title: 2-Aryl indole NK1 receptor antagonists: optimisation of indole substitution.
abstract: The synthesis and biological evaluation of a series of 2-aryl indoles with high affinity for the human neurokinin-1 (hNK1) receptor are reported, concentrating on optimisation of the indole substitution.
authors.affiliation: Department of Medicinal Chemistry, The Neuroscience Research Centre, Harlow, Essex, UK. laura_cooper@merck.com
authors.forename: L C
authors.initials: LC
authors.lastname: Cooper
authors.forename: G G
authors.initials: GG
authors.lastname: Chicchi
authors.forename: K
authors.initials: K
authors.lastname: Dinnell
authors.forename: J M
authors.initials: JM
authors.lastname: Elliott
authors.forename: G J
authors.initials: GJ
authors.lastname: Hollingworth
authors.forename: M M
authors.initials: MM
authors.lastname: Kurtz
authors.forename: K L
authors.initials: KL
authors.lastname: Locker
authors.forename: D
authors.initials: D
authors.lastname: Morrison
authors.forename: D E
authors.initials: DE
authors.lastname: Shaw
authors.forename: K L
authors.initials: KL
authors.lastname: Tsao
authors.forename: A P
authors.initials: AP
authors.lastname: Watt
authors.forename: A R
authors.initials: AR
authors.lastname: Williams
authors.forename: C J
authors.initials: CJ
authors.lastname: Swain
mesh_terms: D000818:Animals; D001522:Behavior, Animal; D001667:Binding, Competitive / Q000187:drug effects; D001923:Brain Chemistry; D016466:CHO Cells; D006224:Cricetinae; D005849:Gerbillinae; D007202:Indicators and Reagents; D007211:Indoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D064729:Neurokinin-1 Receptor Antagonists; D051381:Rats; D013329:Structure-Activity Relationship; D013373:Substance P / Q000378:metabolism
chemical_list: D007202:Indicators and Reagents; D007211:Indoles; D064729:Neurokinin-1 Receptor Antagonists; D013373:Substance P