title: Structure-activity relationships of histamine H2 receptor ligands.
abstract: 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.
authors.affiliation: Institute of Pharmacy, University of Regensburg, D--93040 Regensburg, Germany.
authors.forename: Stefan
authors.initials: S
authors.lastname: Dove
authors.forename: Sigurd
authors.initials: S
authors.lastname: Elz
authors.forename: Roland
authors.initials: R
authors.lastname: Seifert
authors.forename: Armin
authors.initials: A
authors.lastname: Buschauer
mesh_terms: 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
chemical_list: D017442:Histamine Agonists; D006635:Histamine H2 Antagonists; D008024:Ligands; D011970:Receptors, Histamine H2; D019791:Guanidine