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AB142815

Desformylflustrabromine hydrochloride, alpha4beta2 modulator

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MW 357.7 Da, Purity >98%. 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..

View Alternative Names

A4 nicotinic receptor, ACH 4, ACHA4_HUMAN, ACHB2_HUMAN, ACHN, AChR, Acetylcholine receptor alpha 4 neural, Acetylcholine receptor beta 2 neural, Acetylcholine receptor neuronal nicotinic alpha 4 subunit, Acra 4, Acrb 2, Alpha4 nAChR, BFNC, CHRNA 4, Cholinergic receptor nicotinic alpha 4, Cholinergic receptor nicotinic alpha polypeptide 4, Cholinergic receptor nicotinic beta 2, Cholinergic receptor nicotinic beta polypeptide 2, Cholinergic receptor nicotinic beta polypeptide 2 neuronal, Chrnb2, EBN, EBN 1, EFNL 3, NACHR, NACRA 4, Neuronal acetylcholine receptor protein beta 2 chain precursor, Neuronal acetylcholine receptor protein subunit beta 2, Neuronal acetylcholine receptor subunit alpha-4, Neuronal acetylcholine receptor subunit beta-2, Neuronal nicotinic acetylcholine receptor alpha 4 subunit, Neuronal nicotinic acetylcholine receptor beta 2, b2 nAchR, cholinergic receptor, nicotinic, beta 2 (neuronal), nAChRB2

1 Images
Chemical Structure - Desformylflustrabromine hydrochloride, alpha4beta2 modulator (AB142815)
  • Chemical Structure

Lab

Chemical Structure - Desformylflustrabromine hydrochloride, alpha4beta2 modulator (AB142815)

2D chemical structure image of ab142815, Desformylflustrabromine hydrochloride, alpha4beta2 modulator

Key facts

CAS number

951322-11-5

Purity

>98%

Form

Solid

form

Molecular weight

357.7 Da

Molecular formula

C<sub>1</sub><sub>6</sub>H<sub>2</sub><sub>2</sub>BrClN<sub>2</sub>

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.

Product protocols

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