Determination method of radioactive ligand N2S2-Memantine and brain receptor imaging agent 99mTc-Memantine oil-water distribution coefficient

A technology of oil-water partition coefficient and determination method, applied in the field of nuclear medicine analysis and detection

Inactive Publication Date: 2011-05-11
JIANGSU INST OF NUCLEAR MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently useful abroad[ 18 F], [ 11 C] or [ 123 I] Reports of labeling different types of N-methylaspartate (NMDA) receptor antagonists [6-10] ,but 99m Tc-labeled NMDA receptor imaging agents have not been reported at home and abroad

Method used

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  • Determination method of radioactive ligand N2S2-Memantine and brain receptor imaging agent 99mTc-Memantine oil-water distribution coefficient
  • Determination method of radioactive ligand N2S2-Memantine and brain receptor imaging agent 99mTc-Memantine oil-water distribution coefficient
  • Determination method of radioactive ligand N2S2-Memantine and brain receptor imaging agent 99mTc-Memantine oil-water distribution coefficient

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Experimental program
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Effect test

Embodiment 1N2

[0029] Example 1N 2 S 2 -Determination of oil-water partition coefficient of Memantine

[0030] (1) Solution preparation

[0031] Accurately weigh N 2 S 2 -Memantine 1.0g, put in a 100mL measuring bottle, add an appropriate amount of methanol to dissolve, add methanol to the mark, shake well, and obtain a stock solution with a concentration of 10mg / mL.

[0032] (2) Linear relationship

[0033] Precisely measure an appropriate amount of stock solution, place it in a 10mL measuring bottle, add mobile phase to dilute to the mark, shake well, and obtain mass concentrations of 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1.0mg / mL of standard solutions, respectively, accurately draw 20 μL of each series of standard solutions and inject them into the high-performance liquid chromatograph, and record the peak area. to N 2 S 2 -Memantine mass concentration ρ (mg / mL) is the abscissa, and the peak area A is the ordinate to carry out linear regression to get N 2 S 2 -Memantine'...

Embodiment 2

[0043] The selection of embodiment 2 mobile phase

[0044] The effect of different mobile phases on the separation conditions of water phase and oil phase was investigated. Different proportions of methanol-water systems were selected, and the retention time of the main peak was about 6.5 minutes, but the main components of the oil phase were seriously interfered by impurity peaks, and could not be effectively separated; the separation effect was greatly improved by using acetonitrile-water system, When the ratio of acetonitrile and water is selected to be 2:1, the degree of separation is greater than 1.5; adding a certain proportion of trifluoroacetic acid, the peak shape is better and has a suitable retention time. The chromatograms of the oil phase and the water phase are shown in image 3 , Figure 4 .

Embodiment 3

[0045] Embodiment 3 pH is to the influence of partition coefficient

[0046] Change the water used in step (5) method among the embodiment 1 into 0.1mol / L pH value and be respectively the phosphate buffer saline solution of 2.0, 3.0, 4.0, 5.0, 6.0, 7.0, 7.4, 8.0 and 9.0, measure with the same method N in different pH buffers 2 S 2 -Memantine partition coefficient, see Table 2. Results The partition coefficient of n-octanol-phosphate buffer system was not significantly affected by the pH value of the buffer.

[0047] Table 2 Determination of partition coefficient

[0048]

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Abstract

The invention relates to a measuring method of partition coefficient of oil-water of a radioactive ligand N2S2-Memantine and a brain receptor developer <99m>Tc-Memantine, belonging to the technical field of nuclear medicine analysis detection. A precursor N-(2-(N-(2-mercaptoethyl)) carbamyl methyl)-N-(2-mercaptoethyl)-3, 5-dimethyl adamantane amino acetamide is labeled with the radioactive ligand <99m>Tc and is short for N2S2-Memantine. The method of the invention adopts an HPLC method to measure the partition coefficient of oil-water of the N2S2-Memantine in an octanol-water or octanol-phosphate buffer solution system; when the temperature is 25 DEG C, the partition coefficient lgP of oil-water of the N2S2-Memantine is about 1.70; the measuring method of the partition coefficient of oil-water of the brain receptor developer <99m>Tc-Memantine comprises the following steps: firstly the N2S2-Memantine is labeled with <99m>Tc, then the partition coefficient of oil-water of <99m>Tc-Memantine is measured by a Gamma counter in the octanol-water system and the lgP tends to 1.9. The conclusion is that the N2S2-Memantine and the <99m>Tc-Memantine are both fat-soluble.

Description

technical field [0001] Radioligand N 2 S 2 -Memantine and brain receptor imaging agents 99m The invention discloses a method for measuring the oil-water partition coefficient of Tc-Memantine, which belongs to the technical field of nuclear medicine analysis and detection. Background technique [0002] Pathological studies have confirmed that many mental diseases, including dementia, schizophrenia, Parkinson's disease, etc., are related to the abnormality of NMDA (N-methylaspartic acid) receptors in the brain. Research and develop imaging agents that can effectively quantify NMDA receptors in local brain tissue and the changes in the activity state of the receptors, reveal the physiological and pathological states of the brain at the molecular level, diagnose diseases related to the receptors, and use them to guide reasonable Medication, curative effect evaluation and prognosis judgment are crucial. Currently useful abroad[ 18 F], [ 11 C] or [ 123 I] Reports of labelin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): G01N30/02
Inventor 周杏琴钦晓峰张建康徐希杰颜成龙曹国宪邹美芬
Owner JIANGSU INST OF NUCLEAR MEDICINE
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