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. . As with other nicotinic acetylcholine receptors, functional α7 receptors are pentameric [i.e., (α7)5 stoichiometry].

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

Agonists

 * (+)-N-(1-azabicyclo[2.2.2]oct-3-yl)benzo[b]furan- 2-carboxamide: potent and highly subtype-selective
 * A-582941: partial agonist; activates ERK1/2 and CREB phosphorylation; enhances cognitive performance
 * AR-R17779: full agonist, nootropic
 * TC-1698: subtype-selective; neuroprotective effects via activation of the JAK2/PI-3K cascade, neutralized by angiotensin II AT(2) receptor activation
 * TC-5619 - partial agonist, in development for treatment of schizophrenia
 * GTS-21 - partial agonist, in development for treatment of schizophrenia and/or Alzheimer's disease
 * PHA-543,613
 * PNU-282,987
 * PHA-709829: potent and subtype-selective; robust in vivo efficacy in a rat auditory sensory gating model
 * Analogues: improved hERG safety profile over PNU-282,987
 * SSR-180,711: partial agonist
 * Tropisetron: subtype-selective partial agonist; 5-HT3 receptor antagonist
 * WAY-317,538
 * Anabaseine
 * Choline
 * Nicotine

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


 * PNU-120,596
 * NS-1738: marginal effects on α7 desensitization kinetics; modestly brain-penetrant
 * 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 In clinical development for cognitive deficits in schizophrenia.
 * A-867744
 * Ivermectin
 * Galantamine

Antagonists

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