title: Aplysamine-1 and related analogs as histamine H3 receptor antagonists.
abstract: Aplysamine-1 (1), a marine natural product, was synthesized and screened for in vitro activity at the human and rat histamine H3 receptors. Aplysamine-1 (1) was found to possess a high binding affinity for the human H3 receptor (Ki = 30+/-4 nM). Synthetic analogs of 1, including des-bromoaplysamine-1 (10) and dimethyl-{2-[4-(3-piperidin-1-yl-propoxy)-phenyl]-ethyl}-amine (13), were potent H3 antagonists.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. dswanso1@prdus.jnj.com
authors.forename: Devin M
authors.initials: DM
authors.lastname: Swanson
authors.forename: Sandy J
authors.initials: SJ
authors.lastname: Wilson
authors.forename: Jamin D
authors.initials: JD
authors.lastname: Boggs
authors.forename: Wei
authors.initials: W
authors.lastname: Xiao
authors.forename: Richard
authors.initials: R
authors.lastname: Apodaca
authors.forename: Ann J
authors.initials: AJ
authors.lastname: Barbier
authors.forename: Timothy W
authors.initials: TW
authors.lastname: Lovenberg
authors.forename: Nicholas I
authors.initials: NI
authors.lastname: Carruthers
mesh_terms: D000818:Animals; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D051381:Rats; D018100:Receptors, Histamine H3 / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014443:Tyrosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D008024:Ligands; D018100:Receptors, Histamine H3; C509742:aplysamine-1; D014443:Tyrosine