Anseculin is a new coumarine derivative with promising cognition improving properties. We investigated its possible effects on passive avoidance learning in young and aged mice and the possible relationship to its alpha(1)-antagonistic properties.A single dose of anseculin did not affect long-term memory of young and aged mice. Moreover, in young mice, subchronic treatment with anseculin had no effect on cognitive functions, whereas aged, cognitively impaired mice clearly showed improved long-term memory with no effects on short-term memory. Further biochemical studies of aged control mice showed in comparison to the young mice a significant decrease of central alpha(1)-adrenoceptors density, but unchanged alpha(1)-adrenoceptor-mediated IP hydrolysis. Subchronic treatment with anseculin had no effect on the density of central alpha(1)-adrenoceptors in young adult mice and only a small although not significant effect on the density of cognitively-impaired aged mice. Furthermore, anseculin has no effects on alpha(1)-adrenoceptor-mediated IP hydrolysis.

01 Jun 2002·CNS Drug Reviews

Ensaculin (KA‐672. HCl): A Multitransmitter Approach to Dementia Treatment

Review

Author: Michael Noeldner ; Robert Hoerr

ABSTRACTEnsaculin, a novel benzopyranone substituted with a piperazine moiety, showed memory‐enhancing effects in paradigms of passive and conditioned avoidance in both normal and artificially amnesic rodents. It exhibited neuroprotective activities in an NMDA toxicity model and neurotrophic effects in primary cultured rat brain cells. The compound could be characterized as a weak NMDA receptor–operated channel blocker. In receptor‐binding studies, ensaculin was found to have high affinities to serotonergic 5‐HT1A and 5‐HT7 receptors, adrenergic α1, and dopaminergic D2 and D3 receptors. Due to its unique pharmacodynamic profile, ensaculin may have potential as an antidementia agent acting on various transmitter systems.

01 Jun 2000·European Journal of PharmacologyQ3 · MEDICINE

Effects of ensaculin on dopamine metabolite levels and K+-induced glutamate release

Q3 · MEDICINE

Article

Author: Teismann, P. ; Ferger, B.

In vivo microdialysis with the new antidementia compound ensaculin was performed in freely moving rats to study the alterations in dopaminergic and glutamatergic neurotransmission. Ensaculin (0.1 and 1 mg/kg i.p.) significantly increased extracellular levels of the dopamine metabolites 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA). Furthermore, ensaculin (1 mg/kg i.p.) showed a non-significant tendency to reduce the K(+)-induced glutamate release. The data suggest that ensaculin may have moderate D(2) antagonistic properties. Thus, besides its possible role as a cognitive enhancer, ensaculin may also have moderate antipsychotic properties.

100 Deals associated with Ensaculin Hydrochloride

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Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	Phase 3	-	Schwabe AG	-
Alzheimer Disease	Phase 3	DE	Dr. Willmar Schwabe GmbH & Co. KG	-

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