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Cerletti A, Rothlin E. 
“Role of 5-hydroxytryptamine in Mental Diseases and its Antagonism to Lysergic Acid derivatives”. 
Nature. 1955 October 22;176:785.
The possibility that 5-hydroxytryptamine plays a part in abnormal mental processes has been discussed by Gaddum and by Woolley and Shaw. This hypothesis is based on the findings that this substance is a natural constituent of nervous tissue, particularly of the brain, and that certain of its actions are antagonized by lysergic acid diethylamide, a drug which on oral application and in doses of only 0.5-1.o microgram/kgm. produces pronounced psychic disturbances in normal human beings. According to this hypothesis, the effects of lysergic acid diethylamide result from its antagonistic effect on the 5-hydroxytryptamine in the brain.

In the course of screening derivatives of lysergic acid diethylamide for 5-hydtroxytryptamine-blocking effects, we have found in 2-brom-d-lysergic acid diethylamide, coded BOL 148, a compound which, like lysergic acid diethylamide, strongly antagonizes certain effects of 5-hydroxytryptamine, but unlike lysergic acid diethylamide does not produce abnormal psychic disturbances. The introduction of one bromine atom into the molecule of lysergic acid diethylamide thus completely alters its activity; it loses the characteristic property of producing psychic disturbances in man but retains the strong anti-5 hydroxytryptamine action.
Notes # : (auch BOL 3)
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