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 Nicotinic acetylcholine receptors, or nAChRs, are Receptor (biochemistry), receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the c ...

, consisting of α3 and β4 subunits. It is located in the

autonomic ganglia An autonomic ganglion is a cluster of neuron, nerve cell Cell body, bodies (a ganglion) in the autonomic nervous system. The two types are the sympathetic ganglion and the parasympathetic ganglion. References

Autonomic ganglia, Auto ...

and

adrenal medulla The adrenal medulla () is the inner part of the adrenal gland. It is located at the center of the gland, being surrounded by the adrenal cortex. It is the innermost part of the adrenal gland, consisting of chromaffin cells that secrete catecho ...

, where activation yields

post- ''Post-'' (stylized in all caps) is the third solo studio album by American singer-songwriter Jeff Rosenstock, released on January 1, 2018, without any promotional lead-up. The album was released on Polyvinyl Record Co. in the United States and ...

and/or presynaptic excitation, mainly by increased Na⁺ and 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 Stoichiometry () is the relationships between the masses of reactants and Product (chemistry), products before, during, and following chemical reactions. Stoichiometry is based on the law of conservation of mass; the total mass of reactants must ...

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

Source:

Agonists

Acetylcholine Acetylcholine (ACh) is an organic compound that functions in the brain and body of many types of animals (including humans) as a neurotransmitter. Its name is derived from its chemical structure: it is an ester of acetic acid and choline. Par ...

(

endogenous Endogeny, in biology, refers to the property of originating or developing from within an organism, tissue, or cell. For example, ''endogenous substances'', and ''endogenous processes'' are those that originate within a living system (e.g. an ...

neurotransmitter A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a Chemical synapse, synapse. The cell receiving the signal, or target cell, may be another neuron, but could also be a gland or muscle cell. Neurotra ...

that binds non-selectively to nAChRs and

mAChRs Muscarinic acetylcholine receptors (mAChRs) are acetylcholine receptors that form G protein-coupled receptor complexes in the cell membranes of certain neurons and other cells. They play several roles, including acting as the main end-recepto ...

) *

Anabaseine Anabaseine (3,4,5,6-tetrahydro-2,3′-bipyridine) is an alkaloid toxin produced by ''Nemertines'' worms and ''Aphaenogaster'' ants. It is structurally similar to nicotine and anabasine. Similarly, it has been shown to act as an agonist on most ni ...

and other structural analogs *

Carbachol Carbachol, also known as carbamylcholine and sold under the brand name Miostat among others, is a cholinomimetic drug that binds and activates acetylcholine receptors. Thus it is classified as a cholinergic agonist. It is primarily used for v ...

Cytisine Cytisine, also known as baptitoxine, cytisinicline, or sophorine, is an alkaloid that occurs naturally in several plant genera, such as '' Laburnum'' and '' Cytisus'' of the family Fabaceae. It has been used medically to help with smoking cessa ...

(partial agonist) *

Dimethylphenylpiperazinium Dimethylphenylpiperazinium (DMPP) is a nicotinic acetylcholine receptor agonist which is selective for the ganglionic subtype. One of the earliest reports on the pharmacology of DMPP, describing it as a ganglion-stimulating, hypertensive agent ...

Epibatidine Epibatidine is a chlorinated alkaloid that is secreted by the Ecuadoran frog '' Epipedobates anthonyi'' and poison dart frogs from the ''Ameerega'' genus. It was discovered by John W. Daly in 1974, but its structure was not fully elucidated u ...

Lobeline Lobeline is a piperidine alkaloid found in a variety of plants, particularly those in the genus '' Lobelia'', including Indian tobacco ('' Lobelia inflata''), Devil's tobacco ('' Lobelia tupa''), great lobelia ('' Lobelia siphilitica''), '' Lobe ...

Page 149 *

Nicotine Nicotine is a natural product, naturally produced alkaloid in the nightshade family of plants (most predominantly in tobacco and ''Duboisia hopwoodii'') and is widely used recreational drug use, recreationally as a stimulant and anxiolytic. As ...

