Correlation of histamine H1 receptor function and [3H]mepyramine binding in porcine tracheal tissue.
In order to validate the use of [3H]mepyramine as a radioligand to label airway histamine H1 receptors, the results of radioligand binding experiments using porcine tracheal tissue membranes were compared with the results of physiologic studies measuring histamine-induced trachealis muscle contraction. Close agreement was found between histamine-induced [3H]mepyramine binding inhibition and histamine concentration-contraction-response curves. Close agreement was also found between the KD of mepyramine-induced [3H]mepyramine binding inhibition and the K beta of mepyramine antagonism of muscle contractions stimulated by 10(-4) M histamine. [3H]Mepyramine binding was found to be rapid, reversible, saturable and stereospecific. Only H1 agonists and antagonists displayed potent [3H]mepyramine binding inhibition in competition binding studies. The results fulfill criteria for histamine H1 receptor identification by radioligand binding with [3H]mepyramine.
Driver
A G
AG
Department of Medicine, East Carolina University, School of Medicine, Greenville, NC 27858.
Mustafa
S J
SJ
D000631:Aminopyridines / Q000378:metabolism*; D000818:Animals; D066298:In Vitro Techniques; D008954:Models, Biological; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects / Q000378:metabolism*; D011738:Pyrilamine / Q000378:metabolism*; D011968:Receptors, Histamine / Q000187:drug effects*; D011969:Receptors, Histamine H1 / Q000187:drug effects*; D013552:Swine; D013997:Time Factors; D014132:Trachea / Q000033:anatomy & histology / Q000187:drug effects / Q000378:metabolism
D000631:Aminopyridines; D011968:Receptors, Histamine; D011969:Receptors, Histamine H1; D011738:Pyrilamine