[125I]-2-(2,5-dimethoxy-4-iodophenyl)aminoethane ([125I]-2C-I) as a label for the 5-HT2 receptor in rat frontal cortex.
Pharmacology, biochemistry, and behavior January 1, 1990 M P Johnson, C A Mathis, A T Shulgin et al. 56 citations
A radiolabeled compound, [125I]-2C-I, was used to label low-density 5-HT2 agonist binding sites in brain tissue. The nonhydrolyzable GTP analog GppNHp inhibited high-affinity binding, and serotonin along with several 5-HT2 agonists and antagonists showed high affinity for the site. At 37°C, the number of binding sites (Bmax) decreased compared to 24°C, while binding affinity (KD) remained unchanged. Structure-activity relationships for displacing [125I]-2C-I supported the receptor's role in hallucinogen action. The findings demonstrate [125I]-2C-I as a useful radioligand and provide further evidence linking the 5-HT2 receptor to hallucinogenic activity.