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The synthesis of carbon‐14 labeled ( R )‐4‐(dipropylamino)‐1,3,4,5‐tetrahydrobenz[cd]indole‐6‐carboxamide hippurate. A partial ergoline with 5‐HT 1A agonist activity and an 125 I‐labeled analog
Author(s) -
Wheeler William J.,
Swanson Steven P.,
Varie David L.,
O'Ban Douglas D.
Publication year - 2005
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.907
Subject(s) - chemistry , carboxamide , indole test , agonist , stereochemistry , partial agonist , chemical synthesis , in vitro , pharmacology , receptor , biochemistry , medicine
Partial ergoline agonists such as ( R )‐4‐(dipropylamino)‐1,3,4,5‐tetrahydrobenz[cd]‐indole‐6‐carboxamide ( LY228729, 1a ) mimic a locked conformational analog of serotonin and in fact possess potent in vitro activity as agonists of the 5‐HT 1A receptor. In the course of pre‐clinical investigation of 1a for potential use as an anxiolytic agent, 1b was prepared in a five step synthesis from K 14 CN. In addition, an 125 I‐analog of 1a was prepared for aid in the development of a radioimmunoassay (RIA). Copyright © 2005 John Wiley & Sons, Ltd.