Issue 33, 2015

Synthesis, relaxation properties and in vivo assessment of a carborane-GdDOTA-monoamide conjugate as an MRI blood pool contrast agent

Abstract

The synthesis, relaxivity measurements and in vivo assessment of a carborane-GdDOTA-monoamide (CB-GdDOTA-MA) amphiphilic conjugate as a blood pool contrast agent (BPCA) is reported. This BPCA exhibited excellent binding (87.4%) with human serum albumin (HSA) and showed a higher relaxivity value (r1 = 6.8 mM−1 s−1, 7 T) as compared to the clinically used BPCA, MS-325 (r1 = 5.1 mM−1 s−1, 9.4 T) in PBS. The blood pool contrast enhancement (CE) capability of CB-GdDOTA-MA was evaluated by performing MR angiography (MRA) in CF1 mice (n = 4) at a Gd dose of 0.1 mmol per kg body weight. The significant CE of blood vessels persisted for about 3–4 min post-injection (p.i.) and quickly diminishes over time. The significant CE of the bladder for up to 3 h p.i. indicated that the renal system is the primary clearance pathway for CB-GdDOTA-MA. However, the CE of liver tissues and intestine (up to 24 h p.i.) is suggestive of a significant hepatic uptake of the CB-GdDOTA-MA.

Graphical abstract: Synthesis, relaxation properties and in vivo assessment of a carborane-GdDOTA-monoamide conjugate as an MRI blood pool contrast agent

Supplementary files

Article information

Article type
Paper
Submitted
30 Apr 2015
Accepted
14 Jul 2015
First published
15 Jul 2015

Org. Biomol. Chem., 2015,13, 8912-8918

Author version available

Synthesis, relaxation properties and in vivo assessment of a carborane-GdDOTA-monoamide conjugate as an MRI blood pool contrast agent

L. N. Goswami, Q. Cai, L. Ma, S. S. Jalisatgi and M. F. Hawthorne, Org. Biomol. Chem., 2015, 13, 8912 DOI: 10.1039/C5OB00876J

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