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Aminotadalafil hapten, artificial antigen and preparation method thereof

An aminotadanafil and artificial antigen technology, applied in the biological field, can solve the problems of no aminotadanafil monoclonal antibody, high experimental cost, and difficulty in aminotadalafil antigens.

Active Publication Date: 2017-06-30
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, traditional methods are still used to detect the presence of aminotadalafil in Chinese patent medicines or health care products. The extracted samples must be brought back to the laboratory for analysis, or a large test vehicle is used, which is very difficult. Inconvenient, and the reaction time is long, and the experiment costs a lot
However, there is no relevant report about the monoclonal antibody of aminotadalafil
The design of high titer aminotadalafil antigen is still a difficult point for technicians

Method used

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  • Aminotadalafil hapten, artificial antigen and preparation method thereof
  • Aminotadalafil hapten, artificial antigen and preparation method thereof
  • Aminotadalafil hapten, artificial antigen and preparation method thereof

Examples

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preparation example Construction

[0059] In the embodiment provided by the present invention, the preparation method of the hapten shown in formula I comprises steps:

[0060] 1) Mix 1 part of aminotadalafil with 5-13 parts of cyclic anhydride, dissolve in 30 parts of 1,4-dioxane, and then add 5 drops of triethylamine (pH 7.5) drop by drop , 40-50 ℃ airtight stirring reaction 10-12h. After the reaction, the reaction solution was poured into water, extracted 3 times with 100 parts of ethyl acetate, the combined extracts were washed with anhydrous Na 2 SO 4 After drying and concentrating, a solid is obtained, and the solid product obtained by recrystallization from 75% ethanol is an aminotadalafil derivative.

[0061] 2) Mix 1 part of aminotadalafil derivative with 4-10 parts of aliphatic diamine, stir and react at 130°C for 12 hours, and concentrate the product to near dryness under reduced pressure to obtain an oily crude product; add 50 parts of pure water, ultrasonically disperse and wash After that, the ...

Embodiment 1

[0080] Example 1 Preparation of Aminotadalafil Hapten (Scheme 1: n=1)

[0081] Mix 1 part of aminotadalafil with 10 parts of succinic anhydride, dissolve in 30 parts of 1,4-dioxane, then add 5 drops of triethylamine dropwise, and react under closed stirring at 40°C for 12 hours. After the reaction, the reaction solution was poured into water, extracted 3 times with 100 parts of ethyl acetate, the combined extracts were washed with anhydrous Na 2 SO 4 After drying and concentrating, a solid was obtained, which was recrystallized from 75% ethanol to obtain a solid product that was an aminotadalafil derivative (hapten).

[0082] The structure of the resulting product is characterized by: 1 H NMR (400MHz, DMSO) δ7.72(d, J=7.5Hz, 2H), 7.51(t, J=7.8Hz, 1H), 6.98(s, J=7.9Hz, 1H), 6.91(d, J =7.9Hz,1H),6.86(t,J=7.3Hz,1H),6.79(d,J=7.9Hz,1H),6.21(s,1H),5.94(s,2H),4.83(t,J =28.1Hz, 1H), 3.98(s, 2H), 3.07–2.95(m, 2H), 2.63(t, 2H), 2.50(t, 2H).

Embodiment 2

[0083] Example 2 Preparation of Aminotadalafil Hapten (Scheme 1: n=2)

[0084] After mixing 1 part of aminotadalafil with 10 parts of glutaric anhydride, the subsequent steps are the same as in Example 1.

[0085] The structure of the resulting product is characterized by: 1 H NMR (400MHz, DMSO) δ7.85(d, J=7.8Hz, 2H), 7.41(t, J=7.7Hz, 1H), 7.01(s, J=7.3Hz, 1H), 6.91–6.87(m ,J=8.3Hz,2H),6.80(t,J=7.3Hz,1H),6.19(s,J=8.3Hz,1H),5.94(s,J=7.6Hz,2H),4.82(t,J =8.8Hz, 1H), 4.06(s, J=4.9Hz, 2H), 3.03(d, 2H), 2.39–2.33(m, 4H), 2.10(m, J=4.2Hz, 2H).

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Abstract

The invention relates to the bio-technical field, in particular to an aminotadalafil hapten, an artificial antigen and a preparation method thereof. On the basis of retaining the basic structure of aminotadalafil, the hapten introduces a connection arm structure and an active group for coupling macromolecules, so that coupling with the macromolecules is facilitated; furthermore, the own molecular structure and the basic structure of the aminotadalafil with relatively small molecular weight can be fully exposed after the coupling is completed, and the phenomenon of influence on identification of an animal organism due to the fact that the own molecular structure and the basic structure of the aminotadalafil are covered with the macromolecules. According to the preparation method, the aminotadalafil hapten is coupled with protein through an active esterification method to prepare the artificial antigen, so that the coupling ratio can be 18.2, and the aminotadalafil hapten can be used for immune detection of the aminotadalafil.

Description

technical field [0001] The invention relates to the field of biotechnology, in particular to an aminotadalafil hapten, an artificial antigen and a preparation method thereof. Background technique [0002] Amino Tadalafil (Amino Tadalafil), its chemical formula is C 21 h 18 N 4 o 4 , CAS accession number is 385769-84-6, is a new type of serotonin (5-HT) reuptake inhibitor, water-soluble white or off-white powder, it has the effect of aphrodisiac and delayed treatment of sexual dysfunction. Aminotadalafil can effectively inhibit 5-HT reuptake by inhibiting the 5-HT transporter, increase the concentration of 5-HT in the synaptic space, activate the 5-HT2C and 5-HT1A receptors in the postsynaptic membrane, and play a role in delaying ejaculation , so as to effectively control the symptoms of premature ejaculation in men. However, after taking aminotadalafil, patients will have adverse reactions such as headache, indigestion, dizziness, flushing, nasal congestion, back pain ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/14C07K14/765C07K1/107G01N33/558
CPCC07D471/14C07K14/765C07K19/00G01N33/558
Inventor 卢宇靖蔡森源郭晓路黄宝华张焜
Owner GUANGDONG UNIV OF TECH
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