title: 2-(3,5-Dimethylphenyl)tryptamine derivatives that bind to the GnRH receptor.
abstract: 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.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. peter_lin@merck.com
authors.forename: P
authors.initials: P
authors.lastname: Lin
authors.forename: D
authors.initials: D
authors.lastname: Marino
authors.forename: J L
authors.initials: JL
authors.lastname: Lo
authors.forename: Y T
authors.initials: YT
authors.lastname: Yang
authors.forename: K
authors.initials: K
authors.lastname: Cheng
authors.forename: R G
authors.initials: RG
authors.lastname: Smith
authors.forename: M H
authors.initials: MH
authors.lastname: Fisher
authors.forename: M J
authors.initials: MJ
authors.lastname: Wyvratt
authors.forename: M T
authors.initials: MT
authors.lastname: Goulet
mesh_terms: 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*
chemical_list: C434843:2-(3,5-dimethylphenyl)tryptamine; D006727:Hormone Antagonists; D011966:Receptors, LHRH; D014363:Tryptamines; C030820:tryptamine