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Exploring the Nature of Molecular Recognition in Nicotinic Acetylcholine Receptors

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Nicotinic acetylcholine receptors (nAChRs) are the subject of ever increasing interest because of their presumed involvement in the etiology of numerous clinical disorders. Unfortunately, the absence of atomic-level structural data, as well as the pharmacological complexity of these receptors leaves many fundamental questions unanswered. An understanding of how ligands interact with the receptor and, in-turn, how these interactions lead to pharmacological effect is vital in the advancement of nAChR-based therapeutics. We will first explore physico-chemical themes that are evidenced to be of particular importance in nAChR molecular recognition; these are- p-cation interaction, conformational entropy and stereochemistry. The second objective of this review is an interpretive encapsulation of the extensive and disparate body of structure-activity data that now exists for nAChRs. Finally, this review will advocate a re-investigation of distance geometry based methods as well as the need for additional approaches in nicotinic receptor pharmacophore generation.

Keywords: 3 pyridylmethylcholine receptor; 5HT3; GABAA; HAB site; NMDA AMPA kinate; NT receptors; acettkcgikube receptors; affinity relationship; allosterism; azabicyclic analogs; cation interaction; centrald nervous system CNS; clinical disorders; conformational entropy; electoron containing moiety; etiology; high affinity binding; hydrogen bond acceptor; ligand gated ion channel; methylcarbamylcholine; molecular recognition; mrmbrane spanning regions; nAChR based therapeutics; nAChR diversity; nAChRs; neuromusculllar Torpedo receptors; neurotransmitters; nicotine; nicotinic; nicotinic ligands; peripheral nervous system; protonation induced chirality; receptor desensitization; receptor kinetics; receptor structure; stereochemistry; stoichiometry; structure activitiy; subtype

Document Type: Review Article


Publication date: 2000-08-01

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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