99mTc bone scanning agents—VI. Gel chromatographic analysis of the plasma protein binding of 99mTc(Sn)pyrophosphate, 99mTc(Sn)MDP and 99mTc(Sn)HMDP

Kroesbergen, J.; Roozen, A.M.P.; Wortelboer, M.R.; Gelsema, W.J.; Ligny, C.L. De

doi:10.1016/s0969-8051(88)80002-7

Cited by 2 publications

(2 citation statements)

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“…The presence of HS in the radiopharmaceutical solution leads to a protein radioactivity uptake equal to the 5% of the total activity, which confirms data attesting a serum protein removal from 5 to 10% of total radioactivity [19], together with the non-linear binding trend, defined as "ionic exchange" between albumin and 99m Tc-diphosphonates complexes. Alternatively, it could be explained by the replication of dynamic equilibrium between free radiopharmaceuticals in blood, available for pharmacodynamic interaction on their own site of action, and the share bound to plasma proteins.…”

Section: Influence Of Serum Protein On 99msupporting

confidence: 79%

In vitro study: binding of ^99mTc-DPD to synthetic amyloid fibrils

Buroni

Persico

Lodola

et al. 2015

Current Issues in Pharmacy and Medical Sciences

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This paper is an report of the investigation of the in vitro binding of 99mTc-DPD for synthetic amyloid fibrils used for the diagnosis of cardiac amyloidosis (CA), as compared with the use of 99mTc-HMDP and 99mTc-PPI. It also includes an inquiry into the role played by Ca2+ ions and serum proteins on binding to amyloid like materials, as well as the saturability and specificity of DPD for fibrils versus amorphous precipitates (AP). In the work, synthetic insulin fibrils (SIF) and AP were characterized by Congo red staining and TEM imaging. An equal amount of three radiopharmaceuticals were then added to fibrils in Ca2+ (0-4.2 mmol/L) or human serum (HS) adjoined samples and radiopharmaceutical uptake was assessed. To test the saturability of amyloid binding sites, a displacement assays with cold DPD was performed, while adding 50-1500 nmol of 99mTc-DPD to SIF or AP, saturation binding tests were subsequently carried out for evaluating its specificity for amyloid. Herein, synthetic fibrils and AP showed conformational differences at TEM and polarized microscopy analysis. In our study, 99mTc-DPD fibrils uptake was seen to be the highest and increased with calcium ions concentration. What is more, serum proteins reduced the bound fraction to the amyloid deposits of about 15%, and the Kd values of 90 nM and 114 nM relative to SIF and AP, respectively, did not significantly differ. We saw that 99mTc-DPD is the best seeker for amyloid fibrils in cardiac amyloidosis, and that Ca2+ concentration positively influenced DPD fibrils binding. Furthermore, the radioactivity bound to the serum protein clear up the idea of nuclide exchanging dynamic balance between amyloid and circulating proteins. Moreover, non-labeled DPD did not exert a competition for 99mTc-DPD binding sites, and, finally, DPD cannot be defined a radiopharmaceutical specific for amyloid deposits.

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Section: Influence Of Serum Protein On 99msupporting

confidence: 79%

In vitro study: binding of ^99mTc-DPD to synthetic amyloid fibrils

Buroni

Persico

Lodola

et al. 2015

Current Issues in Pharmacy and Medical Sciences

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“…The percentage of protein binding was 11.2%, 12.4%, and 14.7% for 99m Tc-MIPrDP, 99m Tc-MIBDP and 99m Tc-MIPeDP, respectively. As known, different protein binding rate has significant influence on the bone uptake of the tracer agent [ 19 ]. Here, with the extension of carbon chain, the plasma protein binding increases and the maximum bone uptake decreases gradually.…”

Section: Resultsmentioning

confidence: 99%

Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging Agents

Qiu¹,

Cheng²,

Lin³

et al. 2011

Molecules

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A series of novel zoledronic acid (ZL) derivatives 1-hydroxy-3-(2-methyl-1H-imidazol-1-yl)propane-1,1-diyldiphosphonic acid (MIPrDP), 1-hydroxy-4-(2-methyl-1H-imidazol-1-yl)butane-1,1-diyldiphosphonic acid (MIBDP), and 1-hydroxy-5-(2-methyl-1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid (MIPeDP) were prepared and successfully labeled with 99mTc in high labeling yields. The in vitro stability and in vivo biodistribution of 99mTc-MIPrDP, 99mTc-MIBDP and 99mTc-MIPeDP were investigated and compared. The biodistribution studies indicate that the radiotracer 99mTc-MIPrDP has highly selective uptake in the skeletal system and rapid clearance from soft tissues. The present findings indicate that 99mTc-MIPrDP holds great potential for use in bone imaging.

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99mTc bone scanning agents—VI. Gel chromatographic analysis of the plasma protein binding of 99mTc(Sn)pyrophosphate, 99mTc(Sn)MDP and 99mTc(Sn)HMDP

Cited by 2 publications

References 10 publications

In vitro study: binding of ^99mTc-DPD to synthetic amyloid fibrils

In vitro study: binding of ^99mTc-DPD to synthetic amyloid fibrils

Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging Agents

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99mTc bone scanning agents—VI. Gel chromatographic analysis of the plasma protein binding of 99mTc(Sn)pyrophosphate, 99mTc(Sn)MDP and 99mTc(Sn)HMDP

Cited by 2 publications

References 10 publications

In vitro study: binding of 99mTc-DPD to synthetic amyloid fibrils

In vitro study: binding of 99mTc-DPD to synthetic amyloid fibrils

Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging Agents

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Product

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In vitro study: binding of ^99mTc-DPD to synthetic amyloid fibrils

In vitro study: binding of ^99mTc-DPD to synthetic amyloid fibrils