Description
Key facts
CAS number:951322-11-5,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:357.7 Da,
Molecular formula:C16H22BrClN2,
PubChem:56675778,
Nature:Synthetic,
Solubility:Soluble in DMSO to 100 mM,
Biochemical name:Desformylflustrabromine Hydrochloride,
Biological description:Selective positive allosteric nAChR α4β2 modulator (Ki = 3400 nM). Increases whole cell current when co-applied with effective concentrations of ACh. Anti-addictive effects in vivo.,
Canonical smiles:CC(C)(C=C)C1=C(C2=C(N1)C=C(C=C2)Br)CCNC.Cl,
InChi:InChI=1S/C16H21BrN2.ClH/c1-5-16(2,3)15-13(8-9-18-4)12-7-6-11(17)10-14(12)19-15;/h5-7,10,18-19H,1,8-9H2,2-4H3;1H,
InChiKey:GEZWEAPBLKXKGN-UHFFFAOYSA-N,
IUPAC Name:2-[6-bromo-2-(2-methylbut-3-en-2-yl)-1H-indol-3-yl]-N-methylethanamine;hydrochloride
Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions-+4°C, Appropriate long-term storage conditions-+4°C, Storage information-The product can be stored for up to 12 months
Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
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.
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.
