title: The first potent and selective non-imidazole human histamine H4 receptor antagonists.
abstract: Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, 3210 Merryfield Row, San Diego, California 92121, USA.
authors.forename: Jill A
authors.initials: JA
authors.lastname: Jablonowski
authors.forename: Cheryl A
authors.initials: CA
authors.lastname: Grice
authors.forename: Wenying
authors.initials: W
authors.lastname: Chai
authors.forename: Curt A
authors.initials: CA
authors.lastname: Dvorak
authors.forename: Jennifer D
authors.initials: JD
authors.lastname: Venable
authors.forename: Annette K
authors.initials: AK
authors.lastname: Kwok
authors.forename: Kiev S
authors.initials: KS
authors.lastname: Ly
authors.forename: Jianmei
authors.initials: J
authors.lastname: Wei
authors.forename: Sherry M
authors.initials: SM
authors.lastname: Baker
authors.forename: Pragnya J
authors.initials: PJ
authors.lastname: Desai
authors.forename: Wen
authors.initials: W
authors.lastname: Jiang
authors.forename: Sandy J
authors.initials: SJ
authors.lastname: Wilson
authors.forename: Robin L
authors.initials: RL
authors.lastname: Thurmond
authors.forename: Lars
authors.initials: L
authors.lastname: Karlsson
authors.forename: James P
authors.initials: JP
authors.lastname: Edwards
authors.forename: Timothy W
authors.initials: TW
authors.lastname: Lovenberg
authors.forename: Nicholas I
authors.initials: NI
authors.lastname: Carruthers
mesh_terms: D000818:Animals; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D006633:Histamine Antagonists / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D006801:Humans; D007211:Indoles / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D007700:Kinetics; D008024:Ligands; D009474:Neurons / Q000166:cytology; D010879:Piperazines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D011869:Radioligand Assay; D051381:Rats; D011956:Receptors, Cell Surface / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled; D011968:Receptors, Histamine; D000074040:Receptors, Histamine H4; D011994:Recombinant Proteins / Q000187:drug effects / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship; D014162:Transfection
chemical_list: C418607:HRH4 protein, human; D006633:Histamine Antagonists; C498828:Hrh4 protein, rat; D007211:Indoles; D008024:Ligands; D010879:Piperazines; D011956:Receptors, Cell Surface; D043562:Receptors, G-Protein-Coupled; D011968:Receptors, Histamine; D000074040:Receptors, Histamine H4; D011994:Recombinant Proteins