title: Novel human histamine H(3) receptor antagonists.
abstract: High throughput screening, using the recombinant human H(3) receptor, was used to identify novel histamine H(3) receptor antagonists. Evaluation of the lead compounds ultimately afforded potent, selective, orally bioavailable compounds (e.g., 38) with favorable blood-brain barrier penetration.
authors.affiliation: Johnson and Johnson Pharmaceutical Research and Development, L.L.C., San Diego, CA 92121, USA.
authors.forename: Chandra
authors.initials: C
authors.lastname: Shah
authors.forename: Laura
authors.initials: L
authors.lastname: McAtee
authors.forename: J Guy
authors.initials: JG
authors.lastname: Breitenbucher
authors.forename: Dale
authors.initials: D
authors.lastname: Rudolph
authors.forename: Xiaobing
authors.initials: X
authors.lastname: Li
authors.forename: Timothy W
authors.initials: TW
authors.lastname: Lovenberg
authors.forename: Curt
authors.initials: C
authors.lastname: Mazur
authors.forename: Sandy J
authors.initials: SJ
authors.lastname: Wilson
authors.forename: Nicholas I
authors.initials: NI
authors.lastname: Carruthers
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D001812:Blood-Brain Barrier; D001923:Brain Chemistry; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000493:pharmacokinetics* / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D011725:Pyridines / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D018100:Receptors, Histamine H3 / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D006633:Histamine Antagonists; D008024:Ligands; D011725:Pyridines; D018100:Receptors, Histamine H3