ELB-139
Encyclopedia
ELB-139 is an anxiolytic
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
at GABAA receptor
s, with highest affinity for the α3 subtype, but highest efficacy at α1 and α2. It has primarily anxiolytic
and anticonvulsant
effects, but produces little sedative
effects or ataxia
, and has also been demonstrated in rats to increase serotonin
levels in the striatum
and prefrontal cortex
, 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 elbion AG registered a clinical trial in ClinicalTrials.gov
for the treatment of anxiety associated with panic disorder but the results have not been reported.
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...
drug with a novel chemical structure, which is used in scientific research. It has similar effects to benzodiazepine
Benzodiazepine
A benzodiazepine is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring...
drugs, but is structurally distinct and so is classed as a nonbenzodiazepine
Nonbenzodiazepine
The nonbenzodiazepines, also called benzodiazepine-like drugs, are a class of psychoactive drugs pharmacologically resembling the benzodiazepines, with similar benefits, side effects and risks, despite having dissimilar or entirely different chemical structures.-Classes:There are currently three...
anxiolytic.
ELB-139 is a subtype-selective partial agonist
Partial agonist
Partial agonists bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist...
at GABAA receptor
GABA A receptor
The GABAA receptor is an ionotropic receptor and ligand-gated ion channel. Its endogenous ligand is γ-aminobutyric acid , the major inhibitory neurotransmitter in the central nervous system. Upon activation, the GABAA receptor selectively conducts Cl- through its pore, resulting in...
s, with highest affinity for the α3 subtype, but highest efficacy at α1 and α2. It has primarily anxiolytic
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...
and anticonvulsant
Anticonvulsant
The anticonvulsants are a diverse group of pharmaceuticals used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of bipolar disorder, since many seem to act as mood stabilizers, and in the treatment of neuropathic pain. The goal of an...
effects, but produces little sedative
Sedative
A sedative or tranquilizer is a substance that induces sedation by reducing irritability or excitement....
effects or ataxia
Ataxia
Ataxia is a neurological sign and symptom that consists of gross lack of coordination of muscle movements. Ataxia is a non-specific clinical manifestation implying dysfunction of the parts of the nervous system that coordinate movement, such as the cerebellum...
, and has also been demonstrated in rats to increase serotonin
Serotonin
Serotonin or 5-hydroxytryptamine is a monoamine neurotransmitter. Biochemically derived from tryptophan, serotonin is primarily found in the gastrointestinal tract, platelets, and in the central nervous system of animals including humans...
levels in the striatum
Striatum
The striatum, also known as the neostriatum or striate nucleus, is a subcortical part of the forebrain. It is the major input station of the basal ganglia system. The striatum, in turn, gets input from the cerebral cortex...
and prefrontal cortex
Prefrontal cortex
The prefrontal cortex is the anterior part of the frontal lobes of the brain, lying in front of the motor and premotor areas.This brain region has been implicated in planning complex cognitive behaviors, personality expression, decision making and moderating correct social behavior...
, without affecting dopamine
Dopamine
Dopamine is a catecholamine neurotransmitter present in a wide variety of animals, including both vertebrates and invertebrates. In the brain, this substituted phenethylamine functions as a neurotransmitter, activating the five known types of dopamine receptors—D1, D2, D3, D4, and D5—and their...
levels. It has been proposed as a possible candidate for a novel non-sedating anxiolytic or anticonvulsant drug for use in humans. The sponsor elbion AG registered a clinical trial in ClinicalTrials.gov
for the treatment of anxiety associated with panic disorder but the results have not been reported.