Alpha-7 nicotinic receptor

Alpha-7 nicotinic receptor


The alpha-7 nicotinic receptor, also known as the α7 receptor, is a type of nicotinic acetylcholine receptor, consisting entirely of α7 subunits.[1] As with other nicotinic acetylcholine receptors, functional α7 receptors are pentameric [i.e., (α7)5 stoichiometry].

It is located in the brain, lymphocyte and spleen where activation yields post- and presynaptic excitation,[1] mainly by increased Ca2+ permeability.

Medical relevance

Recent work has demonstrated a potential role in reducing inflammatory neurotoxicity in stroke, MI, sepsis, and alzheimers disease.[2][3][4]

An α7 nicotinic agonist appears to have positive effects on neurocognition in persons with schizophrenia.[5]

Ligands

Agonists

Positive Allosteric Modulators (PAMs)

At least two types of positive allosteric modulators (PAMs) can be distinguished.[14]

  • PNU-120,596[15]
  • NS-1738: marginal effects on α7 desensitization kinetics; modestly brain-penetrant[16]
  • 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[17] In clinical development for cognitive deficits in schizophrenia.
  • A-867744[18][19]
  • Ivermectin
  • Galantamine

Other

Antagonists

  • α-conotoxin ArIB[V11L,V16D]: potent and highly subtype-selective; slowly reversible[23]
  • Memantine
  • Quinolizidine (–)-1-epi-207I: α7 subtype preferring blocker[24]

See also

References