The use of an in vitro binding assay to predict histamine H2-antagonist activity.
Thirty-seven compounds were evaluated for their ability to inhibit histamine stimulated adenylate cyclase and to inhibit 3H-tiotidine binding. The compounds examined included a number of known H2-antagonists and a number of potential H2-antagonists of diverse chemical structure. The correlation between the Ki values from the binding assay and from the inhibition of adenylate cyclase was calculated to be r = 0.99, p less than 0.001. Thus 3H-tiotidine binding in guinea-pig cerebral cortex can be used to give a valid assessment of histamine H2-receptor activity.
Norris
D B
DB
Gajtkowski
G A
GA
Wood
T P
TP
Rising
T J
TJ
D000067956:Adenylyl Cyclase Inhibitors; D000818:Animals; D002927:Cimetidine / Q000031:analogs & derivatives / Q000378:metabolism; D005260:Female; D006168:Guinea Pigs; D006635:Histamine H2 Antagonists / Q000494:pharmacology*; D066298:In Vitro Techniques; D008297:Male; D011970:Receptors, Histamine H2 / Q000378:metabolism; D014316:Tritium
D000067956:Adenylyl Cyclase Inhibitors; D006635:Histamine H2 Antagonists; D011970:Receptors, Histamine H2; D014316:Tritium; D002927:Cimetidine; C023990:tiotidine