Premium
Influence of sympathomimetic drugs (1‐phenyl‐2‐amino‐ethan‐1‐ol derivatives) on the biosynthesis of prostaglandins and thromboxane B 2
Author(s) -
Förster W.,
Pönicke K.
Publication year - 1983
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1983.tb09390.x
Subject(s) - chemistry , thromboxane , biosynthesis , propranolol , prostaglandin , prostacyclin , medicine , orciprenaline , endocrinology , phenoxybenzamine , biochemistry , receptor , biology , enzyme , platelet
1 The influence of substituted 1‐phenyl‐2‐amino‐ethan‐1‐ols on prostaglandin and thromboxane biosynthesis was studied using ram seminal vesicle microsomes and homogenates of rat lung and of rat stomach fundus. 2 Clear structure‐activity relationships were to be seen regarding the effects of sympathomimetic drugs on prostacyclin (PGI 2 ) biosynthesis in the rat stomach fundus homogenates. 3′‐ and 4′‐Monohydroxy‐phenyl derivatives as well as 3′,4′‐dihydroxy‐phenyl derivatives stimulated prostaglandin and thromboxane B 2 (TXB 2 ) biosynthesis. Contrary to this the 3′,5′‐dihydroxy‐phenyl derivatives orciprenaline, terbutaline and fenoterol were inhibitors of the biosynthesis in rat organ homogenates. 3 All the sympathomimetic drugs tested stimulated cyclo‐oxygenase. Orciprenaline suppressed the adrenaline‐activated cyclo‐oxygenase in a dose‐dependent manner. 4 The effects of adrenoceptor antagonists were also studied. Phenoxybenzamine had little effect on cyclo‐oxygenase activity whereas phentolamine markedly increased the rate of oxygen uptake. Both the (+)‐ and (−)‐optical isomers of propranolol had no effect on either basal or adrenaline‐stimulated oxygen uptake. In contrast, the (+)‐ and (−)‐isomers of pindolol inhibited basal and adrenaline‐stimulated uptake.