title: Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists.
abstract: Novel derivatives of the highly potent and selective histamine H3-receptor antagonist ciproxifan (3) with different chain lengths as well as with structural variants of the cyclopropyl ketone moiety have been prepared and screened for their antagonist H3-receptor potencies in vitro and in vivo. Some derivatives (2, 6-8, 12) containing other functionalities were effective in vitro in the same (sub)nanomolar concentration range and in vivo in a remarkably low oral dose.
authors.affiliation: Institut für Pharmazie, Freie Universität Berlin, Germany. stark@schunet.pharmazie.fu-berlin.de
authors.forename: H
authors.initials: H
authors.lastname: Stark
authors.forename: X
authors.initials: X
authors.lastname: Ligneau
authors.forename: B
authors.initials: B
authors.lastname: Sadek
authors.forename: C R
authors.initials: CR
authors.lastname: Ganellin
authors.forename: J M
authors.initials: JM
authors.lastname: Arrang
authors.forename: J C
authors.initials: JC
authors.lastname: Schwartz
authors.forename: W
authors.initials: W
authors.lastname: Schunack
mesh_terms: D000818:Animals; D002540:Cerebral Cortex / Q000502:physiology; D015195:Drug Design; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006636:Histamine Release / Q000187:drug effects*; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D015394:Molecular Structure; D051381:Rats; D018100:Receptors, Histamine H3 / Q000187:drug effects* / Q000502:physiology; D013329:Structure-Activity Relationship; D013574:Synaptosomes / Q000187:drug effects / Q000502:physiology
chemical_list: D006633:Histamine Antagonists; D007093:Imidazoles; D018100:Receptors, Histamine H3; C115705:ciproxifan