[General Articles] Muscarinic and Nicotinic Cholinergic Agonists: Structural Analogies and Discrepancies

Zsolt      Bikadi; Miklos      Simonyi

Abstract

Acetylcholine, the first identified neurotransmitter acts on both types of cholinergic receptors. Both rigid and flexible derivatives of acetylcholine could either be selective muscarinic or selective nicotinic agonists while some compounds show activity at both receptor subclasses. Earlier structure-activity considerations are revisited. Ligand and receptor based calculations have been applied in the hope to identify characteristic geometrical and steric requirements for the activity on the receptor subtypes. Results are treated critically and applied cautiously for predicting selective structural requirements by the cholinergic receptor subclasses.

Keywords: acetylcholine conformation, cholinergic agonist, muscarinic selectivity, nicotinic selectivity, torsion angle, heteroatomic distances, steric exclusion, docking

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Current Medicinal Chemistry

Title: [General Articles] Muscarinic and Nicotinic Cholinergic Agonists: Structural Analogies and Discrepancies

Volume: 10 Issue: 23

Author(s): Zsolt Bikadi and Miklos Simonyi

Affiliation:

Keywords: acetylcholine conformation, cholinergic agonist, muscarinic selectivity, nicotinic selectivity, torsion angle, heteroatomic distances, steric exclusion, docking

Abstract: Acetylcholine, the first identified neurotransmitter acts on both types of cholinergic receptors. Both rigid and flexible derivatives of acetylcholine could either be selective muscarinic or selective nicotinic agonists while some compounds show activity at both receptor subclasses. Earlier structure-activity considerations are revisited. Ligand and receptor based calculations have been applied in the hope to identify characteristic geometrical and steric requirements for the activity on the receptor subtypes. Results are treated critically and applied cautiously for predicting selective structural requirements by the cholinergic receptor subclasses.

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Bikadi Zsolt and Simonyi Miklos, [General Articles] Muscarinic and Nicotinic Cholinergic Agonists: Structural Analogies and Discrepancies, Current Medicinal Chemistry 2003; 10 (23) . https://dx.doi.org/10.2174/0929867033456521

DOI https://dx.doi.org/10.2174/0929867033456521	Print ISSN 0929-8673
Publisher Name Bentham Science Publisher	Online ISSN 1875-533X

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