Nicotinic (α4β2) Receptors

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.

Products
Background
Literature (4)
Gene Data

Nicotinic (α4β2) Receptor Agonists

Cat. No. Product Name / Activity
5017 A 85380 dihydrochloride
High affinity and selective α4β2 nAChR agonist
5079 ABT 089 dihydrochloride
High affinity and selective α4β2 nAChR partial agonist
6576 ABT 594 hydrochloride
Selective α4β2 nAChR agonist
3549 3-Bromocytisine
Potent α4β4, α4β2 and α7 nAChR agonist
5236 CC4
High affinity and subtype-selective α6β2 and α4β2 nAChR partial agonist
6706 DPNB-ABT 594
Caged ABT 594 (Cat. No. 6576); suitable for one- or two-photon photolysis
3546 (-)-Nicotine ditartrate
Prototypical nAChR agonist
1053 RJR 2403 oxalate
Selective α4β2 nAChR agonist
4766 SIB 1508Y maleate
Potent agonist of α4β2, α2β4, α4β4 and α3β4 nACh receptors
2737 TC 2559 difumarate
Selective α4β2 nAChR partial agonist
6865 uPSEM 792 hydrochloride
α4β2 partial agonist; uPSEM agonist for PSAM4-GlyR and PSAM4-5HT3; brain-penetrant
3754 Varenicline tartrate
Selective α4β2 nAChR partial agonist; orally active

Nicotinic (α4β2) Receptor Antagonists

Cat. No. Product Name / Activity
2349 Dihydro-β-erythroidine hydrobromide
α4β2, muscle type and Torpedo nAChR antagonist

Nicotinic (α4β2) Receptor Modulators

Cat. No. Product Name / Activity
5963 CMPI hydrochloride
Potent positive allosteric modulator of α4β2 nAChRs; also inhibitor of (α4)2(β2)3, muscle-type and Torpedo nAChRs
3328 Desformylflustrabromine hydrochloride
Positive allosteric modulator of α4β2 nAChRs; also muscle-type nAChR inhibitor
4141 LY 2087101
Allosteric potentiator of α7, α4β2 and α4β4 nAChRs
5112 NS 9283
Positive allosteric modulator of α4β2 nAChRs

Other

Cat. No. Product Name / Activity
2736 Sazetidine A dihydrochloride
α4β2 nAChR ligand; may act as an agonist or a desensitizer

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.

External sources of pharmacological information for Nicotinic (α4β2) Receptors :

Literature for Nicotinic (α4β2) Receptors

Tocris offers the following scientific literature for Nicotinic (α4β2) Receptors to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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Nicotinic ACh Receptors Scientific Review

Nicotinic ACh Receptors Scientific Review

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Nicotinic (α4β2) Receptor Gene Data

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