Synthesis and biological evaluation of technetium(III) mixed-ligand complexes with high affinity for the cerebral 5-HT1A receptor and the alpha1-adrenergic receptor

Tricarbonyl M(I) (M = Re, 99mTc) complexes bearing acridine fluorophores: synthesis, characterization, DNA interaction studies and nuclear targeting

“…25 Unless stated otherwise, the syntheses of the ligands and complexes were carried under a nitrogen atmosphere, using standard Schlenk techniques and dry solvents; the work-up procedures were performed under air. Compounds 2-(4-bromobutyl)isoindoline-1,3-dione, 26 Thin layer chromatography (TLC) was done on Merck silica gel 60 F254 plates. Column chromatography was performed with silica gel 60 (Merck).…”

Synthesis and biological evaluation ofS-[11C]methylated mercaptoimidazole piperazinyl derivatives as potential radioligands for imaging 5-HT1Areceptors by positron emission tomography (PET)

“…The compounds 4-[(2-methoxyphenyl)-1-piperazinyl]butylamine (1) and [(2-mercapto-1-methylimidazol-5-yl)methyloxy]succimide (7) were synthesized as described elsewhere. 23,27 All other solvents and chemicals were used as purchased. [ 11 C]CO 2 was produced by the 14 N(p,a) 11 C reaction on a IBA CYCLONE 18/9 cyclotron.…”

“…This finding is consistent with reports in the literature on compounds bearing a 2-methoxyarylpiperazine moiety showing substantial affinity toward alpha1-adrenergic receptor. 23 However, compound 9 displays an 18-fold higher affinity to the alpha1-adrenergic receptor when compared with compound 10, being 3 and 54 nM, respectively. This difference in the binding affinity and consequently in the selectivity is likely to be influenced by the position at which the arylpiperazine pharmacophore is coupled to the 2-mercaptoimidazole ring and/or the presence of the tertiary amide function in the molecule.…”

“…In both cases, we started from 4-[(2-methoxyphenyl)-1-piperazinyl]butylamine (1), which was synthesized according to literature methods. 23 The synthesis of the labelling precursor 3 was accomplished in 50% yield by cyclization of a diethyl acetal derivative (2) with potassium thiocyanate under acidic conditions, which is a common method for the synthesis of 2-mercaptoimidazoles (Scheme 3). 24,25 Amino acetal 2 has been obtained by alkylation of compound 1 with bromoacetaldehyde diethyl acetal.…”

“…23 3 H]prazosin (NEN, 2.5 TBq/mmol) was used as specific radioligand to measure the alpha1-adrenergic receptor binding.…”