Amidines and related compounds. 6. Structure-activity relations of antihypertensive and antisecretory agents related to clonidine

1975 ◽  
Vol 18 (1) ◽  
pp. 90-99 ◽  
Author(s):  
Timothy Jen ◽  
Helene Van Hoeven ◽  
William Groves ◽  
Richard A. McLean ◽  
Bernard Loev
1985 ◽  
Vol 4 (3) ◽  
pp. 273-278 ◽  
Author(s):  
L.A. King

1 The median fatal concentrations (EC50) of various types of drugs are shown to be determined solely by their aqueous solubilities (S). Among the test substances, EC50 values show a range of 2000-fold, whereas the ratio EC 50/S is essentially constant. This behaviour is typical of 'Ferguson substances', and enables the fatal toxicity of other (depressant) drugs and related compounds to be calculated. 2 The mean relative saturation (EC50/S) is 0.006, a value which shows that humans are more sensitive to narcotic agents than are the lower animals. 3 The Ferguson principle provides a broad framework for quantitative structure-activity relations in fatal drug toxicity. The empirical Hansch equation can be derived from the same thermodynamic concept of free energy which underlies the Ferguson principle.


1972 ◽  
Vol 15 (6) ◽  
pp. 583-589 ◽  
Author(s):  
H. Cairns ◽  
C. Fitzmaurice ◽  
D. Hunter ◽  
P. B. Johnson ◽  
J. King ◽  
...  

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