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Polypeptide hydration salt compound and use for anti-depression aspect
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A technology for hydration of salt compounds and peptides, which is applied in chemical instruments and methods, peptides, tripeptides, etc., and can solve the problems that research has not been widely carried out
Inactive Publication Date: 2009-08-05
北京元森康泰医药研究有限公司 +1
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Problems solved by technology
However, the peptidehydrate salt compound and its application in antidepressant and its related research have not been reported, and the research in this direction has not been widely carried out
Method used
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[0049] (a) Weigh 1.0 g of Fmoc-Rink-MBHA resin (loading capacity 0.65 mmol / g), place it in a glass reactor equipped with a sand core plate for silanization, and add 15 ml of DMF to swell the resin for 30 min.
[0050] (b) DMF is filtered off by suction, and 15ml of piperidine / DMF with a concentration of 20% is added to the resin, and reacted for 5 minutes under slight shaking. React for 15 minutes under shaking, and remove the reaction liquid.
[0051] (c) Wash the resin with DMFx2, MeOHx2, and DMFx2, take out a small amount of resin and put it into a small glass test tube, add a drop of ninhydrin detection reagent, react at 110°C for 5 minutes, the solution and resin are dark blue, indicating that Fmoc is completely removed .
[0052] (d) Weigh 0.90g of Fmoc-Tyr(But)-OH amino acid and 0.27g of HOBt, dissolve in 10ml of DMF, add to the reactor, then add 0.304ml of DIC, and shake for 40min.
[0061] Using Fmoc-Gly-OH, Arg, and trans-4-OH-Pro as raw materials, it was prepared according to the same method as in Example 1. The result of mass spectrometry analysis showed that the m / z was 385.36.
[0064] (a) Weigh 1.0 g of Fmoc-Rink-MBHA resin (loading capacity 0.65 mmol / g), place it in a glass reactor equipped with a sand core plate for silanization, and add 15 ml of DMF to swell the resin for 30 min.
[0065] (b) DMF is filtered off by suction, and 15ml of piperidine / DMF with a concentration of 20% is added to the resin, and reacted for 5 minutes under slight shaking. React for 15 minutes under shaking, and remove the reaction solution.
[0066] (c) Wash the resin with DMFx2, MeOHx2, and DMFx2, take out a small amount of resin and put it into a small glass test tube, add a drop of ninhydrin detection reagent, react at 110°C for 5 minutes, the solution and resin are dark blue, indicating that Fmoc is completely removed .
[0067] (d) Weigh 1.03g of Fmoc-Trp(Boc)-OH amino acid and 0.27g of HOBt, dissolve in 10ml of DMF, add to the reactor, then add 0.304ml of DIC, and shake for 40min.
[0068] (e) W...
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Abstract
The invention relates to a polypeptide hydrated salt compound and an application of the polypeptide hydrated salt compound on the anti-depression aspect, which belong to the filed of antidepressant drugs. The invention solves the problems that the antidepressantmedicine is high in side effect and easy to accumulate in the body, has more interaction with other drugs, has poor affinity with the body, and the like in the prior art, and provides a polypeptide hydrated salt compound with the general formula of x-AA1-AA2-AA3-AA4-AA5-ymH2Oz, wherein the x expresses an acyl with 1-3 carbon atoms; and the compound has the cognition of molecules, and the compounds comprise modification at the amino terminal and the carboxyl terminal and substitution of different amino acid residues. The compounds can be used for the anti-depression field separately or in a merged manner, have higher medical potency, as well as specificity and weaker toxic reaction, are not easy to accumulate in the body, have less interaction with other drugs and better affinity with the body and have the cognition of the molecules.
Description
technical field [0001] The invention relates to a novel polypeptide hydrated salt compound and its application in antidepressant, and belongs to the field of antidepressant drugs. Background technique [0002] With the development of human society and the ever-accelerating pace of life, with the aggravation of various stress factors, depression has become a common disease and high incidence in modern society, and the number of depressed patients is on the rise. Depression is a genetically determined biochemical disorder that renders people unable to cope with stress. Although the classic antidepressants have positive curative effects, they have large toxic and side effects, especially anticholinergic and cardiovascular system side effects, which often make it difficult for patients to tolerate long-term treatment, and about 30% of patients with major depression and about 50% Ineffective in patients with atypical depression. Monoamine oxidase inhibitors are limited in clini...
Claims
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Application Information
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