• nAChRα3β4

    repetitive activation by nicotine measured on the
    Patchliner


  • nAChRα3β4

    nicotine concentration response curve
    measured on the Patchliner

  • nAChRα3β4

    block by mecamylamine
    recorded on the Patchliner

AChRa3b4 | nicotinic acetylcholine receptor alpha 3 beta 4

Family:
Acetylcholine Receptors

Subgroups:
The family has been devided into nicotinic acetylcholine receptors (ionotropic channels) and muscarinic acetylcholine receptors (metabotropic G-protein coupled receptors). Both subgroups are sensitive to acetylcholine.

Topology:
Nicotinic acetylcholine receptors: As typical cys-loop receptors, acetylcholine receptor subunits contain four transmembrane spanning domains TM1-TM4. Five subunits form a pore, homomeric and heteromeric combinations are possible.17 vertebrate subunits have been identified: α genes: CHRNA1 - CHRNA10; β genes: CHRNB1 . CHRNB4, as well as CHRND (delta), CHRNE (epsilon), CHRNG (gamma)
Muscarinic acetylcholine receptors: 5 receptors have been described (M1 - M5), encoded by the 5 genes CHRM1 - CHRM5. These proteins contain seven transmembrane regions and do not form homo or heteromers. 

AChRα3β4: Background Information


Overview:

The alpha-3 beta-4 nicotinic receptor, also known as the α3β4 receptor and the ganglion-type nicotinic receptor, is a type of nicotinic acetylcholine receptor, consisting of α3 and β4 subunits. In the peripheral nervous system (PNS), the most abundant subtypes are α3β2* and α3β4* and are prominently expressed by ganglionic neurons. Because the α3β4 AChR subtype is predominantly expressed in nociceptive DRG neurons, it has been suggested that this subtype may be involved in neuronal signalling of nociception and inflammation.


Data Sheet:

Gene:
CHRNA3, CHRNB4

Human Protein:
UniProt P32297, P30926

Tissue:
Brain, hippocampus, cerebellum, retina. (α3β4β2) nAChRs are present on glutamate axons innervating Stratum radiatum (SR) interneurons and possibly other interneurons. PNS: The α3β4 subtype is prominently expressed in a variety of PNS neurons including those of DRG, superior cervical ganglia, cardiac ganglia, and ganglia innervating the viscera. The α3 subunit is furthermore expressed in the adrenal gland and lymphoid tissue

Function/ Application:
Mediates effects of acetylcholine and nicotine in specific regions of the brain, retina and spinal cord, post- and presynaptic excitation

Pathology:
Sporadic amyotrophic lateral sclerosis, genetic variations in CHRNA3 (Neuronal acetylcholine receptor subunit alpha-3) have been associated with susceptibility to smoking-related behavioral traits and lung cancer, nicotine dependence

Accessory subunits:
Neuronal AChR is composed of two different types of subunits: alpha and beta. Alpha-3 subunit can be combined to beta-2 or beta-4 to give rise to functional receptors (furthermore, the Alpha-3 subunit can form a neuronal nicotinic acetylcholine receptor complex with the AChR Alpha-5 subunit: Alpha-3, Alpha-5, Beta-2 or Alpha-3, Alpha-5, Beta-4)

Interaction:
RIC3, LYPD6, alpha-conotoxin ImI

Modulator:
Acetylcholine, nicotine, epibatidine, DHβE, mecamylamine, α-conotoxin, hexamethonium, A-867744, NS1738

Assays:
Patch Clamp: whole cell, room temperature

Reviews and Links

Data and Applications

Acetylcholine Receptor Alpha 3 Beta 4 - Activation

a3b4

icon sp96   SyncroPatch 96 (a predecessor model of SyncroPatch 384PE) data and applications:

Shown is a raw current response of a HEK293 cell expressing AChR (α3β4) to exposure to 300 μM nicotine. Solutions were  stacked (layered) in the pipette to achieve brief exposure times.

 

Acetylcholine Receptor Alpha 3 Beta 4 - Concentration Response Curve to Nicotine

nAChRa3b4_nic_DRC_PL

icon pl  Patchliner data and applications:

Shown are the a raw current responses of a HEK293 cell expressing AChR (α3β4) to increasing concentrations of nicotine. Solutions were  stacked (layered) in the pipette to achieve brief exposure times.

 

Application Notes

Publications

2020 - Discovery and Development of SUVN-911: A Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression

icon pl  Patchliner publication in Journal of Medicinal Chemistry (2020)

Authors:
Nirogi R., Mohammed A.R., Shinde A.K., Ravella S.R., Bogaraju N., Subramanian R., Mekala V.R., Palacharla R.C., Muddana N., Thentu J.B., Bhyrapuneni G., Abraham R., Jasti V.

 

 

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