Alpha-7 nicotinic receptor
The alpha-7 nicotinic receptor, also known as the α7 receptor, is a type of
subunits.[1] As with other nicotinic acetylcholine receptors, functional α7 receptors are pentameric [i.e., (α7)5 stoichiometry
].
It is located in the
permeability.Further, recent work has implicated this receptor as being important for generation of adult mammal neurons in the retina.
Medical relevance
Recent work has demonstrated a potential role in reducing inflammatory neurotoxicity in stroke, myocardial infarction, sepsis, and Alzheimer's disease.[4][5][6]
An α7 nicotinic agonist appears to have positive effects on neurocognition in persons with schizophrenia.[7]
Activation of α7 nicotinic acetylcholine receptor on mast cells, is a mechanism by which nicotine enhances atherosclerosis.[8]
Both
α7-nicotinic receptors also appear to be involved in
Ligands
Agonists
- (+)-N-(1-azabicyclo[2.2.2]oct-3-yl)benzo[b]furan- 2-carboxamide: potent and highly subtype-selective[14]
- Tilorone.
- A-582941: partial agonist; activates
- AR-R17779: full agonist, nootropic
- Amyloid beta: neurotoxic marker of Alzheimer's disease[16]
- TC-1698: subtype-selective; neuroprotective effects via activation of the angiotensin II AT(2) receptor activation[17]
- Bradanicline - partial agonist, in development for treatment of schizophrenia
- Encenicline - partial agonist with nootropic properties, in development for treatment of schizophrenia and Alzheimer's disease [18][19]
- GTS-21 - partial agonist, in development for treatment of schizophrenia and/or Alzheimer's disease
- PHA-543,613 - selective and potent agonist with nootropic properties [20][21]
- PNU-282,987 - selective and potent agonist, but may cause long QT syndrome
- PHA-709829: potent and subtype-selective; robust in vivo efficacy in a rat auditory sensory gating model[22]
- SSR-180,711: partial agonist[24]
- Tropisetron: subtype-selective partial agonist; 5-HT3 receptor antagonist[25]
- WAY-317,538- selective potent full agonist with nootropic and neuroprotective properties
- Anabasine
- Acetylcholine
- Nicotine
- Epiboxidine[26]
- Choline[27]
- ICH-3: subtype-selective partial agonist[28]
Positive allosteric modulators (PAMs)
At least two types of positive allosteric modulators (PAMs) can be distinguished.[29]
- PNU-120,596[30]
- NS-1738: marginal effects on α7 desensitization kinetics; modestly brain-penetrant[31]
- AVL-3288: unlike the above PAMs, AVL-3288 does not affect α7 desensitization kinetics, and is readily brain penetrant. Improves cognitive behavior in animal models[32] In clinical development for cognitive deficits in schizophrenia.
- A-867744[33][34]
- Ivermectin
Other
Antagonists
It is found that
carboxyl-terminal domains of the receptors.[38]
- Anandamide
- α-Bungarotoxin
- α-Conotoxin ArIB[V11L,V16D]: potent and highly subtype-selective; slowly reversible[39]
- β-Caryophyllene[40]
- Bupropion (very weakly)
- Dehydronorketamine
- Ethanol
- Hydroxybupropion (very weakly)
- Hydroxynorketamine
- Ketamine
- Kynurenic acid
- Memantine
- Lobeline
- Methyllycaconitine[20]
- Norketamine
- Quinolizidine (−)-1-epi-207I: α7 subtype preferring blocker[41]
See also
- α3β2-Nicotinic receptor
- α3β4-Nicotinic receptor
- α4β2-Nicotinic receptor
- chaperone proteinfor α7 receptors
- Endocannabinoids
References
- ^ ISBN 0-443-07145-4, 5th ed., Churchill Livingstone 2003) p. 138.
- PMID 28147247.
- S2CID 25872540.
- PMID 21921156.
- PMID 17273548.
- PMID 21368056.
- PMID 16754836.
- PMID 27834689.
- S2CID 17166624.
- PMID 18844224.
- S2CID 17889977.
- PMID 28551702.
- PMID 22359587.
- PMID 15808471.
- PMID 18482100.
- PMID 23776240.
- S2CID 7730290.
- S2CID 19669958.
- ^ "Archived copy" (PDF). Archived from the original (PDF) on 2013-03-19. Retrieved 2014-03-13.
{{cite web}}: CS1 maint: archived copy as title (link) - ^ S2CID 22477612.
- S2CID 10791918.
- PMID 18490160.
- PMID 17011782.
- PMID 17019409.
- PMID 11212100.
- PMID 22566097.
- ^ González-Rubio, Juana M; Rojo, Jonathan; Tapia, Laura; Maneu, Victoria; Mulet, José; Valor, Luis M.; Criado, Manuel; Sala, Francisco; García, Antonio G. (2004). Borges, R.; Gandía, L. (eds.). Choline as a tool to evaluate nicotinic receptor function in chromaffin cells (PDF). Luis Gandía. Spain: Instituto Teófilo Hernando.
{{cite book}}:|work=ignored (help) - S2CID 21407917.
- S2CID 2460247.
- PMID 15858066.
- S2CID 35392171.
- PMID 17470817.
- PMID 19419141.
- S2CID 5470552.
- PMID 11039729.
- S2CID 27825145.
- S2CID 25914087.
- S2CID 23201726.
- PMID 17497892.
- PMID 26965491.
- S2CID 17490742.