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 (4)

Receptor Data

Acetylcholine Nicotinic Receptor Target Files

• Nicotinic (α4β2) Receptors

• Nicotinic (α7) Receptors

Related Targets

• Acetylcholine Muscarinic Receptors
• Acetylcholine Transporters
• Caged Nicotinic Compounds
• Cholinesterases

• Nicotinic Receptors (Non-selective)
• Nicotinic Receptors (Other Subtypes)
• Other Acetylcholine

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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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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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.

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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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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