title: Identification of a novel, orally bioavailable histamine H(3) receptor antagonist based on the 4-benzyl-(1H-imidazol-4-yl) template.
abstract: A novel series of histamine H(3) receptor antagonists, based on the 4-benzyl-(1H-imidazole-4-yl) template, incorporating urea and carbamate linkers has been prepared. Compound 3j is a selective H(3) antagonist and demonstrates excellent oral plasma levels in the rat and monkey.
authors.affiliation: The Schering Plough Research Institute, Kenilworth, NJ 07033, USA. aslanian@spcorp.com
authors.forename: Robert
authors.initials: R
authors.lastname: Aslanian
authors.forename: Mwangi W
authors.initials: MW
authors.lastname: Mutahi
authors.forename: Neng Yang
authors.initials: NY
authors.lastname: Shih
authors.forename: Kevin D
authors.initials: KD
authors.lastname: McCormick
authors.forename: John J
authors.initials: JJ
authors.lastname: Piwinski
authors.forename: Pauline C
authors.initials: PC
authors.lastname: Ting
authors.forename: Margaret M
authors.initials: MM
authors.lastname: Albanese
authors.forename: Michael Y
authors.initials: MY
authors.lastname: Berlin
authors.forename: Xiaohong
authors.initials: X
authors.lastname: Zhu
authors.forename: Shing Chun
authors.initials: SC
authors.lastname: Wong
authors.forename: Stuart B
authors.initials: SB
authors.lastname: Rosenblum
authors.forename: Yueheng
authors.initials: Y
authors.lastname: Jiang
authors.forename: Robert
authors.initials: R
authors.lastname: West
authors.forename: Susan
authors.initials: S
authors.lastname: She
authors.forename: Shirley M
authors.initials: SM
authors.lastname: Williams
authors.forename: Matthew
authors.initials: M
authors.lastname: Bryant
authors.forename: John A
authors.initials: JA
authors.lastname: Hey
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D000882:Haplorhini; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D007093:Imidazoles / Q000138:chemical synthesis / Q000493:pharmacokinetics* / Q000494:pharmacology; D011485:Protein Binding; D051381:Rats; D018100:Receptors, Histamine H3 / Q000187:drug effects / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D006633:Histamine Antagonists; D007093:Imidazoles; D018100:Receptors, Histamine H3