title: Synthesis, characterization and biological evaluation of novel neutral fac-M(CO)3(SNO) complexes (M=Re, 99mTc) bearing the o-methoxyphenylpiperazine moiety.
abstract: The synthesis, characterization and biological evaluation of two new neutral tricarbonyl fac-M(CO)(3)(SNO) (M=Re, (99m)Tc) bearing o-methoxyphenylpiperazine as pharmacophore and S-functionalized cysteine or penicillamine as chelators are reported. Competition binding tests showed good affinity for the 5-HT(1A) receptor (8 and 54 nM for 4a and 4b, respectively). Biodistribution studies in healthy animals showed high initial blood and liver uptake, fast blood and tissue depuration and negligible brain uptake.
authors.affiliation: Institute of Radioisotopes, Radiodiagnostic Products, National Centre for Scientific Research Demokritos, Athens, Greece.
authors.forename: A
authors.initials: A
authors.lastname: Chiotellis
authors.forename: C
authors.initials: C
authors.lastname: Tsoukalas
authors.forename: M
authors.initials: M
authors.lastname: Pelecanou
authors.forename: I
authors.initials: I
authors.lastname: Pirmettis
authors.forename: M
authors.initials: M
authors.lastname: Papadopoulos
mesh_terms: D000818:Animals; D003545:Cysteine / Q000737:chemistry* / Q000493:pharmacokinetics*; D007553:Isotope Labeling; D008297:Male; D008657:Metabolic Clearance Rate; D009928:Organ Specificity; D010396:Penicillamine / Q000737:chemistry* / Q000493:pharmacokinetics*; D011427:Propiophenones / Q000737:chemistry / Q000493:pharmacokinetics; D019275:Radiopharmaceuticals / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism*; D013667:Technetium / Q000737:chemistry* / Q000493:pharmacokinetics*; D014018:Tissue Distribution
chemical_list: D011427:Propiophenones; D019275:Radiopharmaceuticals; D044282:Receptor, Serotonin, 5-HT1A; C001724:methoxyphenyl piperazinyl; D013667:Technetium; D010396:Penicillamine; D003545:Cysteine