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(175)Yb-TTHMP as a good candidate for bone pain palliation and substitute of other radiopharmaceuticals.

Safarzadeh L - Indian J Nucl Med (2014)

Bottom Line: Biodistribution studies in normal rats were carried out.The results showed favorable biodistribution features of (175)Yb-TTHMP, indicating significant accumulation in bone tissues compared with clinically used bone-seeking radiopharmaceuticals.This research presents (175)Yb-TTHMP can be a good candidate for bone pain palliation and substitute of other radiopharmaceuticals, however, further biological studies in other mammals are still needed.

View Article: PubMed Central - PubMed

Affiliation: Department of Radiation Application Engineering, Shahid Beheshti University, Tehran, Iran.

ABSTRACT
Bone metastasis is one of the most frequent causes of pain in cancer patients. Different radioisotopes such as P-32, Sm-153, Ho-166, Lu-177, and Re-186 with several chemical ligands as ethylenediaminetetramethylene phosphonic acid (EDTMP), 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylene phosphonic acid (DOTMP), and propylenediaminetetramethylene phosphonate (PDTMP) are recommended for bone pain palliation. In this work, (175)Yb-triethylenetetraminehexamethylene phosphonic acid (TTHMP) was produced as a proper alternative to other radiopharmaceuticals. Relatively long half-life (T1/2 = 4.18 days), maximum energy beta particle Eβ =470 keV (86.5%), low abundance gamma emission 396 keV (6.4%), 286 keV (3.01%), 113.8 keV (1.88%) and low cost are considered advantageous of Yb-175 are to wider usage of this isotope; in addition, TTHMP is an ideal carrier moiety for bone metastases. Production, quality control, and biodistribution studies of (175)Yb-TTHMP were targeted. Yb-175 chloride was obtained by thermal neutron bombardment of a natural Yb2O3 sample at Tehran Research Reactor (TRR), radiolabeling was completed in 1 h by the addition of TTHMP at the room temperature and pH was 7.5-8, radiochemical purity was higher than 95%. Biodistribution studies in normal rats were carried out. The results showed favorable biodistribution features of (175)Yb-TTHMP, indicating significant accumulation in bone tissues compared with clinically used bone-seeking radiopharmaceuticals. This research presents (175)Yb-TTHMP can be a good candidate for bone pain palliation and substitute of other radiopharmaceuticals, however, further biological studies in other mammals are still needed.

No MeSH data available.


Related in: MedlinePlus

Chemical structure of ligand
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Figure 1: Chemical structure of ligand

Mentions: The experimental procedure for the synthesis of TTHMP ligand was in accordance with other bisphosphonates as reported. For synthesis of TTHMP, a quantity of 0.48 g (3.3 mmol) of triethylenetetramine was dissolved in 0.75 mL of concentrated HCl and a concentrated aqueous solution of 1.62 g (20 mmol) of phosphorous acid. The resulting solution was heated to reflux temperature and 3.2 mL of 37% aqueous formaldehyde solution (40 mmol) was added dropwise in the course of 1 h to the refluxing solution and refluxing was continued for another 1 h. Chemical structure of TTHMP is shown in Figure 1.


(175)Yb-TTHMP as a good candidate for bone pain palliation and substitute of other radiopharmaceuticals.

Safarzadeh L - Indian J Nucl Med (2014)

Chemical structure of ligand
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4157185&req=5

Figure 1: Chemical structure of ligand
Mentions: The experimental procedure for the synthesis of TTHMP ligand was in accordance with other bisphosphonates as reported. For synthesis of TTHMP, a quantity of 0.48 g (3.3 mmol) of triethylenetetramine was dissolved in 0.75 mL of concentrated HCl and a concentrated aqueous solution of 1.62 g (20 mmol) of phosphorous acid. The resulting solution was heated to reflux temperature and 3.2 mL of 37% aqueous formaldehyde solution (40 mmol) was added dropwise in the course of 1 h to the refluxing solution and refluxing was continued for another 1 h. Chemical structure of TTHMP is shown in Figure 1.

Bottom Line: Biodistribution studies in normal rats were carried out.The results showed favorable biodistribution features of (175)Yb-TTHMP, indicating significant accumulation in bone tissues compared with clinically used bone-seeking radiopharmaceuticals.This research presents (175)Yb-TTHMP can be a good candidate for bone pain palliation and substitute of other radiopharmaceuticals, however, further biological studies in other mammals are still needed.

View Article: PubMed Central - PubMed

Affiliation: Department of Radiation Application Engineering, Shahid Beheshti University, Tehran, Iran.

ABSTRACT
Bone metastasis is one of the most frequent causes of pain in cancer patients. Different radioisotopes such as P-32, Sm-153, Ho-166, Lu-177, and Re-186 with several chemical ligands as ethylenediaminetetramethylene phosphonic acid (EDTMP), 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylene phosphonic acid (DOTMP), and propylenediaminetetramethylene phosphonate (PDTMP) are recommended for bone pain palliation. In this work, (175)Yb-triethylenetetraminehexamethylene phosphonic acid (TTHMP) was produced as a proper alternative to other radiopharmaceuticals. Relatively long half-life (T1/2 = 4.18 days), maximum energy beta particle Eβ =470 keV (86.5%), low abundance gamma emission 396 keV (6.4%), 286 keV (3.01%), 113.8 keV (1.88%) and low cost are considered advantageous of Yb-175 are to wider usage of this isotope; in addition, TTHMP is an ideal carrier moiety for bone metastases. Production, quality control, and biodistribution studies of (175)Yb-TTHMP were targeted. Yb-175 chloride was obtained by thermal neutron bombardment of a natural Yb2O3 sample at Tehran Research Reactor (TRR), radiolabeling was completed in 1 h by the addition of TTHMP at the room temperature and pH was 7.5-8, radiochemical purity was higher than 95%. Biodistribution studies in normal rats were carried out. The results showed favorable biodistribution features of (175)Yb-TTHMP, indicating significant accumulation in bone tissues compared with clinically used bone-seeking radiopharmaceuticals. This research presents (175)Yb-TTHMP can be a good candidate for bone pain palliation and substitute of other radiopharmaceuticals, however, further biological studies in other mammals are still needed.

No MeSH data available.


Related in: MedlinePlus