title: 2-Aryl tryptamines: selective high-affinity antagonists for the h5-HT2A receptor.
abstract: A series of 2-aryl tryptamines have been identified as high-affinity h5-HT2A antagonists. Structure-activity relationship studies have shown that h5-HT2A affinity can be attained via modifications to the tryptamine side chain and that selectivity over h5-HT2C and hD2 receptors can be controlled by suitable C-2 aryl groups.
authors.affiliation: Merck Sharp & Dohme Research Laboratories, Thle Neuroscience Research Centre, Harlow, Essex, UK. graeme_stevenson@merck.com
authors.forename: G I
authors.initials: GI
authors.lastname: Stevenson
authors.forename: A L
authors.initials: AL
authors.lastname: Smith
authors.forename: S
authors.initials: S
authors.lastname: Lewis
authors.forename: S G
authors.initials: SG
authors.lastname: Michie
authors.forename: J G
authors.initials: JG
authors.lastname: Neduvelil
authors.forename: S
authors.initials: S
authors.lastname: Patel
authors.forename: R
authors.initials: R
authors.lastname: Marwood
authors.forename: S
authors.initials: S
authors.lastname: Patel
authors.forename: J L
authors.initials: JL
authors.lastname: Castro
mesh_terms: D000818:Animals; D001667:Binding, Competitive; D006801:Humans; D051381:Rats; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D011985:Receptors, Serotonin / Q000378:metabolism; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014363:Tryptamines / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D017448:Receptors, Dopamine D2; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D014363:Tryptamines