Nicotinic receptor probe

Stauffer, D.A., and Karlin, A. (1994) Electrostatic potential of the acetylcholine binding sites in the nicotinic receptor probed by reaction of binding-site cysteines with charged methanethiosulfonates. Biochemistry 33, 6840-6849. 

The naturally occurring enantiomer, (+)-anatoxin-a, is much more potent than (—)-anatoxin-a [38]. For example, using conditions that preferentially labeled rat brain a4p2 nACh receptors with [ H]nicotine, the natural enantiomer was found to be 1000-fold more potent than (—[-anatoxin [39]. This enantiospecificity of anatoxin-a has provided an excellent tool for probing the stereospedfidty of the ACh binding site on the nicotinic receptor. 

Nowak MW, Kearney PC, Satirpson JR, Saks ME, Labarca CG, Silverman SK, Zhong WG, Thorson J, Abelson JN, Davidson N, Schultz PG, Dougherty DA, Lester HA. Nicotinic receptor binding site probed with urmatural amino acid incorporation in intact cells. Science 1995 268 439-442. 

P), 60,000 (56,279) (y) and 65,000 (57,565) (6) (the first value is from SDS the value in brackets is the exact M, based on amino acid composition) in the ratio 2 1 1 1, with an average 40% amino-acid sequence identity between all 4 chains [B.M.Conti-Troconi et al. Science 218 (1982) 1227-1229]. DNA for all 4 subunits has been cloned and sequenced [M. Noda et al. Nature 301 (1983) 251-254]. The covalent affinity probes, [ H]-bromoacetylcholine and 4-(AI-maleiniideo)- H tenzyl trimethylammonium iodide, label the a-subunit by reacting with cysteine residues 192 and 193. Thus, each of ffie two a-subunits carries an acetylcholine binding site, and there are 2 sites per oligomeric receptor. When incorporated into liposomes or planar li bilaye the nicotinic receptor permits a flux of a, which is promoted... 

Structure of fluorescent probes that have been used to study ligand binding to the Torpedo nicotinic acetylcholine receptor... 

Studies of brain mechanisms have tended to focus primarily on structures associated with the mesolimbic DA pathway. Ideally, all brain regions with major concentrations of nicotinic acetylcholine receptors should be probed with nicotinic... 

Cytisine (30), from Cytisus scoparius L., has been found to be a selective and specific probe for the nicotinic-type acetylcholine receptor (nAChR) as a partial agonist and has served as the lead compound... 

Pereira, E.F.R. et al., Physostigmine and galanthamine probes for a novel binding site on the a4 32 subtype of neuronal nicotinic acetylcholine receptors stably expressed in fibroblast cells, J. Pharmacol. Exp. Ther., 270, 768, 1994. 

NPE-caged ATP was used to probe the kinetics of muscle contraction, but its release rate was modest and, more importantly, the caged compound was not completely inactive [18, 19]. Sometimes, the increased lipophilicity of the cage is undesirable. To prevent the interaction of NPE-caged carbamoylcholin with the nicotin acetylcholine receptor before photolysis a negatively charged... 

Tantama M, Lin W-C, Licht S (2008) An activity-based protein profiling probe for the nicotinic acetylcholine receptor. J Am Chem Soc 130 15766-15767... 

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