Anomalies in hepatobiliary excretion of technetium-99m-MAG3 preparations

Jang

2004

Section: Introductionmentioning

confidence: 99%

Synthesis and biological characterization of ^99mTc(I) tricarbonyl cysteine complex, a potential diagnostic for assessment of renal function

Jang

2004

“…To understand the nature of the impurities, Brandau et al first initiated a thorough HPLC studies and biological investigations on 99m Tc‐MAG 3 and its impurities produced under different methods of complexation reaction. The aforementioned studies on this radiopharmaceutical were repeated by different workers too, with the objective to determine whether those impurities could be eliminated during complex preparation. All these workers were observed apart from the desired 99m Tc‐MAG 3 ; there were four other non‐MAG 3 components in varying proportion depending on the method of complexation and purity of the ligand.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of S‐thiomethyl MAG₃, radiolabelling with technetium‐99m and biological evaluation

Sanyal

Chattopadhyay

Debnath

2012

Protection of the thiolate function of the mercaptoacetyltriglycine (MAG 3 ) by S-thiomethyl group allows automatic deprotection of the protecting group during technetium-99m radiolabelling by transchelation using stannous chloride dihydrate as reductant. Protection of the thiolate group with S-thiomethyl increases the stability of the ligand, desired complex of high radiochemical purity could be prepared under relatively mild labelling condition (at room temperature) omitting the aeration step. The complex prepared from the S-thiomethyl protected MAG 3 ligand were chromatographically (HPLC) and biologically compared with the corresponding complex prepared from the S-benzoylated MAG 3 precursor. This result suggests that technetium-99m complex of MAG 3 could be prepared from S-thiomethylated MAG 3 precursor in comparatively higher purity under relatively milder labelling condition and this method of radiolabelling could be used for the development of less cumbrous single vial MAG 3 kit. Liver1.50 AE 0.26 (2.25 AE 0.31) 4.76 AE 1.72 (4.33 AE 1.34) 2.99 AE 0.79 (2.91 AE 1.24) 4.15 AE 2.42 (4.44 AE 1.55) Intestine 2.29 AE0.44 (2.23 AE 0.33) 2.69 AE 0.58 (2.05 AE 0.16) 3.87 AE 0.84 (3.62 AE 0.59) 2.75 AE 1.93 (2.66 AE 1.64) Kidney 3.07 AE 0.85 (2.48 AE 0.74) 5.47 AE 0.85 (5.32 AE 1.75) 3.21 AE 0.78 (2.53 AE 0.75) 6.73 AE 2.05 (5.39 AE 1.54) Urine 51.92 AE 1.94 (61.03 AE 2.32) 40.52 AE 1.78 (51.21 AE 0.64) 48.87 AE 1.45 (59.95 AE 2.79) 37.64 AE 2.55 (50.24 AE 2.03)Results are expressed as mean AE SD of six mice. In the control set, radiopharmaceuticals were injected to the animals not treated with probenecid.K. Sanyal et al.

Synthesis and biological characteristics of the Technetium‐99m triamide derivatives of mercaptoacetyltriglycine (MAG₃)

Okarvi

Adriaens

Verbruggen

2002

SummaryA number of MAG 3 -derivatives, containing the three-amide functions modified by inverting the sequence -CO-NH-to -NH-CO-in the firstand/or second-amide functions, have been labelled with 99m Tc in order to study the renal characteristics of the resulting MAG 3 -derivatives versus the reference 99m Tc-MAG 3 . The 99m Tc-MAG 3 -derivatives displayed HPLC-profiles similar to that of 99m Tc-MAG 3 . Furthermore, in mice they exhibited biological behaviour comparable or even superior to 99m Tc-MAG 3 , which indicates that the sequence of the first-and/or second-amide bond in 99m Tc-MAG 3 affects the biological behaviour only to a limited degree. However, in baboon the plasma clearance of the 99m Tc-MAG 3 -derivatives was relatively slower than 99m Tc-MAG 3 , which underlines the inter-species variability.