Open AccessSTUDIES ON THE MODE OF ANTAGONISM BETWEEN ADRENERGIC β-MIMETICS AND β-BLOCKING AGENTS (IV) INFLUENCE OF FUNCTIONAL ANTAGONISM BY SPASMOGENS
Author(s) -
M Ohashi
Publication year - 1976
Publication title -
japanese journal of pharmacology/japanese journal of pharmacology
Language(s) - English
Resource type - Journals
eISSN - 1347-3506
pISSN - 0021-5198
DOI - 10.1254/jjp.26.325
Subject(s) - antagonism , propranolol , chemistry , histamine , agonist , carbachol , pharmacology , medicine , receptor , biology , biochemistry
A new theory is presented to describe the effect of functional antagonism on the competitive antagonism between adrenergic beta-mimetics and beta-blockers. According to this theory the shape of the log (dose ratio-1) vs.--log [B] curve and the apparent pA2 value in competitive antagonism should be affected by functional antagonism when the agonist is taken up by the saturable uptake process, and this was experimentally confirmed. The competitive antagonism between isoproterenol (ISO) and propranolol (Prop) was influenced by the functional antagonism between ISO and spasmogens (histamine and carbachol). The log (dose ratio-1) vs. --log [B] curve is ISO-Prop competitive antagonism was shifted variously depending on the concentration of a spasmogen used. Theoretical predictions and experimental results were in good parallel.