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Updated: Aug 14, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
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Published on: August 16, 2018

Acetylcholine nicotinic receptors: finding the putative binding site of allosteric modulators using the "blind

Bogdan Iorga1, Denyse Herlem, Elvina Barré

  • 1Institut de Chimie des Substances Naturelles, CNRS UPR 2301, Avenue de la Terrasse, F-91198, Gif-sur-Yvette, France. Bogdan.Iorga@icsn.cnrs-gif.fr

Journal of Molecular Modeling
|December 24, 2005
PubMed

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Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
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Binding sites linkages can regulate a protein's function.  For example, enzyme activity is often regulated through a feedback mechanism where the end product of the biochemical process serves as an inhibitor.
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