Antagonism pharmacological

Gaddum, J. H. (1957). Theories of drug antagonism. Pharmacological Reviews, 9, 211-268. 

Research for an antidepressant among non-tricyclic compounds with pharmacological effects qualitatively different from those of the conventional tricyclic compounds led to the preparation and testing of a series of indazole derivatives for reserpine-like activity in mice. l-[3-(Dimethylamino)propyl]-5-methyl-3-phenyl-l//-indazole (FS-32 692) antagonizes reserpine-induced effects and potentiates amphetamine-induced self-stimulation and l-Dopa-induced increase in motor activity. FS-32 produces an anticholinergic action mainly on the central nervous System, while the action of imipramine occurs centrally as well as peripherally (79AF511). 

Schild analysis, like all pharmacological tools, necessarily is predicated on the idea that the drugs involved have one and only one pharmacological activity. This often may not be the case and selectivity is only a function of concentration. If the concentrations used in the assay are below those that have secondary effects, then the tool will furnish the parameter of interest with no obfuscation. However, if a secondary effects are operative in the concentration range required to measure antagonism then the resulting parameter may be tainted by this secondary activity. 

Kenakin, T. P., and Boselli, C. (1989). Pharmacologic discrimination between receptor heterogeneity and allosteric interaction Resultant analysis of gallamine and pirenzeipine antagonism of muscarinic responses in rat trachea. J. Pharmacol. Exp. Ther. 250 944—952. 

Ideally, pharmacological data should directly be fit to specific models and parameters derived from the direct fit. However, there are cases where the specific models predict surrogate parameters that can be derived without fitting data to the specific model. This can be an advantage. For example, the equation for simple competitive antagonism of receptors (see Section 6.3) is... 

At the present time, a variety of other pharmaeological agents are being tested for their ability either to antagonize or to potentiate the effect of MDMA in these animals. There is hope that appropriate pharmacological manipulations will eventually be found that will give useful information about the mechanism of action for entactogens. 

Malick, J.B. Pharmacological antagonism of mouse-killing behavior in the olfactory bulb lesion-induced killer rat. Aggressive Behav 2 123-130,... 

Consroe, P. Boren, J.L. and Hsu, C.H. Propranolol antagonizes phencyclidine-induced hyperactivity and stereotypy in rats. Pharmacology 24 96-104, 1982. 

EN formulas contain vitamin K, which can antagonize the pharmacologic activity of warfarin. The vitamin K content of EN formulas generally has been adjusted down over the past... 

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