Novel oxorhenium and oxotechnetium MO(NS)(S)2 complexes in the development of 5-HT1A receptor imaging agents

dc.contributor.author	Τσουκαλάς, Χαράλαμπος	el
dc.contributor.author	Πιρμέττης, Ιωάννης Χ.	el
dc.contributor.author	Πάτσης, Γεώργιος Π.	el
dc.contributor.author	Πελεκάνου, Μαρία	el
dc.contributor.author	Bodó, Katalin	en
dc.date.accessioned	2015-06-09T17:39:04Z
dc.date.available	2015-06-09T17:39:04Z
dc.date.issued	2015-06-09
dc.identifier.uri	http://hdl.handle.net/11400/15608
dc.rights	Αναφορά Δημιουργού-Μη Εμπορική Χρήση-Όχι Παράγωγα Έργα 3.0 Ηνωμένες Πολιτείες	*
dc.rights.uri	http://creativecommons.org/licenses/by-nc-nd/3.0/us/	*
dc.source	http://www.elsevier.com/	en
dc.subject	5-HT1A receptor
dc.subject	Rhenium
dc.subject	Technetium
dc.subject	Ρήνειο
dc.subject	τεχνήτιο
dc.subject	5-ΗΤ1Α υποδοχέας
dc.title	Novel oxorhenium and oxotechnetium MO(NS)(S)2 complexes in the development of 5-HT1A receptor imaging agents	en
heal.type	journalArticle
heal.classification	Technology
heal.classification	Chemical technology
heal.classification	Τεχνολογία
heal.classification	Χημική τεχνολογία
heal.classificationURI	http://id.loc.gov/authorities/subjects/sh85133147
heal.classificationURI	http://skos.um.es/unescothes/C00565
heal.classificationURI	N/A-Τεχνολογία
heal.classificationURI	N/A-Χημική τεχνολογία
heal.keywordURI	http://id.loc.gov/authorities/subjects/sh85133086
heal.contributorName	Ραφτοπούλου, Αικατερίνη Π.	el
heal.contributorName	Τερζής, Αριστείδης	el
heal.contributorName	Παπαδόπουλος, Μηνάς Σ.	el
heal.contributorName	Χιωτέλλης, Ευστράτιος	el
heal.identifier.secondary	DOI: 10.1016/S0162-0134(02)00574-3
heal.language	en
heal.access	campus
heal.publicationDate	2003-01-15
heal.bibliographicCitation	TSOUKALAS, C., PIRMETTIS, I.C., PATSIS, G.P., PELECANOU, M., BODO, K., et al. (2003). Novel oxorhenium and oxotechnetium MO(NS)(S)2 complexes in the development of 5-HT1A receptor imaging agents. Journal of Inorganic Biochemistry. [online] 93 (3-4). p. 213-220. Available from: http://www.elsevier.com/[Accessed 01/02/2003]	en
heal.abstract	The [NS][S]2 mixed-ligand system was applied to synthesize oxorhenium and oxotechnetium complexes of the general formula MO(o-CH3OC6H4N(CH2CH 2)2NCH2CH2S)(p-CH3C 6H4S)2 (M=Re in 1, M=99Tc in 2, and M=99mTc in 3). The bidentate [NS] ligand includes the 1-(2-methoxyphenyl)piperazine moiety which is a fragment of the true 5-HT1A antagonist WAY 100635. The oxorhenium complex 1 was prepared by a ligand exchange reaction using ReOCl3(PPh3)2 as precursor while [Bu4N][99TcOCl4] and 99Tc-gluconate were used as precursors in the synthesis of the oxotechnetium-99 complex 2. Both complexes were characterized by elemental analysis and spectroscopic methods. Crystallographic analysis of 1 showed that the rhenium coordination geometry is trigonal bipyramidal. The basal plane of the trigonal bipyramid is defined by the oxo group and two sulphur atoms, one belonging to the [NS] ligand and the other to an aromatic thiol, while the apical positions are occupied by the nitrogen of the [NS] ligand and the sulphur of the second aromatic thiol. The oxotechnetium-99 complex 2 has almost identical unit cell parameters to those of the oxorhenium complex 1 indicating, in combination with the other analytical data, that the complexes are isostructural. The binding affinity of the oxorhenium complex 1 for the 5-HT1A receptor subtype was determined in rat brain hippocampal preparations (IC50=106 nM). The oxotechnetium-99m complex 3 was prepared by a ligand exchange reaction using 99mTc-glucoheptonate as the precursor. Its structure was established by comparative HPLC studies using the oxotechnetium-99 complex 2 as a reference. Complex 3 was administered by intravenous injection in rats. At 2 min post injection, 0.153% of the injected dose per gram of tissue was measured in rat brain.	en
heal.publisher	Elsevier	en
heal.journalName	Journal of Inorganic Biochemistry	en
heal.journalType	peer-reviewed
heal.fullTextAvailability	true