A. M. Amin
100
90
80
70
60
50
40
30
20
10
0
100-ml phosphate buffer pH 7, 150mg of CAT, and the reaction
mixture was heated at 70ꢀC for 15minutes. Biodistribution studies
show uptake in organs known to contain adrenoceptors with high
localization in the lungs (85%/g at 60 minutes post-injection). In
vivo blocking experiments have indicated the moderate selectivity
of the 125ITB to b2-adrenoceptor. For practical application,123I-
labeled terbutaline is used for lung imaging. A more efficient
preparative purification system would be needed to ensure that
the iodoterbutaline was separated from any iodo-isomers or any
unlabeled terbutaline.
Heart before blocking
Heart after blocking
Lung before blocking
Lung after blocking
Acknowledgement
The author wishes to thank the editor and the referees of the
JLCR for the cooperation and valuable comments.
Conflict of Interest
0.0
0.5
1.0
1.5
2.0
2.5
3.0
3.5
4.0
4.5
Time post injection (Hour)
The authors did not report any conflict of interest.
Figure 9. Lung & Heart uptake of 125ITB tracer before and after the IV administra-
tion of atenolol (selective b1 blocking agent) 30 minutes before the administration
of 125ITB.
References
[1] G. Zhang, T. J. Dilling, C. W. Stevens, K. M. Forster, Functional Lung
Imaging in Thoracic Cancer Radiotherapy, April 2008, Vol. 15, No.
2, Cancer Control, p112–119.
100
[2] A. Gottschalk, H. D. Sostman, R. E. Coleman, et al. Ventilation-
perfusion scintigraphy in the PIOPED study. Part II. Evaluation of
the scintigraphic criteria and interpretations. J. Nucl. Med. 1993,
34, 1119–1126.
[3] B. Harris, D. Bailey, S. Miles, et al. Objective analysis of tomographic
ventilation-perfusion scintigraphy in pulmonary embolism. Am. J.
Respir. Crit. Care Med. 2007, 175, 1173–1180. Epub 2007 Mar 15.
[4] J. Petersson, A. Sánchez-Crespo, M. Rohdin, et al. Physiological
evaluation of a new quantitative SPECT method measuring regional
ventilation and perfusion. J. Appl. Physiol. 2004, 96, 1127–1136. Epub
2003 Nov 14.
[5] K. Suga. Technical and analytical advances in pulmonary ventilation
SPECT with xenon-133 gas and Tc-99 m-Technegas. Ann. Nucl. Med.
2002, 16, 303–310.
[6] N. Ogasawara, K. Suga, Y. Kawakami, et al. Assessment of regional
lung function impairment in airway obstruction and pulmonary
embolic dogs with combined noncontrast electrocardiogram-gated
perfusion and gadolinium diethylenetriaminepentaacetic acid
aerosol magnetic resonance images. J. Magn. Reson. Imaging 2004,
20, 46–55.
90
80
70
60
50
40
30
20
10
0
Heart before blocking
Heart after blocking
Lung before blocking
Lung after blocking
0.0
0.5
1.0
1.5
2.0
2.5
3.0
3.5
4.0
4.5
Time post injection (Hour)
[7] T. Guerrero, K. Sanders, E. Castillo, et al. Dynamic ventilation imaging
from four-dimensional computed tomography. Phys. Med. Biol.
2006, 51, 777–791. Epub 2006 Jan 25.
[8] T. R. Johnson, B. Krauss, M. Sedlmair, et al. Material differentiation by
dual energy CT: initial experience. Eur. Radiol. 2007, 17, 1510–1517.
Epub 2006 Dec 7.
Figure 10. Lung & Heart uptake of 125ITB tracer before and after the IV adminis-
tration of Butoxamine (selective b2 blocking agent)30 minutes before the adminis-
tration of 125ITB.
[9] M. F. Vidal Melo, D. Layfield, R. S. Harris, et al. Quantification of
regional ventilation perfusion ratios with PET. J. Nucl. Med. 2003,
44, 1982–1991.
from Figure 10. The uptake of the heart in comparison with the
uptake of the lungs was very low that may indicate the moderate
selectivity of the tracer to b2-adrenoceptor.
[10] G. Musch, J. D. Layfield, R. S. Harris, et al. Topographical distribution
of pulmonary perfusion and ventilation, assessed by PET in supine
and prone humans. J. Appl. Physiol. 2002, 93, 1841–1851.
[11] H. J. Mersmann. Overview of the effects of beta-adrenergic receptor
agonists on animal growth. J. Anim. Sci. 1998, 76, 160–172.
[12] S. B. Liggett, J. R. Raymond. Pharmacology and molecular biology of
adrenergic receptors. Baillieres Clin. Endocrinol. Metab. 1993, 7, 279–
305.
[13] P. J. Brnes, Neural Control of Airway Smooth Muscle" In The Lung
(Eds.: R. G. Crystal, J. B. West), Raven Publishers: Philadelphia, 1997,
pp. 1269.
[14] A. D. Strosberg. Biotechnology of b-adrenergic receptors. Mol. Neurobiol.
1990, 4, 211–250.
Conclusion
The receptor targeting agent molecules are even small in size
and are generally organic ligands far from all restrictions keeping
in view the need of a safe, convenient, stable, and particularly
cheap radiopharmaceutical for lung scanning agent. Iodine-
terbutaline is a partial selective radioligand suitable to study lung
function and could be prepared easily under normal conditions.
Terbutraline has been successfully labeled with radioactive
iodine-125. The optimum conditions of the labeling of terbutaline
to give a radiochemical yield of 97% were 200-mg terbutaline in
[15] F. Aigbirhio, V. W. Pike, E. Francotte, K. A. Jaeggi, S. L. Waters, J. Label.
Compd. Radiopharm. 1992, 31, 159.
[16] P. H. Elsinga, A. van Waarde, K. A. Jaeggi, G. Schreiber, M. Heldoom,
W. Vaalburg, J. Med. Chem. 1997, 40, 3829.
Copyright © 2012 John Wiley & Sons, Ltd.
J. Label Compd. Radiopharm 2012