Acetylcholine Nicotinic Receptors
Nicotinic receptors (nAChRs) are ligand-gated ion channels that modulate cell membrane potentials. Each receptor is composed of pentameric combinations of subunits (α1-10, β1-4, δ, ε and γ). Nicotinic receptors are generally divided into three functional classes: muscle subunits (α1, β1, δ, ε, γ), standard neuronal subunits (α1-6 and β2-4) that form in pairwise αβ combinations, and subunits (α7-9) that can form homomeric nAChRs. Neuronal nicotinic receptors are found in the central nervous system and in autonomic ganglia where they regulate processes such as transmitter release, cell excitability and neuronal integration. Nicotinic receptors located at the neuromuscular junctions of somatic muscles are responsible for muscular contraction.
Literature for Acetylcholine Nicotinic Receptors
Tocris offers the following scientific literature for Acetylcholine Nicotinic Receptors to showcase our products. We invite you to request* your copy today!
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Nicotinic ACh Receptors Scientific Review
Updated in 2014, this review by Sue Wonnacott summarizes the diverse structure and function of nicotinic acetylcholine receptors and gives an in-depth review of the ligands available for nAChR research. Compounds available from Tocris are listed.
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Nicotinic Receptor (nAChRs) Pharmacological Data
| Gene | Species | Gene Symbol | Gene Accession No. | Protein Accession No. |
|---|---|---|---|---|
| α1 (muscle) | Human | CHRNA1 | NM_000079 | P02708 |
| Mouse | Chrna1 | NM_007389 | P04756 | |
| Rat | Chrna1 | NM_024485 | P25108 | |
| α2 (neuronal) | Human | CHRNA2 | NM_000742 | Q15822 |
| Mouse | Chrna2 | NM_144803 | Q91X60 | |
| Rat | Chrna2 | NM_133420 | P12389 | |
| α3 | Human | CHRNA3 | NM_000743 | P32297 |
| Mouse | Chrna3 | NM_145129 | Q8R4G9 | |
| Rat | Chrna3 | NM_052805 | P04757 | |
| α4 | Human | CHRNA4 | NM_000744 | P43681 |
| Mouse | Chrna4 | NM_015730 | O70174 | |
| Rat | Chrna4 | NM_024354 | P09483 | |
| α5 | Human | CHRNA5 | NM_000745 | P30532 |
| Mouse | Chrna5 | NM_176844 | Q2MKA5 | |
| Rat | Chrna5 | NM_017078 | P20420 | |
| α6 | Human | CHRNA6 | NM_004198 | Q15825 |
| Mouse | Chrna6 | NM_021369 | Q9R0W9 | |
| Rat | Chrna6 | NM_057184 | P43143 | |
| α7 | Human | CHRNA7 | NM_000746 | P36544 |
| Mouse | Chrna7 | NM_007390 | P49582 | |
| Rat | Chrna7 | NM_012832 | Q05941 | |
| α9 | Human | CHRNA9 | NM_017581 | Q9UGM1 |
| Mouse | Chrna9 | NM_001081104 | NP_001074573 | |
| Rat | Chrna9 | NM_022930 | P43144 | |
| α10 | Human | CHRNA10 | NM_020402 | Q9GZZ6 |
| Mouse | Chrna10 | NM_001081424 | NP_001074893 | |
| Rat | Chrna10 | NM_022639 | Q9JLB5 | |
| β1 | Human | CHRNB1 | NM_000747 | P11230 |
| Mouse | Chrnb1 | NM_009601 | P09690 | |
| Rat | Chrnb1 | NM_012528 | P25109 | |
| β2 | Human | CHRNB2 | NM_000748 | P17787 |
| Mouse | Chrnb2 | NM_009602 | Q9ERK7 | |
| Rat | Chrnb2 | NM_019297 | P12390 | |
| β3 | Human | CHRNB3 | NM_000749 | Q05901 |
| Mouse | Chrnb3 | NM_173212 | Q8BMN3 | |
| Rat | Chrnb3 | NM_133597 | P12391 | |
| β4 | Human | CHRNB4 | NM_000750 | P30926 |
| Mouse | Chrnb4 | NM_148944 | Q8R493 | |
| Rat | Chrnb4 | NM_052806 | P12392 | |
| δ | Human | CHRND | NM_000751 | Q07001 |
| Mouse | Chrnd | NM_021600 | P02716 | |
| Rat | Chrnd | NM_019298 | P25110 | |
| ε | Human | CHRNE | NM_000080 | Q04844 |
| Mouse | Chrne | NM_009603 | P20782 | |
| Rat | Chrne | NM_017194 | P09660 | |
| γ | Human | CHRNG | NM_005199 | P07510 |
| Mouse | Chrng | NM_009604 | P04760 | |
| Rat | Chrng | NM_019145 | P18916 |
Nicotinic Pharmacological Receptor Data
| nACh Receptor Subtype | α2β4 | α7 | α3β4 | |
|---|---|---|---|---|
| Localisation | CNS - Cortex, thalamus, hippocampus,striatum | Autonomic ganglia, hippocampus, limbic system, cortex, chick retina | Autonomic ganglia, adrenal gland, hippocampus | |
| Tissue Function | Synaptic transmission, anti-nociception, anxiolytic, memory | Synaptic transmission, auditory gating, memory | Synaptic transmission | |
| Key Compounds | Ki (nM) | |||
| Agonists |
(±-)Anatoxin A (0789) (-)-Cytisine (1390) (±)-Epibatidine (0684) (-)-Lobeline (1077) RJR 2403 (1053) UB 165 (1348) |
1.3-4.2 0.14-2.7 0.01-0.05 4-50 26 0.27-0.44 |
707-1840 1400-3883 20.6-233 11000-13100 36000 2790 |
ND 56-195 0.38 480 ND ND |
| Antagonists |
Chlorisinamide (1001) Dihydro-β-erythroidine (2349) Methylcaconitine (1029) TMPH (2438) |
686000 370* 3700-6100 1400* |
ND ND 0.69-10.3 1000* |
ND 23100* ND 200* |
*IC50 values
Our Nicotinic Acetylcholine Receptor review summarizes the structure and function of nAChR receptors, and the pharmacological ligands used to study them.
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