( sup 125 I)-2-(2,5-dimethoxy-4-iodophenyl)aminoethane (( sup 125 I)-2C-I) as a label for the 5-HT2 receptor in rat frontal cortex

Journal Article · Mon Jan 01 00:00:00 EST 1990 · Pharmacology, Biochemistry and Behavior; (USA)

DOI:https://doi.org/10.1016/0091-3057(90)90228-A· OSTI ID:6969685

Johnson, M P; Mathis, C A; Shulgin, A T; Hoffman, A J; Nichols, D E ^[1]

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1. Purdue Univ., West Lafayette, IN (USA)

Recent studies of 5-HT2 receptor binding have involved the use of radiolabeled agonists. This report describes the use of ({sup 125}I)-2-(2,5-dimethoxy-4-iodophenyl)aminoethane (({sup 125}I)-2C-I) as a label for low-density 5-HT2 agonist binding sites. A nonhydrolyzable analog of GTP, GppNHp, was found to inhibit the high affinity binding of ({sup 125}I)-2C-I. 5-HT and several 5-HT2 agonists and antagonists displayed high affinity for this site. In addition, a significant decrease in the Bmax value, but not the KD for ({sup 125}I)-2C-I was observed at 37 degrees C as compared to that observed at 24 degrees C. Several structure-activity relationships were investigated for displacement of ({sup 125}I)-2C-I, and the results are consistent with the importance of this receptor in the mechanism of action of hallucinogens. This study demonstrates the utility of ({sup 125}I)-2C-I as a novel radioligand and provides further data that the 5-HT2 receptor is significantly linked to hallucinogenic activity for several compounds.

• OSTI ID: 6969685
• Journal Information: Pharmacology, Biochemistry and Behavior; (USA), Vol. 35:1; ISSN 0091-3057
• Country of Publication: United States
• Language: English

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