源自哌啶和氮杂环庚烷的二乙三胺五乙酸（DTPA）类似物的合成：磁共振成像潜在的造影增强剂。

Synthesis of DTPA analogues derived from piperidine and azepane: potential contrast enhancement agents for magnetic resonance imaging.

作者信息

Chong H S, Garmestani K, Bryant L H, Brechbiel M W

机构信息

Chemistry Section, National Cancer Institute, NIH, Bethesda, Maryland, USA.

出版信息

J Org Chem. 2001 Nov 16;66(23):7745-50. doi: 10.1021/jo0106344.

DOI:10.1021/jo0106344

PMID:11701031

Abstract

Two DTPA derivatives (PIP-DTPA and AZEP-DTPA) as potential contrast enhancement agents in MRI are synthesized. The T1 and T2 relaxivities of their corresponding Gd(III) complexes are reported. At clinically relevant field strengths, the relaxivities of the complexes are comparable to that of the contrast agent, Gd(DTPA) which is in clinical use. The serum stability of the (153)Gd-labeled complexes is assessed by measuring the release of (153)Gd from the ligands. The radiolabeled Gd chelates are found to be kinetically stable in human serum for up to at least 14 days without any measurable loss of radioactivity.

摘要

合成了两种作为磁共振成像（MRI）中潜在造影剂增强剂的二乙三胺五乙酸（DTPA）衍生物（哌嗪-DTPA和氮杂环庚烷-DTPA）。报道了它们相应的钆（III）配合物的纵向弛豫率（T1）和横向弛豫率（T2）。在临床相关场强下，这些配合物的弛豫率与临床使用的造影剂钆喷酸葡胺（Gd(DTPA)）相当。通过测量（153）Gd从配体中的释放来评估（153）Gd标记配合物的血清稳定性。发现放射性标记的钆螯合物在人血清中动力学稳定，至少长达14天，且无任何可测量的放射性损失。