Parameters ruling optimization of radiolabelling of polyamino polycarboxylated functionalized peptide derivatives: a case study report.

Parameters studies revealed that successful labeling of DTPA-Neurotensin(8-13) analogues depend on several physico-chemical parameters. The pH of the reaction mixture seemed to be the most critical parameter for obtaining high labeling yields; quantitative radiolabelling was only guaranteed at a pH between 4.2 and 5.

123I-5-I-R91150, a new single-photon emission tomography ligand for 5-HT2A receptors: influence of age and gender in healthy subjects.

5-HT2A receptors have been implicated in the pathophysiology of mood disorders and in the therapeutic effect of the so-called atypical antipsychotics. Recently, a new radioiodinated ligand with high affinity and selectivity for serotonin 5-HT2A receptors, 123iodinated 4-amino-N-1-[3-(4-fluorophenoxy)propyl]-4-methyl-4-piperidinyl] 5-iodo-2-methoxybenzamide (123I-5-I-R91150), has been developed and has been shown to be suitable for single-photon emission tomography (SPET) imaging. In this study the influence of age and gender on the ligand binding was investigated in normal volunteers.

Preclinical evaluation of [123I]R93274 as a SPECT radiotracer for imaging 5-HT2A receptors.

Studies in rodents have suggested that the radioiodinated 5-HT2A receptor antagonist [123I]R93274 (123-iodine-N-[(3-p-fluorophenyl-1-propyl)-4-methyl-4-piperidinyl]-4-ami no- 5-iodo-2-methoxybenzamide) (Kd = 0.1 nM) might be a promising single photon emission computerized tomography (SPECT) radiotracer to image 5-HT2A receptors in the living human brain. In this study, we characterized the brain uptake of [123I]R93274 in baboons.