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Titolo:
Development of novel mixed-ligand oxotechnetium [SNS/S] complexes as potential 5-HT1A receptor imaging agents
Autore:
Papagiannopoulou, D; Pirmettis, I; Maina, T; Pelecanou, M; Nikolopoulou, A; Chiotellis, E; Raptopoulou, CP; Vlahos, AT; Terzis, A; Papadopoulos, M; Chiotellis, E;
Indirizzi:
Natl Ctr Sci Res Demokritos, Inst Radioisotopes Radiodiagnost Prod, GR-15310 Athens, Greece Natl Ctr Sci Res Demokritos Athens Greece GR-15310 -15310 Athens, Greece Natl Ctr Sci Res Demokritos, Inst Biol, GR-15310 Athens, Greece Natl Ctr Sci Res Demokritos Athens Greece GR-15310 -15310 Athens, Greece Natl Ctr Sci Res Demokritos, Inst Sci Mat, GR-15310 Athens, Greece Natl Ctr Sci Res Demokritos Athens Greece GR-15310 -15310 Athens, Greece
Titolo Testata:
JOURNAL OF BIOLOGICAL INORGANIC CHEMISTRY
fascicolo: 3, volume: 6, anno: 2001,
pagine: 256 - 265
SICI:
0949-8257(200103)6:3<256:DONMO[>2.0.ZU;2-G
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; IN-VITRO; RHENIUM(V); TECHNETIUM(V); DIRECTIONS;
Keywords:
oxotechnetium complexes; 5-hydroxytryptamine 1A receptor; single-photon emission computed tomography imaging;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
31
Recensione:
Indirizzi per estratti:
Indirizzo: Chiotellis, E Natl Ctr Sci Res Demokritos, Inst Radioisotopes Radiodiagnost Prod, GR-15310 Athens, Greece Natl Ctr Sci Res Demokritos Athens GreeceGR-15310 Greece
Citazione:
D. Papagiannopoulou et al., "Development of novel mixed-ligand oxotechnetium [SNS/S] complexes as potential 5-HT1A receptor imaging agents", J BIOL I CH, 6(3), 2001, pp. 256-265

Abstract

The "3+1" ligand system [SN(R)S/S combination] was applied in order to synthesize neutral mixed-ligand oxotechnetium complexes of the general formula(99)mTcO[SN(R)S]/[S] as potential 5-HT1A receptor imaging agents. The complexes are carrying the 1-(2-methoxyphenyl)piperazine moiety, a fragment of the true 5-HT1A antagonist WAY 100635, either on the monodentate ligand [S]or on the tridentate ligand [SN(R)S]. The complexes MO[EtN(CH2CH2S)(2)] [o-MeOC6H4N(CH2CH2)(2)NCH2CH2S] (3), MO[o-MeOC6H4N(CH2CH2)(2)N(CH2)(3)N(CH2CH2S)(2)][PhS] (6) and MO[o-MeOC6H4N(CH2CH2)(2)N(CH2)(3)N(CH2CH2S)(2)] [PhCH2CH2S] (9), where M=(99)mTc, were prepared at tracer level using (99)mTc glucoheptonate as precursor. For structural characterization. the analogous oxorhenium (M=Re, 1, 4 and 7, respectively) and oxotechnetium (M=Tc-99g, 2, 5and 8, respectively) complexes were prepared by ligand exchange reactions. All products were characterized by elemental analysis and spectroscopic methods. Complexes 1, 4 and 7 were further characterized by crystallographic analysis. For 1, the coordination geometry about rhenium can be described as trigonally distorted square pyramidal (tau =0.36), while for 4 and 7, as distorted trigonal bipyramidal (tau =0.66 and tau =0.61, respectively). Thecoordination sphere about oxorhenium in all complexes is defined by the SNS donor atom set of the tridentate ligand and the sulfur atom of the monodentate coligand. The structure of the Tc-99m complexes 3, 6 and 9 was established by comparative HPLC using authentic oxorhenium and oxotechnetium samples. The binding affinity of oxorhenium compounds for the 5-HT1A receptor subtype was determined in rat brain hippocampal preparations (IC50=6-31 nM). Preliminary tissue distribution data in healthy mice revealed the ability of all three Tc-99m complexes to cross the intact blood-brain barrier (0.49-1.15% ID at 1 min p.i.). In addition, complexes 6 and 9 showed significantbrain retention. These promising results have demonstrated that the SNS/S mixed-ligand system can be used in the development of Tc-99m complexes as potential 5-HT1A receptor imaging agents.

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Documento generato il 26/01/20 alle ore 09:59:55