title: 1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists.
abstract: With the aim of identifying structurally novel, centrally acting histamine H(3) antagonists, arrays of monoacyldiamines were screened. This led to the discovery of a series of 1-alkyl-4-acylpiperazines which were potent antagonists at the human histamine H(3) receptor. The most potent amides had antagonist potencies in the subnanomolar range.
authors.affiliation: Novo Nordisk A/S, Novo Nordisk Park, DK-2760 Malov, Denmark. flo@novonordisk.com
authors.forename: Florencio
authors.initials: F
authors.lastname: Zaragoza
authors.forename: Henrik
authors.initials: H
authors.lastname: Stephensen
authors.forename: Sanne M
authors.initials: SM
authors.lastname: Knudsen
authors.forename: Lone
authors.initials: L
authors.lastname: Pridal
authors.forename: Birgitte S
authors.initials: BS
authors.lastname: Wulff
authors.forename: Karin
authors.initials: K
authors.lastname: Rimvall
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011869:Radioligand Assay; D018100:Receptors, Histamine H3 / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D006633:Histamine Antagonists; D010879:Piperazines; D018100:Receptors, Histamine H3