D. Mckenna, C. Mathis, A. Shulgin
Jun 4, 1987
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Journal
European journal of pharmacology
Abstract
The selective, high-affinity binding of various psychotomimetic phenylisopropylamine derivatives to 5HT 2 receptors has been previously reported. Optimal stereospecific selectivity was detected for 4-bromoor 4-iodo-R-(-)-2,5-dimethoxy phenylisopropylamines. Both of these derivatives are potent hallucinogenic agents in man (Glennon et al., 1986). Using membrane binding techniques, these workers have characterized the 5HT 2 agonist properties of [3H](+)-DOB, which selectively labels a guanylate-sensitive high-affinity state of the receptor (Titeler et al., 1985). The low specific activity of [3H]DOB renders it impractical for use in autoradiographic receptor localization. The iodine-containing analog DOI (4iodo-2,5-dimethoxyphenylisopropylamine), however, possesses a stereospecific 5HT 2 selectivity comparable to DOB (Glennon et al., 1986), suggesting that 125I-labelled DOI could be used for autoradiographic localization of 5HT 2 receptors. Although 1311or 123I-labelled analogs of DOI have been used in vivo for brain imaging and metabolic studies (Sargent et al., 1984), the utifization of 125I-DOI for in vitro autoradiography has not been previously reported. We have initiated investigations of 125I-DOI as a ligand for autoradiography and report here our preliminary results. The R ( ) enantiomer of t25I-DOI was synthesized to a radiochemical purity of 99 + %. The