Nicotinic (α4β2) Receptors

Supporting information

Nicotinic α4β2 receptors have high affinity for nicotine and account for >90% of [3H]-nicotine binding to brain tissues. A stoichiometry of (α4)2(β2)3 has been proposed, generating two agonist binding sites consistent with the model of the muscle nAChR.

Manipulation of the stoichiometry of α4β2 nAChRs expressed in Xenopus oocytes indicates that (α4)3(β2)2 nAChRs are also viable, displaying lower affinity for ACh and higher Ca2+ permeability; whether native nAChRs with this subunit stoichiometry exist is not known.

Transgenic knockout of either of these subunits eliminates nicotine self administration, whereas virally targeted re-expression of the β2 subunit in mesolimbic areas of β2 knockout mice recovers this behavior, implicating a role for α4β2 nAChRs in nicotine addiction. α4β2 nAChRs are highly expressed in the thalamus and have been suggested to have a putative role in the thalamo-cortical circuitry . As a consequence of their putative role in thalamo-cortical circuitry, gain of function mutations in the M2 domain of either the α4 or β2 subunit give rise to some forms of autosomal dominant nocturnal frontal lobe epilepsy. The human genes encoding the nicotinic α4 and β2 receptor subunits have been localized to chromosomes 13 (q13.2-q13.3) and 1 (1q21.3) respectively.

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Gene Species Gene Symbol Gene Accession No. Protein Accession No.
α4 Human CHRNA4 NM_000744 P43681
Mouse Chrna4 NM_015730 O70174
Rat Chrna4 NM_024354 P09483
β2 Human CHRNB2 NM_000748 P17787
Mouse Chrnb2 NM_009602 Q9ERK7
Rat Chrnb2 NM_019297 P12390

Literature for Nicotinic (α4β2) Receptors

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Nicotinic ACh Receptors Scientific Review

Updated in 2014, this review 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 ACh Receptors Scientific Review
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Our Neurodegeneration guide highlights over 275 products for neurodegeneration research. Request copy or view PDF today.

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Nicotinic ACh Review

Written by Susan Wonnacott

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Our Nicotinic Acetylcholine Receptor review summarizes the structure and function of nAChR receptors, and the pharmacological ligands used to study them. Request copy or view PDF today.

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Our Alzheimer's disease poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease. Request copy or view PDF today.

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