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
Gene:
CHRNA3, CHRNB4
Human Protein:
UniProt P32297, P30926
Tissue:
Brain, retina, spinal cord, peripheral neuronal tissues, including neurons of mammalian sympathetic ganglia, parasympathetic ganglia, sensory neurons such as the trigeminal ganglia and adrenal chromaffin cells
Function/ Application:
Mediates effects of acetylcholine and nicotine in specific regions of the brain, retina and spinal cord
Pathology:
Alzheimer's disease, Parkinson's, Tourette's Syndrome, depression
Accessory subunits:
Interaction:
Modulator:
DHβE, mecamylamine, α-conotoxin, hexamethonium, A-867744, NS1738
Assays:
Patch Clamp: whole cell, room temperature
Cell systems:
Stably-transfected HEK293 cell line
Recommended Reviews:
Physiol Rev 89: 73–120, 2009; doi:10.1152/physrev.00015.2008, Albuquergue et al; Nicotinic acetylcholine receptors, in: Burger’s Medicinal Chemistry, Vol II Drug Discovery and Drug Development, Chapter 11, pp 357-405. Ed. Abraham, D., J. Wiley, New York., Colquhoun et al.
Data and Applications
Acetylcholine Receptor Alpha 3 Beta 4 - Activation
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
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
Acetylcholine Receptor Alpha 3 Beta 4 - " Nicotinic a3b4 receptors recorded on Nanion's Patchliner"
Patchliner application note: 
(0.5 MB)
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
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.