Synthesis and biological evaluation of technetium(III) mixed-ligand complexes with high affinity for the cerebral 5-HT1A receptor and the alpha-1-adrenergic receptor
- Tc(III) and Re(III) complexes [M(NS3)(CNR)] (M = Re, 99mTc, NS3 = 2,2?,2?-nitrilotris(ethanethiol), CNR = functionalized isocyanide bearing a derivative of WAY 100635) have been synthesized and characterized. Re was used as Tc surrogate for chemical characterization and in vitro receptor-binding studies. For two representatives subnanomolar affinities for the 5-HT1A as well as for the alpha1-adrenergic receptor were reached. Biodistribution studies in rats of the 99mTc complexes showed brain uptakes between 0.3 and 0.5% ID/organ (5 min p.i.). In vitro autoradiography of one 99mTc representative in sections of post mortem human brain indicate its accumulation in 5-HT1A receptor-rich brain regions. However, addition of the specific 5-HT1A receptor agonist 8-OH-DPAT as well as the alpha1-adrenoceptor antagonist prazosin could not substantially block this tracer accumulation. A preliminary SPET study in a monkey showed negligible brain uptake.
Autor*innen: | A. Drews, H.-J. Pietzsch, R. Syhre, S. Seifert, K. Varnäs, H. Hall, C. Halldin, Werner Kraus, P. Karlsson |
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Dokumenttyp: | Zeitschriftenartikel |
Veröffentlichungsform: | Verlagsliteratur |
Sprache: | Englisch |
Titel des übergeordneten Werkes (Englisch): | Nuclear medicine and biology |
Jahr der Erstveröffentlichung: | 2002 |
Verlag: | Elsevier Science Inc. |
Verlagsort: | New York, NY |
Jahrgang/Band: | 29 |
Ausgabe/Heft: | 4 |
Erste Seite: | 389 |
Letzte Seite: | 398 |
Freie Schlagwörter: | 5-HT1A receptor; Alpha 1-adrenergic receptor; Autoradiography; Rhenium; SPET; Technetium-99m |
DOI: | 10.1016/S0969-8051(02)00296-2 |
ISSN: | 0883-2897 |
Verfügbarkeit des Dokuments: | Physisches Exemplar in der Bibliothek der BAM vorhanden ("Hardcopy Access") |
Bibliotheksstandort: | Sonderstandort: Publica-Schrank |
Datum der Freischaltung: | 19.02.2016 |
Referierte Publikation: | Nein |