ELB-139
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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 Affinity may refer to: Commerce, finance and law * Affinity (law), kinship by marriage * Affinity analysis, a market research and business management technique * Affinity Credit Union, a Saskatchewan-based credit union * Affinity Equity Par ...
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.gov
for 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 {{Anxiolytic-stub