Imaging Sigma-1 Receptor (S1R) Expression Using Iodine-124-Labeled 1-(4-Iodophenyl)-3-(2-adamantyl)guanidine ([¹²⁴I]IPAG).

ABSTRACT:

Purpose

Sigma-1 receptors (S1Rs) are overexpressed in almost all human cancers, especially in breast cancers. 1-(4-Iodophenyl)-3-(2-adamantyl)guanidine (IPAG) is a validated high-affinity S1R antagonist. The objective of the current study is to evaluate the potential of iodine-124-labeled IPAG ([¹²⁴I]IPAG) to image S1R-overexpressing tumors.

Procedures

[¹²⁴I]IPAG was synthesized from a tributyltin precursor dissolved in ethanol using chloramine-T as oxidant. Purity was analyzed using HPLC. In vitro and in vivo studies were performed using the breast cancer cell line MCF-7. Competitive inhibition studies were performed using haloperidol and cold IPAG. Tumors were established in athymic nude mice by injecting 10⁷ cells subcutaneously. Mice were

SUBMITTER: Gangangari KK 

PROVIDER: S-EPMC6893110 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature