General construction pattern of histamine H3-receptor antagonists: change of a paradigm.
Novel omega-phenyl substituted and unsubstituted alkyl and alkenyl imidazole derivatives were prepared and tested for their antagonist activity in vitro and in vivo at histamine H3-receptors. Some compounds showed high in vitro and in vivo H3-receptor activity despite their structure bearing no polar moiety in the centre of the molecule which is a common structural feature of all other antagonists known. Quite probably there are further in vivo effects for some compounds resulting from other receptor interactions.
Stark
H
H
Institut für Pharmazie I, Freie Universität Berlin, Germany. stark@schunet.pharmazie.fu-berlin.de
Ligneau
X
X
Arrang
J M
JM
Schwartz
J C
JC
Schunack
W
W
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D006168:Guinea Pigs; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006636:Histamine Release / Q000187:drug effects; D007082:Ileum / Q000187:drug effects / Q000502:physiology; D066298:In Vitro Techniques; D051379:Mice; D051381:Rats; D018100:Receptors, Histamine H3 / Q000187:drug effects*; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism
D006633:Histamine Antagonists; D018100:Receptors, Histamine H3