Study on the reaction kinetics of 99Tcm-labeled BIDP

RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE

Study on the reaction kinetics of ⁹⁹Tc^m-labeled BIDP

LIN Jianguo，

WANG Yan，

LUO Shineng，

QIU Ling，

ZHAI Haozhen

Nuclear Science and Techniques

Vol.22, No.3

pp.174-177

Published in print 20 Jun 2011

DOI：10.13538/j.1001-8042/nst.22.174-177

29600

A novel zoledronic acid derivative, 1-hydroxy-2-(2-butyl-1H-imidazole-1-yl)-ethylidene-1,1- diphosphonic acid (BIDP), was synthesized and labeled with ⁹⁹Tc^m. The detailed kinetic study on the labeling reaction between BIDP and ⁹⁹Tc^m was carried out. The results indicated that the reaction rate constants k were 0.0258, 0.0268, 0.0305, 0.0323, 0.0351 and 0.0384 min^-1 at 0°C, 5°C, 10°C, 15°C, 20°C and 25°C, respectively. From the Arrhenius equation k=A·e^–Ea/(RT), the activation energy E_a of the labeling reaction was calculated to be 10.45 kJ/mol. And the correlation between k and temperature (T) was also deduced as ln k=–1258.8×(1/T)+0.9531. In addition, it was found that in order to get a high radiolabeling yield (RLY) (> 90%), the reaction temperature must be up to 12°C.

99Tcm-BIDPLabeling reaction kineticsReaction rate constant kReaction activation energy EaRadiolabeling yield (RLY)

References

[1]

EI-Mabhouh A A, Mercer J R. Eur J Nucl Med Mol Imaging, 2008, 35: 1240-1248.

[2]

Green J R. J Org Chem, 2005, 690: 2439-2448.

[3]

Ross J R, Saunders Y, Edmonds P M, et al. Health Technol Asses, 2004, 4: 1-16.

[4]

Ogawa K, Mukai T, Arano Y, et al. Nucl Med Biol, 2006, 33: 513-520.

[5]

Garcia E,Schibli R,Schubiger P A. Nucl Sci Tech, 2007, 18: 88-100.

[6]

Shalaby-Rana E, Majd M. J Nucl Med, 2001, 42: 878-883.

[7]

Widler L, Jaeggi K A, Glatt M, et al. J Med Chem, 2002, 45: 3721-3738.

[8]

Wang H Y, Luo S N, Xie M H, et al. Nucl Tech, 2006, 29: 438-441.

[9]

Asikoglu A, Durak F G. Appl Radiat Isot, 2009, 67: 1616-1621.

[10]

Luo S N, Wang H Y, Xie M H, et al. Chin J Nucl Med, 2005, 25: 341-344.

[11]

Guo X H, Luo S N, Wang H Y, et al. Nucl Sci Tech, 2006, 17: 285-288.

[12]

Yan X H, Luo S N, Niu G S, et al. Nucl Sci Tech, 2008, 19: 165-168.

[13]

Niu G S, Luo S N, Yan X H, et al. Nucl Tech, 2008, 31: 698-701.

[14]

Chen C Q, Luo S N, Lin J G, et al. Nucl Sci Tech, 2009, 20: 302-306.

[15]

Lin J G, Luo S N, Chen C Q, et al. Appl Radiat Isot, 2010, 68: 1616-1622.

[16]

Kung H F, Liu B L, Pan S R. Appl Radiat Isot, 1989, 40: 677-681.

[17]

Wei Y, Wang X B, Liu B L, et al. Nucl Tech, 1990, 13: 445-448.

[18]

Luo S N, Xie M H, Fang P, et al. Nucl Tech, 1992, 15: 296-299.

[19]

Liu S, Edwards D S, Harris A R, et al. Appl Radiat Isot, 1997, 48: 1103-1111.

[20]

EI-Mabhouh A A, Angelov C A, Cavell R, et al. Nucl Med Biol, 2006, 33: 715-722.

[21]

Zhu J Q, Wu C Y, Lu C X. Nucl Sci Tech, 2003, 14: 135-137.

[22]

DjokićD D, JankovićD L, NikolićN S. Bioorgan Med Chem, 2008, 16: 4457-4465.