[en] [5-131I]Iodotropapride is a benzamidic compound which displays high affinity and selectivity for dopaminergic receptors. It was prepared from the corresponding brominated compound by a nucleophilic substitution with [131I]iodine (t1/2 = 8.02 days, E gamma = 364 keV) based on the use of Cu(I) as catalyst and high specific activity of [131I]NaI. After i.v. injection in rats the tracer crosses the blood-brain barrier (0.42 +/- 0.06% of injected dose in the total brain) and demonstrates a high affinity binding to the striatum. The striatum-to-cerebellum ratio increases with time and reaches values of 9 and 22 at 30 and 120 min after injection, respectively. This specific uptake in the striatum is saturable and can be blocked by pretreatment with different D2 antagonists. When labeled with 123I (t1/2 = 13 h, E1 = 159 keV), the corresponding [123I]iodotropapride may be useful for the investigation of the D2 dopamine receptors in humans with single photon emission computer tomography (SPECT).
Research Center/Unit :
GIGA CRC (Cyclotron Research Center) In vivo Imaging-Aging & Memory - ULiège
Disciplines :
Chemistry
Author, co-author :
Cantineau, Robert
Guillaume, Marcel
Damhaut, Philippe; Université de Liège - ULiège > Centre de recherches du cyclotron
Lemaire, Christian ; Université de Liège - ULiège > Centre de recherches du cyclotron
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Bibliography
Brucke, Podreka, Angelberger, Wenger, Topitz, Kufferle, Müller, Deecke (1991) Dopamine D2 receptor imaging with SPECT: studies in different neuropsychiatric disorders. J. Cereb. Bld Flow Metab. 11:220-228.
Brucke, Wenger, Asenbaum, Fertl, Pfafflmeyer, Müller, Podreka, Angelberger (1993) Dopamine D2 receptor imaging and measurement with SPECT. Adv Neurol 60:494-500.
Cantineau, Damhaut, Plenevaux, Lemaire, Guillaume (1991) Synthesis and preliminary animal studies of [131-I]iodotropapride: a cerebral dopamine D2 receptor ligand. J. Labelled Compd. Radiopharm. 30:360-361.
Chalon, Frangin, Guilloteau, Caillet, Guimbal, Schmitt, Desplanches, Baulieu, Besnard (1990) Iodoethylspiperone, a new potential agent for exploration of central dopamine D2 receptors: synthesis and preliminary in vivo study. Nucl. Med. Biol. 17:389-395.
Clanton, de Paulis, Schmidt, Ansari, Manning, Baldwin, Kessler (1991) Preparation of [123I] and [125I]epidepride: a dopamine D2 receptor antagonist radioligand. J. Labelled. Cmpd. Radiopharm. 29:745-751.
Damhaut, Cantineau, Lemaire, Plenevaux, Christiaens, Guillaume (1992) 2- and 4- [18F]fluorotropapride, two specific D2 receptor ligands for positron emission tomography: n.c.a. syntheses and animal studies. Appl. Radiat. Isot. 43:1265-1274.
Gildersleeve, Lin, Wieland, Ciliax, Olson, Young (1989) Synthesis of a high specific activity 125I labeled analog of PK-11195, potential agent for SPECT imaging of the peripheral benzodiazepine binding site. Nucl. Med. Biol. 16:423-429.
Jalfre, Bucher, Dorme, Mocquet, Porsolt (1983) Neuropharmacological profile of MD 790501, a new benzamide derivative. Arch. Int. Pharmacodyn. Ther. 264:232-256.
Kessler, de Paulis, Ansari, Gillespie, Clanton, Smith, Ebert, Manning (1989) High affinity iodine substituted benzamides for SPECT. J. Nucl. Med. 30:803-808.
Kung, Billings, Guo, Blau, Ackerhalt (1988) Preparation and biodistribution of [125I]IBZP: a potential CNS D1 dopamine receptor imaging agent. Nucl. Med. Biol. 15:185-189.
Kung, Guo, Billings, Xu, Mach, Blau, Ackerhalt (1988) Preparation and biodistribution of [125I]IBZP: a potential CNS D2 dopamine receptor agent. Nucl. Med. Biol. 15:195-201.
Kung, Pan, Kung, Billings, Kasliwal, Reilley, Alavi (1989) In vitro and in vivo evaluation of [123I]IBZM: a potential CNS D2 dopamine receptor imaging agent. J. Nucl. Med. 30:88-92.
Kung, Alavi, Chang, Kung, Keyes, Velchik, Billings, Pan, Noto, Rausch, Reilley (1990) In vivo SPECT imaging of CNS D-2 dopamine receptors: initial studies with iodine-123-IBZM in humans. J. Nucl. Med. 31:573-579.
Laduron, Janssen, Leysen (1982) In vivo binding of [3H]ketanserine on serotonin S2-receptors in rat brain. Eur. J. Pharmacol. 81:43-48.
Landvatter (1985) Preparation and purification of [125I]labeled iodospiroperidol. J. Labelled Cmpd. Radiopharm. 22:273-278.
Lever, Musachio, Scheffel, Stathis, Wagner (1989) Synthesis of 125/123I]N-iodoallylspiperone for in vivo studies of dopamine D2 receptors. J. Nucl. Med. 30:803-808.
Leysen (1984) Receptors for neuroleptic drugs. Advances in Human Psychopharmacology , JAI Press, New York; 3:315-356.
Leysen (1989) Use of 5-HT receptor agonists and antagonists for the characterization of their respective receptor sites. Drugs as Tools in Neurotransmitter Research , A.B. Boulton, G.B. Baker, A.V. Jurio, The Humana Press, Clifton, N. J; 12:299-349.
Loc'h, Guillaume, Stulzaft, Cantineau, Ottaviani, Mazière, Mazière (1993) Preparation of [Br-76]-bromotroparide, a new dopamine D2 receptor ligand for PET studies. J. Labelled Cmpd. Radiopharm. 32(20 F):291.
Loc'h, Guillaume, Mazière, Brutesco, Bourguignon, Bottlaender, Syrota, Mazière (1993) Radiohalogens derivatives of tropapride for PET and SPECT investigations of dopamine D2 receptors. J. Nucl. Med. 34(995):211P.
Loonen, Soudijn (1985) Halopemide, a new psychotropic agent. Cerebral distribution and receptor interactions. Pharm. Weekbl., Sci. Ed. 7:1-9.
Martres, Bouthenet, Sales, Sokoloff, Schwartz (1985) Widespread distribution of brain dopamine receptors evidenced with [125I]iodosulpride, a highly selective ligand. Science 228:752-755.
Mazière, Loc'h, Stulzaft, Hantraye, Ottaviani, Comar, Mazière (1986) [76Br]Bromolisuride: a new tool for quantitative in vivo imaging of D2 dopamine receptors. Eur. J. Pharmacol. 127:239-247.
Mazière, Loc'h, Bourguignon, Raynaud, Hantraye, Martinot, Syrota, Mazière (1989) PET and SPECT imaging of D2 brain receptors in baboon and human brain using [76Br] and [123I] lisuride. Eur. J. Nucl. Med. 15:403.
Mertens, Vanryckeghem, Gysemans, Eersels, Finda-Panek, Carlsen (1987) New fast preparation of [123I] labeled radiopharmaceuticals. Eur. J. Nucl. Med. 13:380-381.
Mertens, Bossuyt-Piron, De Geeter, Christiaens, Cantineau, Guillaume, Leysen (1989) Evaluation of pure 2′-[123I]-iodospiperone as a promising tracer for in vivo D2 receptor studies with SPECT. J. Nucl. Med. 30:926-930.
Moerlein, Mathis, Brennan, Budinger (1987) Synthesis and in vivo evaluation of [122I] and [131I] labeled iodoperidol, a potential agent for the tomographic assessment of cerebral perfusion. Nucl. Med. Biol. 14:91-98.
Murphy, Kung, Kung, Billings (1990) Synthesis and characterisation of iodobenzamide analogues: potential D2 dopamine receptor imaging agents. J. Med. Chem. 33:171-178.
Oertel, Tatsch, Schwartz, Kraft, Trenkwalder, Sherer, Weinzierl, Vogl, Kirsch (1992) Decrease of D2 receptors indicated by I-123 iodobenzamides SPECT relates to neurological deficit in treated Wilson's disease. Ann. Neurol. 32:743-748.
Rumigny, Strolin-Benedetti, Dostert (1984) Investigation on central dopaminergic receptors D2 using the antagonistic properties of new benzamides. J. Pharm. Pharmacol. 36:373-377.
Saji, Nakatsuka, Shiba, Tokui, Horiuchi, Yoshitake, Torizuka, Yokohama (1987) Radioiodinated 2′-iodospiperone: a new radioligand for in vivo dopamine receptor study. Life Sci. 41:1999-2006.
Schotte, Janssen, Verwimp, Guillaume, Leysen (1992) [125I]iodotropapride, a new high affinity ligand for dopamine D2 receptors. Proc. “9th Int. Cong. Histochemistry and Citochemistry”, Maastricht, Augustus 30; .
Schwartz, Tatsch, Arnold, Gasser, Trenkwalder, Kirsch, Oertel (1992) I-123-iodobenzamide-SPECT predicts dopaminergic responsiveness in patients with de novo parkinsonism. Neurology 42:556-561.
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