RESUMO
Manganese-based contrast agents (MnCAs) have emerged as suitable alternatives to gadolinium-based contrast agents (GdCAs). However, due to their kinetic lability and laborious synthetic procedures, only a few MnCAs have found clinical MRI application. In this work, we have employed a highly innovative single-pot template synthetic strategy to develop a MnCA, MnLMe , and studied the most important physicochemical properties inâ vitro. MnLMe displays optimized r1 relaxivities at both medium (20 and 64â MHz) and high magnetic fields (300 and 400â MHz) and an enhanced r1b =21.1â mM-1 s-1 (20â MHz, 298â K, pHâ 7.4) upon binding to BSA (Ka =4.2×103 â M-1 ). Inâ vivo studies show that MnLMe is cleared intact into the bladder through renal excretion and has a prolonged blood half-life compared to the commercial GdCA Magnevist. MnLMe shows great promise as a novel MRI contrast agent.
RESUMO
Manganese-based contrast agents (MnCAs) have emerged as suitable alternatives to gadolinium-based contrast agents (GdCAs). However, due to their kinetic lability and laborious synthetic procedures, only a few MnCAs have found clinical MRI application. In this work, we have employed a highly innovative single-pot template synthetic strategy to develop a MnCA, MnLMe, and studied the most important physicochemical properties inâ vitro. MnLMe displays optimized r 1 relaxivities at both medium (20 and 64â MHz) and high magnetic fields (300 and 400â MHz) and an enhanced r 1 b=21.1â mM-1 s-1 (20â MHz, 298â K, pHâ 7.4) upon binding to BSA (K a=4.2×103â M-1). Inâ vivo studies show that MnLMe is cleared intact into the bladder through renal excretion and has a prolonged blood half-life compared to the commercial GdCA Magnevist. MnLMe shows great promise as a novel MRI contrast agent.