In vivo evaluation of 4-[123I]iodo-N-{2-[4-(6-trifluoromethyl-2-pyridinyl)-1-piperazinyl]ethyl}benzamide, a potential SPECT radioligand for the 5-HT1A receptor
| Autor: | H. Vermeirsch, G. De Ley, R. A. J. O. Dierckx, F. De Vos, Kurt Audenaert, Guido Slegers, D. Leysen, Marleen Vandecapelle |
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| Rok vydání: | 2001 |
| Předmět: |
Male
Cancer Research Biodistribution Ketanserin Pyridines Pharmacology Piperazines Rats Sprague-Dawley Radioligand Assay chemistry.chemical_compound In vivo medicine Radioligand Animals Tissue Distribution Radiology Nuclear Medicine and imaging Benzamide 5-HT receptor Tomography Emission-Computed Single-Photon 8-Hydroxy-2-(di-n-propylamino)tetralin Brain Isolated brain Rats Serotonin Receptor Agonists chemistry Receptors Serotonin Benzamides Molecular Medicine 5-HT1A receptor Serotonin Antagonists Receptors Serotonin 5-HT1 medicine.drug |
| Zdroj: | Nuclear Medicine and Biology. 28:639-643 |
| ISSN: | 0969-8051 |
| DOI: | 10.1016/s0969-8051(01)00223-2 |
| Popis: | 4-[ 123 I]Iodo-N-{2-[4-(6-trifluoromethyl-2-pyridinyl)-1-piperazinyl]ethyl}benzamide (1. 123 I), a potential SPECT 5-HT 1A radioligand, was evaluated in vivo in rats. Biodistribution studies were performed leading to a % ID in the brain of 0.22 at 5 min p.i. No significant differences in % ID/g tissue of the different isolated brain regions (hippocampus, hypothalamus, striatum, cortex and cerebellum) could be demonstrated. Blocking experiments with 8-OH-DPAT, WAY100635 and ketanserin could not show any significant change in tracer uptake in the isolated brain regions. These data suggest that uptake in the brain does not represent binding of 1. 123 I to the 5-HT 1A receptor. |
| Databáze: | OpenAIRE |
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