Kinetic analysis of the interaction of mifentidine with gastric H2-receptors in the conscious dog.
The H2-receptor antagonists mifentidine and cimetidine were compared for their ability to antagonize the activation of H2-receptors in the conscious dog. Dose-response curves to dimaprit in stimulating gastric secretion were displaced to the right in a dose-related fashion by both drugs. Schild and Eadie-Hofstee analysis of these data indicated that mifentidine and cimetidine inhibited in vivo activation of H2-receptors in a manner compatible with competitive surmountable antagonism. Mifentidine displayed a 24fold greater potency than cimetidine as H2 antagonist in the conscious dog.
D000818:Animals; D002927:Cimetidine / Q000494:pharmacology*; D017259:Dimaprit; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D005260:Female; D005744:Gastric Acid / Q000378:metabolism; D005753:Gastric Mucosa / Q000187:drug effects* / Q000378:metabolism; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D007093:Imidazoles / Q000494:pharmacology*; D011897:Random Allocation; D011970:Receptors, Histamine H2 / Q000187:drug effects*; D013890:Thiourea / Q000037:antagonists & inhibitors
D006635:Histamine H2 Antagonists; D007093:Imidazoles; D011970:Receptors, Histamine H2; C039796:mifentidine; D002927:Cimetidine; D013890:Thiourea; D017259:Dimaprit