The transport of the neutral amino acid L-leucine as well as of choline and D-glucose across the blood-brain barrier (BBB) of male Wistar rats was studied after 14-day exposure to ethanol and treatment with the nootropic drug AWD 52-39 (1). After ethanol exposure the half-saturation constant (Km) and the maximum velocity of transport (Vmax) declined in the majority of the investigated brain regions. Also, the treatment elicited a regionally different increase of the permeability-surface area (PS) product of choline (between 10% and 33%) and glucose (between 12% and 27%). The changes in the blood-brain transfer of the three compounds were diminished or prevented by additional application of 1. The cerebral blood flow was increased by the exposure to ethanol by maximally 44%. After additional administration of 1 the changes were reversed and the blood flow reached control values. In addition, the activity of the enzyme acetylcholine esterase was determined in the striatum and the hippocampus. After ethanol exposure the enzyme activity declined by 32%. It was less diminished after treatment with 1. The latter effects let assume that the changes of the BBB permeability elicited by ethanol and 1 are related to alterations of brain metabolism.

01 Feb 1992·Die Pharmazie

Effect of AWD 52-39 on vasoconstriction induced by noradrenaline and 5-hydroxytryptamine in vitro and in vivo in rats.

Article

Author: Glusa, E ; Müller, H

The vascular effect of the potential nootropic AWD 52-39 (1; N,N-diacetoxyethyl-9,10-dihydrolysergic acid amide) as well as its influence on noradrenaline- or 5-HT-induced vasoconstriction were studied in the isolated rat aorta and in anesthetized normotensive and pithed rats. Vasoconstriction was determined by measuring the increase in mean arterial pressure (MAP). Both in vitro and in pithed rats, 1 caused a slight vasoconstriction, whereas a dose-dependent short-lasting decrease in mean arterial pressure was found in normotensive rats. In vitro and in pithed rats, 1 exerted no influence on the noradrenaline-induced vasoconstriction, while the 5-HT-induced contractile response was significantly inhibited. These findings characterize 1 as a competitive antagonist at vascular 5-HT2 receptors without any alpha-adrenolytic effect.

01 Apr 1989·Activitas nervosa superior

AWD 52-39, an ergot derivative with potential nootropic activity.

Article

Author: Hoffman, W ; Siegemund, C ; Rostock, A ; Bartsch, R

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Indication	Highest Phase	Country/Location	Organization	Date
Cognition Disorders	Phase 2	-	Degussa AG	-
Cognition Disorders	Phase 2	-	elbion AG	-
Cognition Disorders	Phase 2	DE	elbion NV	-

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