Alpha-4 beta-2 nicotinic receptor
Encyclopedia
The alpha-4 beta-2 nicotinic receptor, also known as the α4β2 receptor, is a type of nicotinic acetylcholine receptor
, consisting of α4
and β2
subunit
s. It is located in the brain
, where activation yields post-
and presynaptic excitation, mainly by increased Na+
and K+
permeability.
The receptors exist in the two stoichiometries:
Nicotinic acetylcholine receptor
Nicotinic acetylcholine receptors, or nAChRs, are cholinergic receptors that form ligand-gated ion channels in the plasma membranes of certain neurons and on the postsynaptic side of the neuromuscular junction...
, consisting of α4
CHRNA4
Neuronal acetylcholine receptor subunit alpha-4 is a protein that in humans is encoded by the CHRNA4 gene....
and β2
CHRNB2
Neuronal acetylcholine receptor subunit beta-2 is a protein that in humans is encoded by the CHRNB2 gene....
subunit
Protein subunit
In structural biology, a protein subunit or subunit protein is a single protein molecule that assembles with other protein molecules to form a protein complex: a multimeric or oligomeric protein. Many naturally occurring proteins and enzymes are multimeric...
s. It is located in the brain
Brain
The brain is the center of the nervous system in all vertebrate and most invertebrate animals—only a few primitive invertebrates such as sponges, jellyfish, sea squirts and starfishes do not have one. It is located in the head, usually close to primary sensory apparatus such as vision, hearing,...
, where activation yields post-
Excitatory postsynaptic potential
In neuroscience, an excitatory postsynaptic potential is a temporary depolarization of postsynaptic membrane potential caused by the flow of positively charged ions into the postsynaptic cell as a result of opening of ligand-sensitive channels...
and presynaptic excitation, mainly by increased Na+
Sodium
Sodium is a chemical element with the symbol Na and atomic number 11. It is a soft, silvery-white, highly reactive metal and is a member of the alkali metals; its only stable isotope is 23Na. It is an abundant element that exists in numerous minerals, most commonly as sodium chloride...
and K+
Potassium
Potassium is the chemical element with the symbol K and atomic number 19. Elemental potassium is a soft silvery-white alkali metal that oxidizes rapidly in air and is very reactive with water, generating sufficient heat to ignite the hydrogen emitted in the reaction.Potassium and sodium are...
permeability.
The receptors exist in the two stoichiometries:
- (α4)2(β2)3 receptors have high sensitivity to nicotineNicotineNicotine is an alkaloid found in the nightshade family of plants that constitutes approximately 0.6–3.0% of the dry weight of tobacco, with biosynthesis taking place in the roots and accumulation occurring in the leaves...
and low Ca2+ permeability (HS receptors) - (α4)3(β2)2 receptors have low sensitivity to nicotine and high Ca2+ permeability (LS receptors)
Agonists
- AcetylcholineAcetylcholineThe chemical compound acetylcholine is a neurotransmitter in both the peripheral nervous system and central nervous system in many organisms including humans...
- CytisineCytisineCytisine, also known as baphitoxine and sophorine, is a pyridine-like alkaloid. In medical use, it improves the rate of smoking cessation. It is less effective but much cheaper than similar products. Its structure is similar to nicotine and has similar pharmacological effects...
- EpibatidineEpibatidineEpibatidine is an alkaloid found on the skin of the endangered Ecuadorian frog, Epipedobates tricolor. These frogs, like other poison dart frogs, are best known for their ability to sequester poisons from their prey and secrete these poisons onto their backs. Many Amerindian tribes would swipe the...
- NicotineNicotineNicotine is an alkaloid found in the nightshade family of plants that constitutes approximately 0.6–3.0% of the dry weight of tobacco, with biosynthesis taking place in the roots and accumulation occurring in the leaves...
- A-84,543
- A-366,833A-366,833A-366,833 is a drug developed by Abbott, which acts as an agonist at neural nicotinic acetylcholine receptors selective for the α4β2 subtype, and has been researched for use as an analgesic, although it has not passed clinical trials....
- ABT-418ABT-418ABT-418 is a drug developed by Abbott, which acts as an agonist at neural nicotinic acetylcholine receptors. It binds with high affinity to the α4β2, α2β2 and α7 subtypes, but not to the α3β4 subtype. It has nootropic, neuroprotective and anxiolytic effects, and has been researched for treatment of...
- AltiniclineAltiniclineAltinicline is a drug which acts as an agonist at neural nicotinic acetylcholine receptors with high selectivity for the α4β2 subtype...
- DianiclineDianiclineDianicline is a drug developed by Sanofi-Aventis which acts as a partial agonist at neural nicotinic acetylcholine receptors. It is subtype-selective, binding primarily to the α4β2 subtype. It is being developed as a medication for the treatment of nicotine dependence to assist in smoking cessation...
- IsproniclineIsproniclineIspronicline is a drug which acts as a partial agonist at neural nicotinic acetylcholine receptors. It is subtype-selective, binding primarily to the α4β2 subtype. It has antidepressant, nootropic and neuroprotective effects, and is under development for the treatment of dementia and Alzheimer's...
- Pozanicline
- RivaniclineRivaniclineRivanicline is a drug which acts as a partial agonist at neural nicotinic acetylcholine receptors. It is subtype-selective, binding primarily to the α4β2 subtype...
- TebaniclineTebaniclineTebanicline is a drug developed by Abbott, which acts as a partial agonist at neuronal nicotinic acetylcholine receptors, binding to both the α3β4 and the α4β2 subtypes...
- Varenicline
- Sazetidine ASazetidine ASazetidine A is a drug which acts as a subtype selective partial agonist at α4β2 neural nicotinic acetylcholine receptors, acting as an agonist at 23 pentamers, but as an antagonist at 32 pentamers...
: full agonist on (α4)2(β2)3, 6% efficacy on (α4)3(β2)2 - N-(3-pyridinyl)-bridged bicyclic diamines
Antagonists
- (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane
- 2-fluoro-3-(4-nitro-phenyl)deschloroepibatidine
- Coclaurine - alkaloid from Nelumbo nuciferaNelumbo nuciferaNelumbo nucifera, known by a number of names including Indian Lotus, Sacred Lotus, Bean of India, or simply Lotus, is a plant in the monogeneric family Nelumbonaceae...
- MecamylamineMecamylamineMecamylamine is a nonselective and noncompetitive antagonist of the nicotinic acetylcholine receptors that was introduced in the 1950s as an antihypertensive agent.- Uses :...
- α-Conotoxin
- PNU-120,596
See also
- α3β4-Nicotinic receptorAlpha-3 beta-4 nicotinic receptorThe alpha-3 beta-4 nicotinic receptor, also known as the α3β4 receptor, is a type of nicotinic acetylcholine receptor, consisting of α3 and β4 subunits. It is located in the brain, where activation yields post- and presynaptic excitation....
- α7-Nicotinic receptorAlpha-7 nicotinic receptorThe alpha-7 nicotinic receptor, also known as the α7 receptor, is a type of nicotinic acetylcholine receptor, consisting entirely of α7 subunits....