title: [Pharmacological actions of alkylaminoalkyl-phenylbenzisothazole compounds on the gastrointestinal tract].
abstract: In the present paper pharmacological properties studied on the gastrointestinal tract of two new alkylaminoalkylphenylbenzisothiazole derivatives, 4-dimethylamino-2-phenyl-2-(1,2-benzisothiazole-3-yl)butyramide (PM2) and N,N-dimethyl-3-phenyl-3-(1,2-benzisothiazole-3-yl)propylamine (PM3) have been reported. Both drugs showed antispasmodic effects on gastroduodenal junction of the anaesthetized rat stimulated by Caerulein, according to previous results obtained on guinea-pig isolated ileum. On this substrate they were different in the potency being PM3 more active than PM2. On the contrary, the hypersecretion induced by Histamine or Gastrin-17 in rat perfused stomach was potentiated by PM2 and inhibited by PM3. Similar effects were observed on guinea-pig "in vitro" stomach preparation where PM2 and Papaverine were ineffective in modifying Histamine dose-response curves and PM3 reduced significantly maximal peak effects of Histamine, behaving as a non-competitive antagonist. The significant differences observed on gastric secretion but not on other substrates, from compounds structural analysis, appear scarcely justified and seem to us important to be further investigated.
mesh_terms: D000818:Animals; D002108:Ceruletide / Q000494:pharmacology; D004064:Digestive System / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D005753:Gastric Mucosa / Q000378:metabolism; D005755:Gastrins / Q000494:pharmacology; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D010208:Papaverine / Q000494:pharmacology; D051381:Rats; D013844:Thiazoles / Q000494:pharmacology*
chemical_list: D005755:Gastrins; D013844:Thiazoles; C013550:gastrin 17; D006632:Histamine; C042000:N,N-dimethylamino-3-phenyl-3-(1,2-benzisothiazol-3-yl)propylamine; C041799:4-dimethylamino-2-phenyl-2-(1,2-benzisothiazol-3-yl)butyramide; D002108:Ceruletide; D010208:Papaverine
vernacular_title: Azioni farmacologiche di composti alchilaminoalchilfenilbenzisotiazolici sul tratto gastrointestinale.