α3β4-nicotinic Receptor

The alpha-3 beta-4 nicotinic receptor, also known as the α3β4 receptor and the ganglion-type nicotinic receptor,Pharmacology, (Rang, Dale, Ritter & Moore, , 5th ed., Churchill Livingstone 2003) p. 138. is a type of nicotinic acetylcholine receptor, consisting of CHRNA3, α3 and CHRNB4, β4 Protein subunit, subunits. It is located in the autonomic ganglia and adrenal medulla, where activation yields excitatory postsynaptic potential, post- and/or excitatory presynaptic potential, presynaptic excitation, mainly by increased sodium, Na⁺ and potassium, K⁺ permeability.

As with other nicotinic acetylcholine receptors, the α3β4 receptor is pentameric [(α3)_m(β4)_n where m + n = 5]. The exact subunit stoichiometry is not known and it is possible that more than one functional α3β4 receptor assembles in vivo with varying subunit stoichiometries.

Ligands which inhibit the α3β4 receptor have been shown to modulate drug-seeking behavior, making α3β4 a promising target for the development of novel antiaddictive agents.

Ligands

Agonists

* Acetylcholine (endogenic, endogenous neurotransmitter that binds non-selectively to nAChRs and mAChRs)
* Anabaseine and other structural analogs
* Carbachol
* Cytisine (partial agonist)
* Dimethylphenylpiperazinium
* Epibatidine
* Lobeline Page 149
* Nicotine
* RJR-2429

Antagonists

Competitive

* Dihydro-beta-erythroidine, DHβE
* SR 16584, highly selective over α4β2 and α7

Noncompetitive

* Dextromethorphan
* Dextrorphan
* Dextropropoxyphene
* Hexamethonium
* Imipramine
* Levacetylmethadol
* Mecamylamine
* Methadone
* Tubocurarine
*Bupropion
*Reboxetine
*Ibogaine
*Voacangine
*18-Methoxycoronaridine, 18-MC
*18-Methylaminocoronaridine, 18-MAC
*2-Methoxyethyl-18-methoxycoronaridinate, ME-18-MC
*AT-1001
*Choline

See also

* Alpha-3 beta-2 nicotinic receptor, α3β2-Nicotinic receptor
* Alpha-4 beta-2 nicotinic receptor, α4β2-Nicotinic receptor
* Alpha-7 nicotinic receptor, α7-Nicotinic receptor
* Muscle-type nicotinic receptor

References

{{Nicotinic acetylcholine receptor modulators

Ion channels
Nicotinic acetylcholine receptors