Deuterated FP-beta-CIT, preparation method and application thereof

Abstract

The invention discloses deuterated FP-beta-CIT, a preparation method and application thereof, wherein the chemical structural general formula of the deuterated FP-beta-CIT is shown in the specification, R1 is C1-4 alkyl, the hydrogen atom of R1 is not substituted by deuterium or any one or more hydrogen atoms of R1 are substituted by deuterium, R2-R8 are independently H or D, and at least one hydrogen atom in R1-R8 is deuterated. According to the invention, the deuterated FP-beta-CIT is used as a contrast agent, and the contrast agent can be used for detecting a diagnostic marker dopamine transporter of the Parkinson's disease, so that early diagnosis of the Parkinson's disease is realized; the deuterated FP-beta-CIT used in the invention can stably exist in vivo as a contrast agent, and does not cause harm to a human body after multiple times of detection; a standard nuclear magnetic resonance spectrometer can be used for detection, and special equipment is not needed, so that the cost is lower; and conversion of the deuterium mark can be directly monitored by using standard magnetic resonance spectrum acquisition hardware and signal processing, so that the method is simple and practical, the precision is high, the result is reliable, and the metabolic condition can be analyzed in a quantitative positioning manner.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a deuterated FP-β-CIT and its preparation method and application. Background technique [0002] The increasing use of hydrogen and its isotopes in the pharmaceutical industry, for example, studies in magnetic resonance molecular imaging have resulted in two promising isotopic methods for imaging glucose metabolism: Hyperpolarization (HP) 13 C Magnetic resonance imaging (MRI) and deuterium metabolic imaging (DMI). Although 13 There are several possible pathways for C hyperpolarization, but the HP 13 C MRI most often relies on 13 Dynamic nuclear polarization prepolarization of C-labeled substrates followed by rapid dissolution produces massive (albeit transient) signal enhancement four to five orders of magnitude greater than Boltzmann polarization at clinically feasible MRI field strengths, enabling spectral Imaging for targeted metabolic studies. However, 13 The short magn...

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Problems solved by technology

[0005] In view of the above-mentioned deficiencies in the prior art, the purpose of the present invention is to provide a deuterated FP-β-CIT and its preparation method and application, aiming at solving the problem of using positron radionuclides as contrast agents in the prior art, which is difficult for patients. Multiple detections are likely to cause secondary damage, and cannot be used as a tracking problem for the entire metabolic process

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