Cholinergic ligands

Decker MW, Brioni JD, Sullivan JP, Buckley MJ, Radek RJ, Raszkiewicz JL, Kang CH, Kim DJ, Giardina WJ, Wasicak JT, et al. (1994). (S)-3-methyl-5-(l-methyl-2-pyrrolidinyl)isoxazole (ABT 418) a novel cholinergic ligand with cognition-enhancing and anxiolytic activities II. In vivo characterization. J Pharmacol Exp Ther. 270(1) 319-28. 

Prinz H, Maelicke A. 1983. Interaction of cholinergic ligands with the purified acetylcholine receptor protein. II. Kinetic studies. J Biol Chem 258 10273-10282. 

G. A. Development of a nonisotopic acetylcholine receptor assay for the investigation of cholinergic ligands. Anal. Chim. Acta 1992, 267, 55-62. 

Cholinergic ligands Nicotinic acetylcholine receptor (nAChR) [85]... 

Does the "active" conformation of a cholinergic ligand correspond to its preferred stereochemistry or is an energetically less favored form bound to the receptor ... 

The affinity of MLA for the nicotinic receptor in the cockroach nerve cord also appeared to be rather less than that for the housefly head receptor, suggesting that there might be different subclasses of insect receptor. This theory was proposed recently by Battersby and Hall (13), who showed that lobeline, another plant-derived cholinergic ligand, had a higher affinity for the cockroach receptor than for the housefly head receptor. 

R.A., 1999a. Synthesis, receptor binding and QSAR studies on 6-substituted nicotine derivatives as cholinergic ligands. Eur. J. Med. Chem. 34, 31-40. 

Stereochemistry of cholinergic ligands and stereoselectivity of receptors has played an important role in design of cholinergic ligands as therapeutic agents. This role becomes apparent in subsequent sections. 

The techniques used include equilibrium dialysis [11] and fluorescence procedures [12]. Another method is based on the observation that the rate of binding of a-bungarotoxin (aBgt) to the receptor is affected by cholinergic ligands [13] and permits rapid estimation of the receptor affinities of a wide spectrum of nonradioactive, nondialyzable drugs. 

Table 1. Competition between a-bungarotoxin and other cholinergic ligands studied by partition...

One major protein, MW 40,000, is labeled labeling is blocked by reversible cholinergic ligands or snake neurotoxins... 

Burgermeister, W., W. L. Klein, M. Nirenberg, and B. Witkop Comparative binding studies with cholinergic ligands and histrionicotoxin at muscarinic receptors of neural cell lines. Mol. Pharmacol. 14, 751—767 (1978). 

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