2-(3,5-Dimethylphenyl)tryptamine derivatives that bind to the GnRH receptor.
A series of 2-(3,5-dimethylphenyl)tryptamine derivatives was prepared and evaluated on a rat gonadotropin releasing hormone receptor assay. Some para-substituents on the 4-phenylbutyl side chain attached to the tryptamine nitrogen led to compounds with potent GnRH receptor binding. The study has helped define structural requirements for GnRH receptor binding for the 2-aryltryptamine GnRH antagonists.
Lin
P
P
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. peter_lin@merck.com
Marino
D
D
Lo
J L
JL
Yang
Y T
YT
Cheng
K
K
Smith
R G
RG
Fisher
M H
MH
Wyvratt
M J
MJ
Goulet
M T
MT
D000818:Animals; D001665:Binding Sites / Q000502:physiology; D015195:Drug Design; D005260:Female; D006727:Hormone Antagonists / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D051381:Rats; D011966:Receptors, LHRH / Q000378:metabolism*; D014363:Tryptamines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*
C434843:2-(3,5-dimethylphenyl)tryptamine; D006727:Hormone Antagonists; D011966:Receptors, LHRH; D014363:Tryptamines; C030820:tryptamine