resin that removes Fmoc protecting group;

[0060] (3) Indene test: pick a small amount of resin into a colorless and transparent test tube, add indene test reagent, and place it in boiling water for 3 minutes. If the Fmoc group is complete...

Embodiment 3

[0070] Example 3: Analgesic experiments based on chimeric peptides of cannabinoid (r) VD-Hpα and NPFF

[0071] The chimeric peptide based on cannabinoid (r) VD-Hpα and NPFF of the present invention is a brand-new chimeric peptide constructed based on cannabinoid (r) VD-Hpα and NPFF. Side effects of analgesic tolerance. The analgesic and tolerance effects of the chimeric peptides VF-11 and VF-13 of the present invention will be described below through pharmacological experiments.

[0072] 1. Analgesic experiment

[0073] After the compounds VF-11 and VF-13 prepared in Example 1 and Example 2 were injected into the lateral ventricle and intrathecally, the in vivo pain regulation was carried out in the models of acute pain induced by light and heat and inflammatory pain induced by carrageenan Activity detection and comparison of effects.

[0074] (1) Embedding catheter in the lateral ventricle of mice

[0075] Stereotaxic apparatus for the brain is Rui Wo De 68001 type. Kunm...

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Abstract

The present invention discloses a chimeric peptide based on cannabinoid peptide (r)VD-Hpα and neuropeptide FF and its preparation method and application, that is, based on the N-terminal sequence of (r)VD-Hpα and the C-terminal sequence of neuropeptide FF The new chimeric peptides VF‑11 and VF‑13 were constructed. Compared with the prior art, the present invention has the following advantages: (1) Compared with the reported (r) VD-Hpα and (m) VD-Hpα, the analgesic activity of VF-11 and VF-13 in vivo is significantly Enhanced, resulting in a more potent analgesic effect than the parent molecule. (2) VF‑11 and VF‑13 solve the problem of analgesic tolerance of classic cannabinoid agonists and parent molecules, and produce analgesic effects without tolerance, which can be used for the treatment of acute pain and pathological pain .

Description

technical field [0001] The invention belongs to the technical field of biochemistry, and in particular relates to a chimeric peptide based on cannabinoid (r) VD-Hpα and neuropeptide FF, a preparation method and application thereof. Background technique [0002] Pain is a sensory mechanism that humans evolved to protect their integrity. However, some chronic and refractory pain seriously affect people's quality of life, and there are great challenges in clinical treatment. Cannabinoids have been used in the treatment of pain for thousands of years (J Psychoactive Drugs. 1981, 13(1): 23; Pain Res Manag. 2001, 6(2): 80). The cannabinoid system in organisms mainly includes two cannabinoid receptors (CB1 receptor and CB2 receptor), endogenous cannabinoid ligands and related metabolic enzymes. CB1 receptors are widely distributed throughout the body, especially in the central nervous system; the distribution area of ​​CB2 receptors is relatively conservative, mainly expressed in...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K19/00C07K1/36C07K1/16C07K1/34C07K1/04C07K1/06A61K38/08A61K38/10A61P29/00
CPCA61K38/00A61P29/00C07K7/06C07K2319/00
Inventor 方泉许彪张梦娜张润李宁
Owner LANZHOU UNIVERSITY
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