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

Acetylcholine Nicotinic Receptor Targets

Nicotinic (α4β2) Receptors

Nicotinic (α7) Receptors (Nicotinic (α7) Receptors)

Related Targets

Acetylcholine Muscarinic Receptors

Nicotinic Receptors (Other Subtypes)

Cholinesterases (Cholinesterases)

Other Acetylcholine

Nicotinic Receptors (Non-selective)

 

Literature 

Alzheimer's Disease Poster

Alzheimer's disease (AD) is a debilitating and progressive neurodegenerative disease and the most common cause of dementia, affecting approximately 30% of individuals aged over 85 years. This poster summarizes the cellular and molecular mechanisms of AD.

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Parkinson's Disease 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.

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Receptor Data

Nicotinic Receptor (nAChRs) Pharmacological Data

GeneSpeciesGene SymbolGene Accession No.Protein Accession No.
α1 (muscle)HumanCHRNA1NM_000079P02708
MouseChrna1NM_007389P04756
RatChrna1NM_024485P25108
α2 (neuronal)HumanCHRNA2NM_000742Q15822
MouseChrna2NM_144803Q91X60
RatChrna2NM_133420P12389
α3HumanCHRNA3NM_000743P32297
MouseChrna3NM_145129Q8R4G9
RatChrna3NM_052805P04757
α4HumanCHRNA4NM_000744P43681
MouseChrna4NM_015730O70174
RatChrna4NM_024354P09483
α5HumanCHRNA5NM_000745P30532
MouseChrna5NM_176844Q2MKA5
RatChrna5NM_017078P20420
α6HumanCHRNA6NM_004198Q15825
MouseChrna6NM_021369Q9R0W9
RatChrna6NM_057184P43143
α7HumanCHRNA7NM_000746P36544
MouseChrna7NM_007390P49582
RatChrna7NM_012832Q05941
α9HumanCHRNA9NM_017581Q9UGM1
MouseChrna9NM_001081104NP_001074573
RatChrna9NM_022930P43144
α10HumanCHRNA10NM_020402Q9GZZ6
MouseChrna10NM_001081424NP_001074893
RatChrna10NM_022639Q9JLB5
β1HumanCHRNB1NM_000747P11230
MouseChrnb1NM_009601P09690
RatChrnb1NM_012528P25109
β2HumanCHRNB2NM_000748P17787
MouseChrnb2NM_009602Q9ERK7
RatChrnb2NM_019297P12390
β3HumanCHRNB3NM_000749Q05901
MouseChrnb3NM_173212Q8BMN3
RatChrnb3NM_133597P12391
β4HumanCHRNB4NM_000750P30926
MouseChrnb4NM_148944Q8R493
RatChrnb4NM_052806P12392
δHumanCHRNDNM_000751Q07001
MouseChrndNM_021600P02716
RatChrndNM_019298P25110
εHumanCHRNENM_000080Q04844
MouseChrneNM_009603P20782
RatChrneNM_017194P09660
γHumanCHRNGNM_005199P07510
MouseChrngNM_009604P04760
RatChrngNM_019145P18916

Nicotinic Pharmacological Receptor Data

nACh Receptor Subtypeα2β4α7α3β4
LocalisationCNS - Cortex, thalamus, hippocampus,striatumAutonomic ganglia, hippocampus, limbic system, cortex, chick retinaAutonomic ganglia, adrenal gland, hippocampus
Tissue FunctionSynaptic transmission, anti-nociception, anxiolytic, memorySynaptic transmission, auditory gating, memorySynaptic transmission
Key CompoundsKi (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
AntagonistsChlorisinamide (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