New preparation of (123I) iodolisuride from the 2-tri-n-butylstannalisuride derivative

作者: L Mauclaire , C Loc’h , E Berthommier , M Ottaviani , H.D Boulanger

DOI: 10.1016/S0969-8051(98)00103-6

关键词: TributyltinChemistryNuclear chemistryRadiochemistrySpecific activityEx vivoDerivative (chemistry)HalogenationIodineLisurideHigh-performance liquid chromatography

摘要: Abstract A simplified and efficient method is described for the preparation of [ 123 I]2-iodolisuride. The radioiodination 3-(9,10-didehydro-6methyl-8a-ergolinyl)-1,1-diethylurea (lisuride) based on tributyltin to I exchange in oxidative conditions. After optimization reaction parameters I]2-iodolisuride was obtained without high performance liquid chromatography purification with radiochemical yields >90% a purity higher than 95%. specific activity product more 500 MBq/nmol. In vitro binding studies striatal membranes ex vivo autoradiography rats showed that I] or 125 prepared using this method, have same radiopharmacological characteristics as radioiodinated iodolisuride Iodogen® method.

参考文章(16)
J. James Frost, Henry N. Wagner, Quantitative imaging : neuroreceptors, neurotransmitters, and enzymes Raven Press. ,(1990)
A. Lewis Farr, Oliver H. Lowry, Rose J. Randall, Nira J. Rosebrough, Protein Measurement with the Folin Phenol Reagent Journal of Biological Chemistry. ,vol. 193, pp. 265- 275 ,(1951)
Y. Samson, B. Mazière, C. Loc'h, M.H. Bourguignon, M. Zilbovicius, H. Chabriat, Y. Agid, A. Syrota, A.M. Bonnet, M. Vidailhet, M. Levasseur, C. Raynaud, In-Vivo SPECT Imaging of D2 Receptor with, Iodine-Iodolisuride: Results in Supranuclear Palsy The Journal of Nuclear Medicine. ,vol. 33, pp. 1481- 1485 ,(1992)
D E Schmidt, R G Manning, M H Ebert, R M Kessler, D Gillespie, J A Clanton, M S Ansari, H E Smith, T de Paulis, High affinity dopamine D2 receptor radioligands. 1. Regional rat brain distribution of iodinated benzamides. The Journal of Nuclear Medicine. ,vol. 32, pp. 1593- 1600 ,(1991)
John Reilley, Sangren Pan, Jeffrey Billings, Hank F. Kung, Mei-Ping Kung, Abass Alavi, Ravindra Kasliwal, In vitro and in vivo evaluation of [123I]IBZM: a potential CNS D-2 dopamine receptor imaging agent. The Journal of Nuclear Medicine. ,vol. 30, pp. 88- 92 ,(1989)
Ray W. Fuller, James A. Clemens, Edmund C. Kornfeld, Harold D. Snoddy, E. Barry Smalstig, Nicholas J. Bach, Effects of (8β)-8-[(Methylthio)methyl]-6-propylergoline on dopaminergic function and brain dopamine turnover in rats Life Sciences. ,vol. 24, pp. 375- 382 ,(1979) , 10.1016/0024-3205(79)90334-5
Christian Pellevoisin, Denis Guilloteau, Jean-Louis Baulieu, Christian Loc'h, Anne-Marie Dognon, Laurent Mauclaire, Jean-Claude Saccavini, Jean-Claude Besnard, Sylvie Chalon, Iodolisuride and iodobenzamide, two ligands for SPECT exploration of the dopaminergic D2 receptors: a comparative study. Synapse. ,vol. 24, pp. 79- 86 ,(1996) , 10.1002/(SICI)1098-2396(199609)24:1<79::AID-SYN8>3.0.CO;2-D
Helmut Wachtel, Wolfgang Kehr, Gerhard Sauer, Central antidopaminergic properties of 2-bromolisuride, an analogue of the ergot dopamine agonist lisuride. Life Sciences. ,vol. 33, pp. 2583- 2597 ,(1983) , 10.1016/0024-3205(83)90342-9
Reinhard Horowski, Helmut Wachtel, Direct dopaminergic action of lisuride hydrogen maleate, an ergot derivative, in mice European Journal of Pharmacology. ,vol. 36, pp. 373- 383 ,(1976) , 10.1016/0014-2999(76)90091-1
Dirk Bier, Klaus Dutschka, E.Joachim Knust, Radiochemical synthesis of [123I]2-iodo-lisuride for dopamine D2-receptor studies Nuclear Medicine and Biology. ,vol. 23, pp. 373- 376 ,(1996) , 10.1016/0969-8051(96)00018-2