ELB-139 (LS-191,811) is an
anxiolytic
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiet ...
drug with a novel chemical structure, which is used in scientific research. It has similar effects to
benzodiazepine drugs, but is structurally distinct and so is classed as a
nonbenzodiazepine anxiolytic.
ELB-139 is a subtype-selective
partial agonist
In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonis ...
at
GABAA receptors, with highest
affinity
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for the α3 subtype, but highest
efficacy at α1 and α2. It has primarily
anxiolytic
An anxiolytic (; also antipanic or antianxiety agent) is a medication or other intervention that reduces anxiety. This effect is in contrast to anxiogenic agents which increase anxiety. Anxiolytic medications are used for the treatment of anxiet ...
and
anticonvulsant effects, but produces little
sedative effects or
ataxia
Ataxia is a neurological sign consisting of lack of voluntary coordination of muscle movements that can include gait abnormality, speech changes, and abnormalities in eye movements. Ataxia is a clinical manifestation indicating dysfunction of ...
, and has also been demonstrated in rats to increase
serotonin levels in the
striatum and
prefrontal cortex
In mammalian brain anatomy, the prefrontal cortex (PFC) covers the front part of the frontal lobe of the cerebral cortex. The PFC contains the Brodmann areas BA8, BA9, BA10, BA11, BA12, BA13, BA14, BA24, BA25, BA32, BA44, BA45, BA46 ...
, without affecting
dopamine levels. It has been proposed as a possible candidate for a novel non-sedating anxiolytic or anticonvulsant drug for use in humans The sponsor registered a clinical trial in
ClinicalTrials.govfor the treatment of anxiety associated with panic disorder but the results have not been reported. It was developed by Arzneimittelwerk Dresden in the 1990s.
References
Anxiolytics
Chloroarenes
Imidazolines
Ureas
Lactams
1-Piperidinyl compounds
GABAA receptor positive allosteric modulators
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