Desformylflustrabromine hydrochloride, alpha4beta2 modulator

Supplementary info

This supplementary information is collated from multiple sources and compiled automatically.

Activity summary

The Nicotinic Acetylcholine Receptor alpha 4 (CHRNA4) and beta 2 (CHRNB2) also known as nAChR α4β2 are subunits of a pentameric ligand-gated ion channel. This receptor is involved in neurotransmission by binding with the neurotransmitter acetylcholine causing an ion flow through the channel. The receptor which has a mass of approximately 290 kDa is expressed in the central nervous system particularly in areas such as the cerebral cortex and thalamus. Its expression is important for the modulation of synaptic activity and cognitive functions.

Biological function summary

These nicotinic receptors play a role in the complex of heteromeric assemblies contributing to the regulation of ion influx in neurons. They influence neural excitability and synaptic plasticity impacting processes such as learning and memory. The formation of these receptors requires the assembly of both alpha 4 and beta 2 subunits which dictates the receptor's specific functional properties and pharmacological profile.

Pathways

The nAChR α4β2 receptor significantly contributes to the cholinergic signaling pathway. This pathway is critical in mediating responses to the neurotransmitter acetylcholine in both the autonomic nervous system and the central nervous system. The receptor interacts with other proteins such as GABA receptors influencing neurotransmitter release which integrates into the network of choline metabolism and signaling processes.

Associated diseases and disorders

Mutations or dysfunction in the nAChR α4β2 receptor associate with neurological conditions like epilepsy and Alzheimer's disease. For instance mutations in CHRNA4 can lead to autosomal dominant nocturnal frontal lobe epilepsy. The altered receptor function can disrupt normal neural communication resulting in the symptoms observed in these disorders. The receptor's interactions with other proteins like the dopamine transporter further link it to conditions such as nicotine addiction and reward pathways.