Sophion

nAchR - alpha7

The nicotic alpha-7 receptor (α7) is a monomeric type of nicotinic acetylcholine receptor, consisting entirely of α7 subunits.

It is involved in controlling post- and presynaptic excitation, mainly by increased Ca2+ permeability.

Localization:
Brain

QPatch recordings of alpha7


Fig. 1: α7 response to 10 mM Ach. The rise time was found to be between 5-10 ms for 10 mM Ach.

 

Agonist:
Acetylcholine, Nicotine, 3-2,4 dimethoxybenzylidene anabaseine (DMXBA)

 
Fig. 2: Hill fit analysis of acetylcholine induced alpha7 response

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

PNU-120596: Removal of desensitization

NS-1738: Marginal effects on α7 desensitization kinetics, increases peak amplitude.

Sophion material:

Application reports:
GH4-C1 Nicotinic Acetylcholine α7

Posters:
Parallel patch clamp of α7 nicotinic acetylcholine receptor channels (1.85 MB)

Article:
Request a copy of the article "Characterization of compounds on nicotinic acetylcholine receptor alpha7 channels using higher throughput electrophysiology".

Other references:

Timmerman et al, 2007: An allosteric Modulator of the α7 nicotinic Acetylcholine Receptor Possessing Cognition Enhancing Properties in vivo, Journal of Pharmacology and Experimental Therapeutics

John Dunlop, Renza Roncarati Brian Jow, Hendrick Bothmann, Tim Lock, Dianne Kowal, Mark Bowlby and Georg c. Terstappen: In vitro screening strategies for nicotinic receptor ligands, biochemical pharmacology 74 (2007) 1172 - 1181

Briggs CA and McKenna DG, 1996: Effect of MK-801 at the human α7 nicotinic acetylcholine receptor. Neuropharmacology 35: 407 - 414

Hurst et al, 2005: A Novel Positive allosteric Modulator of the α7 Neuronal Nicotinic Acetylcholine Receptor: In Vitro and In Vivo Characterization, The Journal of Neuroscience April 27, 2005, 25(17): 4396 - 4405


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