Phenobarbital derivative and preparation method and application thereof

A technology for phenobarbital and derivatives, which is applied in the field of phenobarbital derivatives and its preparation, can solve the problems of health hazards for operators, high price, and high cost, and achieve full automation, improved detection efficiency, and high accuracy. Improved effect

Active Publication Date: 2012-10-31
苏州博源医疗科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

High-performance liquid chromatography takes a long time, and the sample pretreatment and operation process is extremely complicated, which requires high technical level of the testing personnel; the radioactive rays of the radioimmunoassay method have caused great harm to the health of the operators. Rarely used; the reagents required by the fluorescence polarization method are mainly imported and extremely expensive, and expensive analytical instruments need to be purchased at the same time

Method used

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  • Phenobarbital derivative and preparation method and application thereof
  • Phenobarbital derivative and preparation method and application thereof
  • Phenobarbital derivative and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: Synthesis and structure confirmation of phenobarbital derivatives

[0036] The synthetic route of the phenobarbital derivative shown in formula (IV) is as follows:

[0037]

[0038] Concrete synthetic steps are as follows:

[0039] 1. Synthesis of Compound 2

[0040]

[0041] 1) Accurately weigh 2.5g (9.32mmol) of potassium nitrosodisulfonate (KSO 3 ) 2 NO, Fremy’s salt, and 1.8g (12.70mmol) disodium hydrogen phosphate Na 2 HPO 4 , put them together into beaker A, add 95ml double distilled water to dissolve, and adjust the pH to 7.22;

[0042] 2) Accurately weigh 2.96g (12.76mmol) of compound 1 phenobarbital (purchased from Sigma), put it into beaker B, add 60ml of acetone to dissolve;

[0043] 3) Mix the solutions in beaker A and beaker B and stir vigorously to obtain a purple solution;

[0044] 4) Add the above purple solution into the acetone solution, keep stirring for 10 minutes, filter, and put it in the refrigerator overnight;

[0045] 5)...

Embodiment 2

[0082] Example 2: Synthesis of BSA-phenobarbital immunogen

[0083] The BSA-phenobarbital immunogen is composed of bovine serum albumin BSA and -O-(CH 2 ) n The -COO- groups are connected, and the structural formula is shown in formula (II). The following takes n=4 as an example to introduce its synthesis method in detail:

[0084] 1) Dissolve 20mg of BSA in 5ml of 0.2M, pH=8.5 phosphate buffer solution (PBS), and place the phosphate buffer solution in beaker C;

[0085] 2) Add the following chemicals into the small beaker D and stir to dissolve: 20mg phenobarbital derivatives, 0.35ml dimethylformamide (DMF), 0.35ml ethanol, 0.7ml 10mM, pH=5.0 potassium phosphate buffer solution, 40mg 1-ethyl-3-(-3-dimethylaminopropyl) carbodiimide, 5mg N-hydroxysuccinimide (N-hydroxysuccinimide, Sulfo-NHS), stirred and dissolved at room temperature 30 minutes;

[0086] 3) Add the solution dissolved in the small beaker D to the beaker C dropwise, and stir overnight at 2-8°C to obtain the ...

Embodiment 3

[0088] Embodiment three: the preparation of anti-phenobarbital specific antibody

[0089] The obtained phenobarbital immunogen was inoculated into experimental animal rabbits by conventional methods, and the antiserum was taken after booster immunization. The specific steps were as follows:

[0090] Dilute the synthesized phenobarbital immunogen to 1.0 mg / ml with PBS, then mix 1.0 ml of the antigen solution with Freund's complete adjuvant, and inject the experimental animal rabbit.

[0091] After 2 to 3 weeks, the rabbits were injected once with 1.0 ml of the same antigen solution and Freund's incomplete adjuvant, and then injected once every four weeks, for a total of 4 injections.

[0092] Blood was collected from the above-mentioned experimental animal rabbit, and the anti-phenobarbital specific antibody was obtained by separation and purification. After determination, the titer of the anti-phenobarbital specific antibody is 1:30000.

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Abstract

The invention discloses a phenobarbital derivative, a preparation method thereof, a phenobarbital immunogen directly obtained from the derivative, a phenobarbital specific antibody indirectly obtained from the derivative, and a detection reagent containing the specific antibody. The preparation method has the beneficial effects: a novel phenobarbital derivative is used, so that various main functional radicals of phenobarbital are retained, and higher performance of identifying and distinguishing nonspecific medicaments is realized; the phenobarbital immunogen and phenobarbital antibody with high specificity are prepared from the novel phenobarbital derivative, and do not undergo any cross reaction with the conventional 45 kinds of medicaments; and the phenobarbital detection reagent can be used for detecting a plurality samples simultaneously on a full-automatic biochemistry analyzer, so that high-flux rapid determination of phenobarbital is realized, high accuracy and high specificity are achieved, the accuracy and detection efficiency are greatly increased than before, and full automation of a detection process is realized simultaneously.

Description

technical field [0001] The invention relates to a phenobarbital derivative and a preparation method thereof, as well as the application of the derivative in the preparation of phenobarbital immunogen, anti-phenobarbital specific antibody and phenobarbital detection reagent. Background technique [0002] Phenobarbital (Phenobarbital) structural formula is shown in formula (III): [0003] [0004] Formula (III) [0005] Phenobarbital, also known as luminal, is a drug for sedation and hypnosis. It is suitable for the treatment of insomnia caused by nervous overexcitement. It also has anticonvulsant, antiepileptic and pre-anesthesia administration effects. However, due to the narrow range of its effective therapeutic concentration, the therapeutic effect cannot be achieved when the concentration is low, and after overdose, it will cause headache, fatigue, lack of energy and even coma, severe respiratory and cardiovascular depression, hypotension and shock. Renal failure, de...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/62C07K14/765C07K16/44G01N21/31G01N33/53G01N35/00
Inventor 虞留明张曼田军蔡江丽
Owner 苏州博源医疗科技有限公司
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