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.

Targets
Literature
Receptor Data

Literature for Acetylcholine Nicotinic Receptors

Neurodegeneration

Neurodegeneration Product Guide

A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

  • Alzheimer's disease
  • Parkinson's disease
  • Huntington's disease
Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
Nicotinic ACh Receptors

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.

Alzheimer's

Alzheimer's Poster

Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.

Learning & Memory

Learning & Memory Poster

Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.

Pain

Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.

Parkinson's

Parkinson's Poster

Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.

Schizophrenia

Schizophrenia Poster

Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.

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