title: Oxatomide: in vivo assessment of antagonistic activity, and effects on histamine release and enzymatic histamine degradation in skin.
abstract: The antagonistic activity of oxatomide, and its effects on evoked histamine release and histamine-N-methyl transferase activity in skin, have been studied. Oxatomide antagonizes H1 activity in a dose-dependent but non-competitive manner. It also shows some atropine-like activity. Oxatomide did not cause detectable inhibition of antigen-stimulated histamine release from skin slices of sensitized guinea-pigs although the possibility that oxatomide may cause weak inhibition could not be excluded. In the presence of low concentrations of histamine, oxatomide suppressed human skin histamine-N-methyl transferase, but in the presence of higher substrate concentrations it enhanced activity of this enzyme. These observations, which were limited by the poor solubility of oxatomide in aqueous media, should encourage further in vivo studies of oxatomide's histamine-suppressing properties in the human subjects.
mesh_terms: D000109:Acetylcholine / Q000037:antagonists & inhibitors; D000818:Animals; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists; D006637:Histamine N-Methyltransferase / Q000378:metabolism*; D006636:Histamine Release / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D008780:Methyltransferases / Q000378:metabolism*; D009119:Muscle Contraction / Q000187:drug effects; D010879:Piperazines / Q000494:pharmacology*; D012867:Skin / Q000187:drug effects* / Q000201:enzymology
chemical_list: D006634:Histamine H1 Antagonists; D010879:Piperazines; D008780:Methyltransferases; D006637:Histamine N-Methyltransferase; C015408:oxatomide; D000109:Acetylcholine