RJR-2429 RJR-2429 is a drug that acts as an agonist at neural nicotinic acetylcholine receptors, binding to both the α3β4 and the α4β2 subtypes. RJR-2429 is stronger than nicotine Nicotine is a natural product, naturally produced alkaloid in ...

Antagonists

Competitive

* DHβE * SR 16584, highly selective over α4β2 and α7

Noncompetitive

Dextromethorphan Dextromethorphan, sold under the brand name Robitussin among others, is a cough suppressant used in many cough and Common cold, cold medicines. In 2022, the US Food and Drug Administration (FDA) approved the combination dextromethorphan/bupropi ...

Dextrorphan Dextrorphan (DXO) is a psychoactive drug of the morphinan class which acts as an antitussive or cough suppressant and in high doses a dissociative hallucinogen. It is the dextrorotatory enantiomer of racemorphan; the levorotatory enantiome ...

Dextropropoxyphene Dextropropoxyphene is an analgesic in the opioid category, patented in 1955 and manufactured by Eli Lilly and Company. It is an optical isomer of levopropoxyphene. It is intended to treat mild pain and also has antitussive (cough suppressan ...

Hexamethonium Hexamethonium is a non-depolarising ganglionic blocker, a neuronal nicotinic ( nAChR) receptor antagonist that acts in autonomic ganglia by binding mostly in or on the nAChR receptor, and not the acetylcholine binding site itself. It does no ...

Imipramine Imipramine, sold under the brand name Tofranil, among others, is a tricyclic antidepressant (TCA) mainly used in the treatment of depression. It is also effective in treating anxiety and panic disorder. Imipramine is taken by mouth. Common s ...

Levacetylmethadol Levacetylmethadol (INN), levomethadyl acetate ( USAN), OrLAAM (trade name) or levo-α-acetylmethadol (LAAM) is a synthetic opioid similar in structure to methadone. It has a long duration of action due to its active metabolites. Medical uses LA ...

Mecamylamine Mecamylamine (INN, BAN; or mecamylamine hydrochloride (USAN); brand names Inversine, Vecamyl) is a non-selective, non-competitive antagonist of the nicotinic acetylcholine receptors (nAChRs) that was introduced in the 1950s as an antihypertens ...

Methadone Methadone, sold under the brand names Dolophine and Methadose among others, is a synthetic opioid used medically to treat chronic pain and opioid use disorder. Prescribed for daily use, the medicine relieves cravings and opioid withdrawal sym ...

Tubocurarine Tubocurarine (also known as ''d''-tubocurarine or DTC) is a toxic benzylisoquinoline alkaloid historically known for its use as an arrow poison. In the mid-1900s, it was used in conjunction with an anesthetic to provide skeletal muscle relaxat ...

Bupropion Bupropion, formerly called amfebutamone, and sold under the brand name Wellbutrin among others, is an atypical antidepressant that is indicated in the treatment of major depressive disorder, seasonal affective disorder, and to support smo ...

Reboxetine Reboxetine, sold under the brand name Edronax among others, is a selective norepinephrine reuptake inhibitor (sNRI) medication marketed as an antidepressant by Pfizer for use in the treatment of major depressive disorder, although it has also be ...

Ibogaine Ibogaine is a psychoactive indole alkaloid derived from plants such as '' Tabernanthe iboga'', characterized by hallucinogenic and oneirogenic effects. Traditionally used by Central African foragers, it has undergone controversial research ...

Voacangine Voacangine (12-methoxyibogamine-18-carboxylic acid methyl ester) is an alkaloid found predominantly in the root bark of the ''Voacanga africana'' tree, as well as in other plants such as '' Tabernanthe iboga'', ''Tabernaemontana africana'', '' Tra ...

* 18-MC * 18-MAC * ME-18-MC * AT-1001 *

Choline Choline is a cation with the chemical formula . Choline forms various Salt (chemistry), salts, such as choline chloride and choline bitartrate. An essential nutrient for animals, it is a structural component of phospholipids and cell membrane ...

References