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Multi-target peptide molecules of opium and neuropeptide FF receptors, and preparation and application thereof

A neuropeptide, multi-target technology, applied in the field of biochemical peptide drugs, can solve the problems of unsatisfactory analgesic effect intensity and drug effect time, etc.

Active Publication Date: 2016-11-09
SHANGHAI TIANCI LIFE SCI DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the analgesic effect intensity and drug effect time of this chimeric peptide BN-9 are not ideal enough

Method used

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  • Multi-target peptide molecules of opium and neuropeptide FF receptors, and preparation and application thereof
  • Multi-target peptide molecules of opium and neuropeptide FF receptors, and preparation and application thereof
  • Multi-target peptide molecules of opium and neuropeptide FF receptors, and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0152] Embodiment 1, the synthesis of compound 1

[0153] (1) Resin pretreatment: Weigh 600 mg of Rink-Amide-MBHA resin with a substitution value of 0.43 mmol / g and add it to the synthesizer, then add DCM and stir for 30 min to fully swell the resin and dry the solvent under reduced pressure.

[0154] (2) Removal of Fmoc group protection: Add a mixed solution of hexahydropyridine, DBU, and DMF (the volume ratio of the three is 1:1:98) to the resin that has been swollen and drained of solvent, stir for 5 minutes and then pump Dry, repeat 3 times and then drain. The DMF that was added at the end was stirred for 3 min and then sucked dry. This was repeated 4 times to obtain a resin sample from which the protection of the Fmoc group was removed.

[0155] (3) Indene test: add to the test tube in the following order: resin sample, 0.1 ml reagent ①, 0.2 ml reagent ②, 0.1 ml reagent ③, observe after boiling water bath for 3-10 min. Both the solution and the resin are blue, indicatin...

Embodiment 2

[0160] Embodiment two, the synthesis of compound 2

[0161] (1) Resin pretreatment: Weigh 600 mg of Rink-Amide-MBHA resin with a substitution value of 0.43 mmol / g and add it to the synthesizer, then add DCM and stir for 30 min to fully swell the resin and dry the solvent under reduced pressure.

[0162] (2) Removal of Fmoc group protection: same as Example 1.

[0163] (3) Indene detection: Same as Example 1.

[0164] (4) Condensation of amino acids: N-α-Fmoc protected Fmoc-Phe-OH, N-hydroxybenzotriazole, O-benzotriazole-N,N,N',N'-tetramethyl Urea-hexafluorophosphate was completely dissolved in DMF at a molar ratio of 1:1:1, then added diisopropylethylamine (DIEA) twice the amount of Fmoc-Phe-OH and mixed thoroughly to obtain a mixed solution ; the mixed solution and step (2) obtained by removing the Fmoc group protected resin (the molar ratio of Fmoc-Phe-OH to the resin removed from the Fmoc group protected resin is 1:2.5) was added to the synthesizer, under argon The react...

Embodiment 3

[0168] Embodiment three, the synthesis of compound 3

[0169] (1) Resin pretreatment: Weigh 600 mg of Rink-Amide-MBHA resin with a substitution value of 0.5 mmol / g and add it to the synthesizer, then add DCM and stir for 30 min to fully swell the resin and dry the solvent under reduced pressure.

[0170] (2) Removal of Fmoc group protection: same as Example 1.

[0171] (3) Indene detection: Same as Example 1.

[0172] (4) Condensation of amino acids: N-α-Fmoc protected Fmoc-Phe-OH, N-hydroxybenzotriazole, O-benzotriazole-N,N,N',N'-tetramethyl Urea-hexafluorophosphate is completely dissolved in DMF at a molar ratio of 1:1:1, and then diisopropylethylamine (DIEA) is added to twice the molar amount of Fmoc-Phe-OH and mixed thoroughly to obtain a mixture solution; the mixed solution and the resin obtained in step (2) to remove the Fmoc group protection (the molar ratio of Fmoc-Phe-OH to the resin removed from the Fmoc group protection is 1:2.5) was added to the synthesizer, and ...

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Abstract

The invention discloses multi-target polypeptides of opium and neuropeptide FF receptors; amino acid substitution is performed based on an opium peptide Biphalin and an NPFF chimeric peptide BN-9, and a series of multi-target polypeptides which can activate various receptors of an opium and NPFF system at the same time are obtained. By in-vitro cAMP function identification and identification of body analgesic activity and central side effects and other pharmacological activities, the multi-target polypeptides are indicated to activate the opium and NPFF receptors at the same time, have high-efficiency analgesic activity and cannot generate the analgesic tolerance phenomenon, and moreover, have the advantages of showing low side effects on body temperature, gastrointestinal motility, cardiovascular activity and the like. Therefore, the multi-target polypeptides have high application value in preparation of clinical analgesic drugs.

Description

technical field [0001] The invention relates to a class of multi-target polypeptides that simultaneously activate opioid and neuropeptide FF receptors and a preparation method thereof. The invention also relates to the application of such multi-target polypeptides in the preparation of high-efficiency, low-side-effect analgesics, which belongs to biochemistry field of peptide medicine. Background technique [0002] Pain is a complex physiological and psychological activity. Pain in a physiological state can be used as a warning of damage to the body, but pathological chronic pain or persistent severe pain is an unbearable torture for the body. Therefore, analgesia is an important task faced by medical workers. Clinically, opioid analgesics such as morphine and fentanyl are widely used to treat and relieve various severe pains, such as postoperative pain and cancer pain. However, opioid analgesics can cause serious adverse reactions such as tolerance, addiction, constipati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K1/20C07K1/16C07K1/06C07K1/04A61K38/08A61P25/04
CPCC07K7/06A61K38/00A61P25/04A61P29/00A61K38/08A61K38/10C07K1/04Y02P20/55C07K7/08
Inventor 王锐方泉王子龙
Owner SHANGHAI TIANCI LIFE SCI DEV CO LTD
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