title: 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.
authors.affiliation: International Institute of Nano and Molecular Medicine, School of Medicine, University of Missouri, Columbia, MO 65211-3450, USA. hawthornem@missouri.edu.
authors.forename: Lalit N
authors.initials: LN
authors.lastname: Goswami
authors.forename: Quanyu
authors.initials: Q
authors.lastname: Cai
authors.forename: Lixin
authors.initials: L
authors.lastname: Ma
authors.forename: Satish S
authors.initials: SS
authors.lastname: Jalisatgi
authors.forename: M Frederick
authors.initials: MF
authors.lastname: Hawthorne
mesh_terms: D000818:Animals; D001880:Boranes / Q000138:chemical synthesis* / Q000737:chemistry; D003287:Contrast Media / Q000138:chemical synthesis* / Q000737:chemistry; D015637:Gated Blood-Pool Imaging; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D006801:Humans; D018810:Magnetic Resonance Angiography; D008279:Magnetic Resonance Imaging; D051379:Mice; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D012709:Serum Albumin / Q000378:metabolism; D013054:Spectrophotometry, Atomic
chemical_list: D001880:Boranes; D003287:Contrast Media; D006571:Heterocyclic Compounds; D009942:Organometallic Compounds; D012709:Serum Albumin; C050823:gadolinium 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetate