In vivo studies of [125I]iodobenzamide and [11C]iodobenzamide: A ligand suitable for positron emission tomography and single photon emission tomography imaging of cerebral D2 dopamine receptors
- 1 November 1992
- Vol. 12 (3) , 236-241
- https://doi.org/10.1002/syn.890120309
Abstract
Iodobenzamide (IMB) labeled with either [11C] or [125I] was studied in mice and baboons. Pharmacological studies demonstrated an in vivo binding profile compatible with D2 dopamine receptors. Mouse biodistribution studies with both [11C]IMB and [125I]IMB showed a similar brain distribution of radioactivity. Mouse [125I]IMB studies with amphetamine and reserpine pretreatment suggested that IMB may be less susceptible to endogenous dopamine competition for D2 receptor binding in vivo as compared to raclopride. Preliminary baboon studies showed haloperidol competition for IMB binding sites.Keywords
This publication has 28 references indexed in Scilit:
- Preparation of [123I]‐ and [125I]epidepride: A dopamine D‐2 receptor antagonist radioligandJournal of Labelled Compounds and Radiopharmaceuticals, 1991
- Synthesis and in vitro evaluation of 2,3-dimethoxy-5-(fluoroalkyl)-substituted benzamides: high-affinity ligands for CNS dopamine D2 receptorsJournal of Medicinal Chemistry, 1991
- Potential antipsychotic agents. 9. Synthesis and stereoselective dopamine D-2 receptor blockade of a potent class of substituted (R)-N-[(1-benzyl-2-pyrrolidinyl)methyl]benzamides. Relations to other side chain congenersJournal of Medicinal Chemistry, 1991
- Fluoroalkylbenzenes: Synthesis of (S)-2.3-Dimethoxy-5-[(3-fluoro)propyll-6-hydroxy-N-](1-ethyl-2-pyr-rrolidinyl)methyllbenzamideJournal of Fluorine Chemistry, 1991
- Potential antipsychotic agents. 6. Synthesis and antidopaminergic properties of substituted N-(1-benzyl-4-piperidinyl)salicylamides and related compounds. QSAR based design of more active membersEuropean Journal of Medicinal Chemistry, 1990
- Potential antipsychotic agents. 7. Synthesis and antidopaminergic properties of the atypical highly potent (S)-5-bromo-2,3-dimethoxy-N-[(1-ethyl-2-pyrrolidinyl)methyl]benzamide and related compounds. A comparative studyJournal of Medicinal Chemistry, 1990
- Carbon-11 labelling of eticlopride in two different positions—a selective high-affinity ligand for the study of dopamine D-2 receptors using PETInternational Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes, 1990
- In vivo [3H]Spiperone Binding: Evidence for Accumulation in Corpus Striatum by Agonist-Mediated Receptor InternalizationJournal of Cerebral Blood Flow & Metabolism, 1988
- An improved synthesis of (3-N-[11C]methyl)spiperoneInternational Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes, 1986
- Effects of amphetamine on the turnover rate of brain catecholamines and motor activityBritish Journal of Pharmacology, 1972