Deuterated taltirelin contrast agent

Abstract

The invention discloses a deuterated taltirelin contrast agent. The chemical structural general formula of deuterated taltirelin contrast agent is shown in the specification, wherein R1 is C1-4 alkyl, hydrogen atoms of R1 are not substituted by deuterium or any one or more hydrogen atoms of R1 are substituted by deuterium, R2-R16 are respectively and independently H or D, and at least one hydrogen atom in R1-R16 is substituted by deuterium. The deuterated taltirelin contrast agent provided by the invention can be used as a DMI contrast agent for diagnosing spinocerebellar ataxia, has higher detection resolution and sensitivity, can detect the dynamic exchange of a single metabolite, and by measuring the change of a 1H proton magnetic resonance spectrum, the metabolite which cannot be detected by a 2H proton magnetic resonance spectrum can be detected under the high spectral resolution, so that the in-vivo metabolic cycle rate is obtained, steady state information and metabolic rates of several metabolites can be provided by one-time acquisition, and the human body cannot be hurt by multiple times of detection.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a deuterium-substituted tatirelin contrast agent. 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 magnetization lifeti...

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Problems solved by technology

[0005] In view of the above-mentioned deficiencies in the prior art, the object of the present invention is to provide a deuteretin contrast agent, which aims to solve the problem that the prior art uses positron-type radionuclides as contrast agents, which is easy to cause problems for multiple detections of patients. secondary damage, and cannot be used as a tracking problem for the entire metabolic process

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