Abstract
The octapeptide D-Ala-Ser-Thr-Thr-Thr-Asn-Tyr-Thr-NH 2 ([D-Ala 1]TNH 2), an analog of peptide T (H-Ala-Ser-Thr-Thr-Thr-Asn-Tyr-Thr-OH) associated with CD 4/T 4 receptors involved in human immunodeficiency virus infection, was combined with the chelating polyazamacrocycle 1,4,8,11-tetraazacyclotetradecane (cyclam) to afford the bifunctional ligand cyc-[D-Ala 1]TNH 2. This was then reacted with [ 99mTcO 4] − and Sn 2+ to yield the monocationic complex [ 99mTc(O) 2(cyc-[D-Ala 1]TNH 2)] +. Biological activity of both the cyclam-peptide conjugate and the resulting Tc-99m complex were evaluated by measuring their chemotactic indexes. Results showed that N-cyclam acylation and subsequent labeling with Tc-99m of [D-Ala 1]TNH 2 were tolerated, and both cyc-[D-Ala 1]TNH 2 and [ 99mTc(O) 2(cyc-[D-Ala 1]TNH 2)] + retained the high chemotactic capacity of the original octapeptide. Biodistribution of the Tc-99m complex was carried out in rats. Fast blood clearance and no accumulation in organs of interest were observed.
Published Version
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call