Structure-activity relationships of histamine H2 receptor ligands.
Recent research on histamine H2 receptor agonists was focused on quantitative structure-activity relationships and receptor models explaining the activity of imidazolylpropylguanidines. Their selectivity for guinea pig vs. human isoforms was investigated using H2 receptor-Gsalpha fusion proteins and attributed to amino acid differences in transmembrane domains 1 and 7. New antagonists result from approaches to improve pharmacokinetic properties and to design hybrid drugs which additionally have gastroprotective or anti H. pylori activity.
Dove
Stefan
S
Institute of Pharmacy, University of Regensburg, D--93040 Regensburg, Germany.
Elz
Sigurd
S
Seifert
Roland
R
Buschauer
Armin
A
D000818:Animals; D019791:Guanidine / Q000737:chemistry; D017442:Histamine Agonists / Q000737:chemistry / Q000494:pharmacology; D006635:Histamine H2 Antagonists / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D011970:Receptors, Histamine H2 / Q000378:metabolism*; D013329:Structure-Activity Relationship
D017442:Histamine Agonists; D006635:Histamine H2 Antagonists; D008024:Ligands; D011970:Receptors, Histamine H2; D019791:Guanidine