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Carrier-free 131I-meta-iodobenzylguanidine: comparison of production from meta-diazobenzylguanidine and from meta-trimethylsilylbenzylguanidine.

Publication ,  Journal Article
Mairs, RJ; Gaze, MN; Watson, DG; Skellern, GG; Constable, P; McKellar, K; Owens, J; Vaidyanathan, G; Zalutsky, MR
Published in: Nucl Med Commun
April 1994

Meta-iodobenzylguanidine (MIBG) is a drug which is selectively accumulated by the uptake-1 process in adrenergic tissues. When labelled with 131I, it may be used for the targetted radiotherapy of tumours such as phaeochromocytoma and neuroblastoma. This paper describes the preparation of carrier-free 131I-MIBG by radioiodination of meta-diazobenzylguanidine, and compares this process with one involving iododesilylation of meta-trimethylsilylbenzylguanidine. Both processes result in the formation of carrier-free 131I-MIBG whose specific activity at greater than 3 x 10(16) Bq mol-1 is at least 100 times higher than that of commercially available 131I-MIBG for therapeutic use. The therapeutic use of 131I-MIBG with a higher than usual specific activity is predicted to result in a greater target-to-nontarget ratio, and therefore enhanced efficacy because of an increased therapeutic index. As the radiochemical yield of the process involving the metadiazobenzylguanidine intermediate is only 13%, compared with 98% for the iododesilylation reaction, the latter is the preferred synthetic route.

Duke Scholars

Published In

Nucl Med Commun

DOI

ISSN

0143-3636

Publication Date

April 1994

Volume

15

Issue

4

Start / End Page

268 / 274

Location

England

Related Subject Headings

  • Trimethylsilyl Compounds
  • Radiochemistry
  • Nuclear Medicine & Medical Imaging
  • Magnetic Resonance Spectroscopy
  • Iodobenzenes
  • Iodine Radioisotopes
  • Guanidines
  • Guanidine
  • Gas Chromatography-Mass Spectrometry
  • Diazonium Compounds
 

Citation

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MLA
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Mairs, R. J., Gaze, M. N., Watson, D. G., Skellern, G. G., Constable, P., McKellar, K., … Zalutsky, M. R. (1994). Carrier-free 131I-meta-iodobenzylguanidine: comparison of production from meta-diazobenzylguanidine and from meta-trimethylsilylbenzylguanidine. Nucl Med Commun, 15(4), 268–274. https://doi.org/10.1097/00006231-199404000-00157
Mairs, R. J., M. N. Gaze, D. G. Watson, G. G. Skellern, P. Constable, K. McKellar, J. Owens, G. Vaidyanathan, and M. R. Zalutsky. “Carrier-free 131I-meta-iodobenzylguanidine: comparison of production from meta-diazobenzylguanidine and from meta-trimethylsilylbenzylguanidine.Nucl Med Commun 15, no. 4 (April 1994): 268–74. https://doi.org/10.1097/00006231-199404000-00157.
Mairs RJ, Gaze MN, Watson DG, Skellern GG, Constable P, McKellar K, et al. Carrier-free 131I-meta-iodobenzylguanidine: comparison of production from meta-diazobenzylguanidine and from meta-trimethylsilylbenzylguanidine. Nucl Med Commun. 1994 Apr;15(4):268–74.
Mairs, R. J., et al. “Carrier-free 131I-meta-iodobenzylguanidine: comparison of production from meta-diazobenzylguanidine and from meta-trimethylsilylbenzylguanidine.Nucl Med Commun, vol. 15, no. 4, Apr. 1994, pp. 268–74. Pubmed, doi:10.1097/00006231-199404000-00157.
Mairs RJ, Gaze MN, Watson DG, Skellern GG, Constable P, McKellar K, Owens J, Vaidyanathan G, Zalutsky MR. Carrier-free 131I-meta-iodobenzylguanidine: comparison of production from meta-diazobenzylguanidine and from meta-trimethylsilylbenzylguanidine. Nucl Med Commun. 1994 Apr;15(4):268–274.

Published In

Nucl Med Commun

DOI

ISSN

0143-3636

Publication Date

April 1994

Volume

15

Issue

4

Start / End Page

268 / 274

Location

England

Related Subject Headings

  • Trimethylsilyl Compounds
  • Radiochemistry
  • Nuclear Medicine & Medical Imaging
  • Magnetic Resonance Spectroscopy
  • Iodobenzenes
  • Iodine Radioisotopes
  • Guanidines
  • Guanidine
  • Gas Chromatography-Mass Spectrometry
  • Diazonium Compounds