A Quantitative study of histamine H2-receptor bockade by burimamide in isolated artica.
The onset of burimamide inhibition of histamine stimulation of rabbit atria is rapid, and a near steady-state blockade occurs at approximately 15 min ( larger than or equal to 90% complete). The blockade is reversible but requires several washings suggesting the disassociation is slow. The administration of histamine may accelerate the decay of the burimamide effect. Reciprocal plots (rate response versus histamine concentration) of dose-response curves are linear for both rabbit and guinea pig atria. In the presence of low concentrations of burimamide; (2.4  times 10-5 M), the displacement of curves suggests a competitive type of inhibition both for rabbit and guinea guinea pig atria. The apparent association constants calculated from these curves are: K1 (rabbit) 3.7 times 10-6M and K-1 (guinea pig) 6.7 times 10-6M. These results for guinea pig atria are in satisfactory agreement with the value obtained in another laboratory (2). At higher concentrations of burimamide, inhibition curves showed distinct evidence of departure from competitive character for both guinea pig and rabbit atria.
D000818:Animals; D001665:Binding Sites; D001667:Binding, Competitive; D004305:Dose-Response Relationship, Drug; D005260:Female; D006168:Guinea Pigs; D006325:Heart Atria / Q000378:metabolism; D006339:Heart Rate / Q000187:drug effects*; D006634:Histamine H1 Antagonists; D007093:Imidazoles / Q000037:antagonists & inhibitors; D066298:In Vitro Techniques; D008297:Male; D011817:Rabbits; D013890:Thiourea / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors; D013997:Time Factors
D006634:Histamine H1 Antagonists; D007093:Imidazoles; D013890:Thiourea