99mtc marked 2-methoxyphenyl piperazine derivative complexes as well as preparation method and uses thereof

Abstract

The invention relates to a 2-methoxy benzene group piperazine derivative complex marked by radioactive <99m>Tc. The 2-methoxy benzene group piperazine derivative complex considers the <99m>Tc as a central core; one ligand is 2-methoxy benzene group piperazine derivative compound, the structure of which is shown in a formula (A), wherein, n is an integer of 1 to 6; carbon chain length is shown as C1 to C6; the other ligand is one kind of nitrilotriacetic acid, tris (hydroxymethyl) methyl glycine, di (hydroxymethyl) methyl glycine or hydroxyethylethylenediaminetriacetic acid. The complex can beused as 5-HT1A brain receptor imaging agent and has the advantages of simple preparation, low price, high target / non-target ratio etc. The invention also relates to a preparation method of the complex and an application of the complex as the 5-HT1A brain receptor imaging agent.

Description

A 99mTc-labeled 2-methoxyphenylpiperazine complex and its preparation method and application technical field The invention relates to a 99mTc-labeled radioactive complex, especially a 99mTc-labeled 2-methoxyphenylpiperazine complex, a preparation method thereof and application as a 5-HT1A brain receptor imaging agent. Background technique Functional imaging of central nervous system (CNS) receptors has become an important field in radiopharmaceutical research. Changes in neuroreceptor density and function are closely related to neurological and psychiatric disorders (GrossC, ZhuangX, StarkK, et al. SerotoninlAreceptoracts during development to establish normal laxiety-like behavior in an adult [J]. Nature, 2002, 416(6879): 396). In particular, the subtype 5-HT1A of the central neurotransmitter 5-hydroxytryptamine (5-HT) receptor is related to insomnia, anxiety, depression, schizophrenia and senile dementia (Alzheimer's disease). 5-HT1A receptor is a kind of G-protein coup...

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Problems solved by technology

More importantly, although these 99mTc-labeled complexes show high receptor affinity in vitro, the in vivo experimental results are not satisfactory, mainly due to low brain uptake and poor specificity. The possible reason is the lipid solubility of the complexes. Too strong and too much molecular weight, etc.

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