Nicotinic assay acetylcholine receptor

Salminen, O., Whiteaker, P., Grady, S.R., Collins, A.C., McIntosh, J.M., Marks, M.J. The subunit composition and pharmacology of alpha-Conotoxin Mil-binding nicotinic acetylcholine receptors studied by a novel membrane-binding assay. Neuropharmacology. 48 696, 2005. 

To illustrate the principles of an equilibrium dialysis experiment, we will describe the binding of [ H] acetylcholine to the nicotinic acetylcholine receptor (nAChR) in native membranes from Torpedo electro-plax. The data obtained from such an experiment are shown in Figure 10-7 where they are compared with data obtained from a centrifugation assay described below (Protocol 4.2). 

Anderson DJ, Puttfarcken PS, Jacobs 1, Faltynek C (2000) Assessment of nicotinic acetylcholine receptor-mediated release of [ H]-norepinephrine from rat brain slices using a new 96-well format assay. Neuropharmacology 39 2663-2672 Anney RJ, Olsson CA, Lotfi-Miri M, Patton GC, Williamson R (2004) Nicotine dependence in a prospective population-based study of adolescents the protective role of a functional tyrosine hydroxylase polymorphism. Pharmacogenetics 14 73-81 Auerbach A, Akk G (1998) Desensitization of mouse nicotinic acetylcholine receptor channels. 

Rao, T. S., Correa, L. D., Reid, R. T., Lloyd, G. K. Evaluation of anti-nociceptive effects of neuronal nicotinic acetylcholine receptor (nAChR) ligands in the rat tail-flick assay, Neuropharmacology 1996, 35, 393-405. 

Sullivan, J. P., Briggs, C. A., Donnelly-Roberts, D., Brioni, J. D., Radek, R. J., McKenna, D. G., Campbell, J. E., Arneric, S. P., Decker, M. W. (+)-Epibatidine can differentially evoke responses mediated by putative subtypes of nicotinic acetylcholine receptors (nAChR) ligands in the rat tail-flick assay, Med. Chem. Res. 1994, 4, 502-516. 

Keywords Recombinant human receptors Functional assays Altinicline Nicotine Parkinson s disease nAChR subtypes Nicotinic acetylcholine receptors Nicotine flux . SIB-1765F Cognitive deficits... 

The anthelmintic activity of the quinolizidine alkaloids has been reviewed [394]. It is well recognised that quinolizidine alkaloids deter or repel insects and non-insect herbivores [394], These compounds can interfere with protein biosynthesis and some bind to acetylcholine receptors with high affinity. (-)-N-methylcytisine (233) and (-)-anagyrine (234) were isolated from the roots of Sophora flavescens, a plant used in traditional Chinese medicine as an anthelmintic. N-methyl cytisine was twice as active as anagyrine but only half as active as (-)cytisine and nicotine [395,396] The alkaloids (3-6 pg) inhibited reproduction of B. xylophilus in the cotton balls assay. 

ACETYLCHOLINE In most regions of the CNS, the effects of ACh, assessed either by iontophoresis or by radioligand-binding assays, appear to be generated by interaction with a mixture of nicotinic and muscarinic receptors. Several presumptive chohnergic pathways have been proposed in addition to that of the motoneuron-Renshaw cell. Eight major clusters of ACh neurons and their pathways have been characterized. 

Lukas, R., and Cullen, M. (1988). An Isotopic Rubidium Ion Efflux Assay for the Functional Characterization of Nicotinic Acetylcholine Receptors on Clonal Cell Lines, . 4na/, Biochem. 175 212—218. 

Acetylcholine receptors can be prepared from a variety of excitable tissues from animals. An example is the electric organ of electric eels, a very dense concentration of excitable tissue and a source of many neuronal receptors. A number of other chemicals competitively bind with anatoxin-a for the acetylcholine receptor (e.g., nicotine, acetylcholine itself, a-bungarotoxin) and have been radiolabeled and used in receptor binding assays for anatoxin-a. 

Nomoto, H., Nagaki, Y, Ishikawa, M., Shoji, H., and Hayashi, K. (1992). Solid-phase neurotoxin binding assay for nicotinic acetylcholine receptor—changes of the binding ability of the receptor with various treatments, y. iVh/. Toxicol. 1 33-44. 

Assays of acetyl- and butyrylcholine esterases inhibition, as well as of modulation of calcium channels and nicotinic receptors have been conducted in vivo. Moreover, their interaction with the active center of acetylcholine esterase has been simulated by molecular dynamics. For synthesized compounds the IC50 of acetylcholine esterase inhibition was about 9 X M, and for the most active the value was four to five times... 

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