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.
Nicotinic (α4β2) Receptor Agonists |
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|---|---|
| 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 |
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| 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 |
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| 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
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