Erowid References Database
Sandoz Laboratories Basle.
“Methysergide (UML-491), a new serotonin antagonist”.
Scientific Exhibit, Federation of American Societies for Experimental Biology. 1960 April.
UML (with the generic name methysergide) is a highly effective and highly specific serotonin antagonist. It may be used in affections in the pathogenesis of which serotonin might be of importance. Favorable results were reported especially in migraine and other vascular headaches. As a further indication primary chronic joint rheumatism and related affections, allergy and Raynaud's disease are mentioned. . Chemically UML (1-methyl-lysergic acid butanolamide) is a closely related to Methergine (lysergic acid butanolamide), but is pharmacologically significantly different. Its toxicity in animal experiments is much lower (LD50 i.v. in rabbits 28.0 mg/kg, Methergine 2.6 mg/kg). The oxytocic effect on the rabbit uterus in situ is 16 times weaker than that of Methergine. . The antiserotonin effect of UML is in vitro on the isolated rat uterus, 4000f that of LSD (Methergine 73.5%). The effect is highly specific, since on this experimental object the antagonism of UML towards serotonin is 9200 times stronger than that towards acetylcholine. In vivo UML proved superior to LSD etc. in experiments on rats which were given UML or LSD and the sensitivity of the isolated uterus of these animals to serotonin was tested. The serotonin edema of the rat paw is antagonized 4.4 times stronger by UML than by LSD. The strong antiserotonin effect on the intact animal is demonstrated also on the inhibition of the pressor effect of serotonin in dogs, as well as on the inhibition of the barbiturate- potentiating effect of serotonin in mice. The barbiturate-potentiating effect of chlorpromazine is not influenced by UML, an indication of the specificity of its serotonin antagonism.
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