Dephosphorylation and biodistribution of 1‐13C‐phospholactate in vivo. (3rd July 2014)

• Record Type: Journal Article
• Authors: Shchepin, Roman V.; Pham, Wellington; Chekmenev, Eduard Y.
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 57:Number 8(2014)
• Page Start: 517
• Page End: 524
• Publication Date: 2014-07-03
• Subjects: Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3207
• Languages: English
• ISSNs: 0362-4803

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <p>Here, we present a new approach for the delivery of a metabolic contrast agent for <italic>in vivo</italic> molecular imaging. The use of a phosphate‐protecting group that facilitates parahydrogen‐induced polarization of 1‐¹³C‐phospholactate potentially enables the <italic>in vivo</italic> administration of a hydrogenated hyperpolarized adduct. When injected, nonhyperpolarized 1‐¹³C‐phospholactate is retained in the vasculature during its metabolic conversion to 1‐¹³C‐lactate by blood phosphatases as demonstrated here using a mucin 1 mouse model of breast cancer and <italic>ex vivo</italic> high‐resolution ¹³C NMR. This multisecond process is a suitable mechanism for the delivery of relatively short‐lived ¹³C and potentially ¹⁵N hyperpolarized contrast agents using –OH phosphorylated small molecules, which is demonstrated here for the first time as an example of 1‐¹³C‐phospholactate. Through this approach, <sc>dl</sc>‐1‐¹³C‐lactate is taken up by tissues and organs including the liver, kidneys, brain, heart, and tumors according to a timescale amenable to hyperpolarized magnetic resonance imaging.</p> </abstract>