title: Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring.
abstract: Three novel series of histamine H(4) receptor (H(4)R) antagonists containing the 2-aminopyrimidine motif are reported. The best of these compounds display good in vitro potency in both functional and binding assays. In addition, representative compounds are able to completely block itch responses when dosed ip in a mouse model of H(4)-agonist induced scratching, thus demonstrating their activities as H(4)R antagonists.
authors.affiliation: Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-6100, USA. john.r.koenig@abbott.com
authors.forename: John R
authors.initials: JR
authors.lastname: Koenig
authors.forename: Huaqing
authors.initials: H
authors.lastname: Liu
authors.forename: Irene
authors.initials: I
authors.lastname: Drizin
authors.forename: David G
authors.initials: DG
authors.lastname: Witte
authors.forename: Tracy L
authors.initials: TL
authors.lastname: Carr
authors.forename: Arlene M
authors.initials: AM
authors.lastname: Manelli
authors.forename: Ivan
authors.initials: I
authors.lastname: Milicic
authors.forename: Marina I
authors.initials: MI
authors.lastname: Strakhova
authors.forename: Thomas R
authors.initials: TR
authors.lastname: Miller
authors.forename: Timothy A
authors.initials: TA
authors.lastname: Esbenshade
authors.forename: Jorge D
authors.initials: JD
authors.lastname: Brioni
authors.forename: Marlon
authors.initials: M
authors.lastname: Cowart
mesh_terms: D000631:Aminopyridines / Q000494:pharmacology*; D000818:Animals; D006633:Histamine Antagonists / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors*; D011968:Receptors, Histamine; D000074040:Receptors, Histamine H4
chemical_list: D000631:Aminopyridines; D006633:Histamine Antagonists; C498829:Hrh4 protein, mouse; D043562:Receptors, G-Protein-Coupled; D011968:Receptors, Histamine; D000074040:Receptors, Histamine H4; C032439:alpha-aminopyridine