A series of 2-(3.5-dimethylphenyl)tryptamine derivatives was prepared and e
valuated on a rat gonadotropin releasing hormone receptor assay. Some para-
substituents on the 4-phenylbutyl side chain attached to the tryptamine nit
rogen led to com pounds with potent GnRH receptor binding. The study has he
lped define structural requirements for GnRH receptor binding for the 2-ary
ltryptamine GnRH antagonists. (C) 2001 Elsevier Science Ltd. All rights res
erved.