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Cerletti A, Doepfner W. 
“Spezifische Steigerung der serotoninantagonistischen Wirkung von Lysergsäurederivaten durch Methylierung des Indolstickstoffes der Lysergsäure.”. 
Helvet. physiol. pharmacol. acta. 1958;16:C55-C57.
Methylation of the indole N (position 1) in LSD nd BOL 148 increases the antagonism to serotonin (5-HT) on the isolated rat uterus by 3.7 fold and 5.3 fold respectively (Cerletti & Doepfner, J.Pharmacol.Exper.Therap. 122, 124, 1958). . Methylation produces a much greater increase in the anti-5-HT effect of various derivatives of LSD which are themselves greatly inferior to LSD as antagonists of 5-HT. If the anti-5-HT effect of LSD is taken as 100, methylation increased the antagonism of lysergic acid ethylamide (LAE) from 12 to 835, of lysergic acid pyrrolidid from 4.7 to 130, of lysergic acid amide from 4.3 to 160, of ergonovine from 17 to 400, of Methergine from 60 to 250. . These studies were made on the rat uterus. The methyl derivatives are not all more powerful than the corresponding initial preparations with regard to the inhibition of edema induced in the rat paw by 5-HT. Thus, the s.c. doses of LSD, BOL 148 and their methyl derivatives required for 50 0nhibition of the edema are not significantly different. By contrast, methylation of ergonovine and Methergine enhances the antagonism to 5-HT in the rat paw. The specific nature of this effect also increases, as the uterotonic effect and certain central nervous effects diminish.
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