Structure-activity relationships of histamine H1-receptor agonists.
Significant progress in the development of potent and selective histamine H1-receptor agonists has been achieved since 1990. Optimisation of the class of 2-phenylhistamines has furnished 2-[3-(trifluoromethyl)phenyl]histamine and its Nalpha-methyl derivative. The discovery of histaprodifen (2-[2-(3,3-diphenylpropyl)-1H-imidazol-4-yl]ethanamine) and the novel lead compound suprahistaprodifen (Nalpha-2-[(1H-imidazol-4-yl)ethyl]histaprodifen) represents additional milestones in the H1-receptor agonist field.
Pertz
Heinz H
HH
Freie Universität Berlin, Institut für Pharmazie, Königin-Luise-Str. 2+4, 14195 Berlin, Germany. hpertz@zedat.fu-berlin.de.
Elz
Sigurd
S
Schunack
Walter
W
D000818:Animals; D006632:Histamine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D017442:Histamine Agonists / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D007093:Imidazoles / Q000737:chemistry; D008761:Methylhistamines / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D017442:Histamine Agonists; D007093:Imidazoles; D008761:Methylhistamines; C118994:histaprodifen; C118995:methylhistaprodifen; C029899:imidazole; D006632:Histamine