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 α3 and β4

subunit Subunit may refer to: *Subunit HIV vaccine, a class of HIV vaccine *Protein subunit, a protein molecule that assembles with other protein molecules *Monomer, a molecule that may bind chemically to other molecules to form a polymer *Sub-subunit, a ...

s. It is located in the

autonomic ganglia An autonomic ganglion is a cluster of nerve cell bodies (a ganglion) in the autonomic nervous system The autonomic nervous system (ANS), formerly referred to as the vegetative nervous system, is a division of the peripheral nervous system that s ...

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

Zaveri's nAChR-selective ligand number 5 (2010) with tube model

* 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

References