Premium
2‐Amino‐3‐(1‐(4‐(4‐(2‐methoxyphenyl) piperazine‐1‐yl)butyl)‐1 H ‐1,2,3‐triazol‐4‐yl) propanoic acid: synthesized, 99m Tc‐tricarbonyl labeled, and bioevaluated as a potential 5HT 1A receptor ligand
Author(s) -
Hassanzadeh Leila,
Erfani Mostafa,
Sadat Ebrahimi Seyed Esmaeil
Publication year - 2012
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2953
Subject(s) - piperazine , chemistry , biodistribution , lipophilicity , moiety , propanoic acid , ligand (biochemistry) , chelation , in vivo , azide , tropane , click chemistry , stereochemistry , in vitro , combinatorial chemistry , receptor , organic chemistry , biochemistry , microbiology and biotechnology , biology
To develop a novel 5HT 1A receptor imaging agent, a new methoxyphenyl piperazine derivative was synthesized and radiolabeled with 99m Tc‐tricarbonyl precursor. We used the Cu (I)‐catalyzed cycloaddition of azide and terminal alkynes to synthesize 1, 2, 3 triazole as the metal chelating system. This synthesis provided reliable and reproducible method to attach technetium to the methoxyphenyl piperazine moiety. 99m Tc‐tricabonyl labeling of ligand was performed at high radiochemical purity (greater than 95%). The radiolabeled compound was stable at least 24 h in room temperature. In vitro stability study in human serum albumin showed more than 90% stability in 37 °C incubation for 6 h. Biodistribution studies in rat have shown brain hippocampus uptake of 0.31 ± 0.02 %ID/g at 5‐min post‐injection. The favorable in vitro/in vivo stability, lipophilicity, and biodistribution profiles suggest that this radioconjugate is a good candidate for further exploration of its potential clinical application. Copyright © 2012 John Wiley & Sons, Ltd.