68724-22-1Relevant articles and documents
Molecular requirements at the cholinergic receptors. Importance of ether oxygens in the dioxolane series
Melchiorre,Angeli,Giannella,et al.
, p. 357 - 361 (2007/10/07)
The synthesis and the pharmacological screening of cis-5-methyl-3-dimethylaminomethyltetrahydrofurane methiodide (1) and 4-dehydroxymuscarine (2) are reported. The high cholinergic activity exhibited by 1 and 2 shows that the substitution of the oxygen atoms in 3 or in 1 of cis-2-methyl-4-dimethylaminomethyl-1,3-dioxolane methiodide (3), taken as a model of the best fitting agonist, does not alter sensitively the biological profile of the molecule. The hypothesis is then formulated that the occupation of only one of the two receptorial sites reacting with the nuclear oxygens of 3 is sufficient to induce a clear-cut cholinergic activity.