Dioxane and oxathiane nuclei: Suitable substructures for muscarinic agonists
Copyright policy )Dioxane and oxathiane nuclei: Suitable substructures for muscarinic agonists
Muscarinic agonists, bearing 1,4-dioxane and 1,4-oxathiane nuclei, were synthesized and tested to evaluate their potency at M(1)-M(4) muscarinic receptor subtypes. The stereochemical relationship between the 2-side chain and the 6-methyl group plays an important role in drug-receptor interaction, since the cis isomers are more potent than the corresponding trans isomers. However, the latter are able to discriminate between the muscarinic receptor subtypes. Among them compound 5b proves particularly interesting, since it selectively activates the ileal M(3) receptor subtype and is devoid of agonist activity at the others.
- University of Florence Italy
- University of Bari Aldo Moro Italy
- University of Camerino Italy
Male, Models, Molecular, Magnetic Resonance Spectroscopy, Subtype selectivity, Guinea Pigs, 1,4-Dioxane nucleu, 1,4-Oxathiane nucleu, Muscarinic Agonists, Crystallography, X-Ray, Dioxanes, Heterocyclic Compounds, 1-Ring, Isomerism, Ileum, Animals, Heart Atria, Lung, Receptor, Muscarinic M3, Receptor, Muscarinic M2, Dose-Response Relationship, Drug, Receptor, Muscarinic M1, 1,4-Oxathiane nucleus, Muscle, Smooth, 540, Muscarinic agonist, Indicators and Reagents, Rabbits
Male, Models, Molecular, Magnetic Resonance Spectroscopy, Subtype selectivity, Guinea Pigs, 1,4-Dioxane nucleu, 1,4-Oxathiane nucleu, Muscarinic Agonists, Crystallography, X-Ray, Dioxanes, Heterocyclic Compounds, 1-Ring, Isomerism, Ileum, Animals, Heart Atria, Lung, Receptor, Muscarinic M3, Receptor, Muscarinic M2, Dose-Response Relationship, Drug, Receptor, Muscarinic M1, 1,4-Oxathiane nucleus, Muscle, Smooth, 540, Muscarinic agonist, Indicators and Reagents, Rabbits
selected citations These citations are derived from selected sources.This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).38 popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.Top 10% influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).Top 10% impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.Top 10%
Citations provided by BIP!Popularity provided by BIP!