Abstract
Gabapentin (GBP) is an anticonvulsant and is widely used in the treatment of epilepsy. In this study, GBP and an allyl derivative of GBP were radioiodinated with 131I using the iodogen method; then their radiopharmaceutical potential in rats and rabbits was investigated. The radiochemical purity of 131I-GBP and its derivatives was determined by RTLC. The labeling yield was 95±2%. Biological evaluation was performed in normal rats and rabbits. Labeled compounds were intravenously injected into two rabbits via the ear vein after anesthetizing. The dynamic and static scintigrams were obtained using a gamma camera at different time. Then the labeled compounds were administered intravenously into the rats. The distribution was studied by counting the radioactivity in the removed organs. The results of biodistribution in the rats showed the clearance of 131I-ALGBP was faster than 131I-GBP. On the other hand, the uptake of 131I-ALGBP in the brain was higher than 131I-GBP at 60 minutes.
Similar content being viewed by others
References
P. Gareri, T. Gravina, G. Ferreri, G. De Sarro, Progr. Neurobiol., 58 (1999) 389.
P. Terrance, G. Snutch Kathy, W. Sutton Gerald, Curr. Opinion Pharmacol., 1 (2001) 11.
S-C. Nirmala, W. Louise, R. H. David, N. W. Geoffrey, European J. Pharmacol.: Molec. Pharmacol., 244 (1993) 293.
J. T. Richard, P. Jason, N. S. Brown, R. H. Gee David, N. W. Geoffrey, European J. Pharmacol.: Molec. Pharmacol., 247 (1993) 341.
R. H. David, S-C. Nirmala, N. W. Geoffrey, European J. Pharmacol.: Molec. Pharmacol., 244 (1993) 303.
T. A. C. Vermeij, P. M. Edelbroek, J. Chromatogr., B810 (2004) 297.
D. Lebsack Alec, J. Gunzner, B. Wang, R. Pracitto, H. Schaffhauser, A. Santini, J. Aiyar, R. Bezverkov, B. Munoz, W. Liu, S. Venkatraman, Bioorg. Medicinal Chem. Lett., 14 (2004) 2463.
J-M. Receveur, J. S. Bryans, M. J. Field, L. Singh, D. C. Horwell, Bioorg. Medicinal Chem. Lett., 9 (1999) 2329.
L. S. Janet, C. P. Taylor, Epilepsy Res., 41 (2000) 155.
U.S. Patent, Appl. Publ., 2004, 2004014940.
F. Y. Lambrecht, K. Durkan, Y. Yildirim, Ç. Acar, Chem. Pharm. Bull., 54 (2006) 245.
K. O. Vollmer, A. Von Hodenberg, E. U. Kolle, Arzneimittelforsch., 36 (1986) 830.
M. A. Rose, P. C. A. Kam, Anaesthesia, 57 (2002) 451.
Author information
Authors and Affiliations
Corresponding author
Rights and permissions
About this article
Cite this article
Akat, H., Yildirim, Y., Yurt Lambrecht, F. et al. Biological distribution of iodo-allyl gabapentin and iodo-gabapentin. J Radioanal Nucl Chem 275, 387–393 (2008). https://doi.org/10.1007/s10967-007-7014-5
Received:
Published:
Issue Date:
DOI: https://doi.org/10.1007/s10967-007-7014-5