In order to get infolmation on the molecular requirements of the cholinergic receptor, pure cis and, trans 2-methyl-5-dimethylaminomethyl-1,3-oxathiolane methiodide 2a-b and the corresponding sulfoxides 3a-b and sulfones 4a-b have synthesized and tested. Compound 2a was found to be very active, being 2 times more potent than muscarone and some 20 times more potent than Ach on Guinea Pig lleum, while 3a is equipotent with ACh on he same pràparation. The results of the pharmacological screening seem to suggest that 2a-b and 3a-d-interact with different subsite of the receptor.
Molecular requirements of the active sites of thecholinergic receptors XVII. 1,3-oxathiolane nucleus as a carrier of the active moeties / Maria, Pigini; Brasili, Livio; Mario, Giannella; Fulvio, Gualtieri. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 16:(1981), pp. 415-419.
Molecular requirements of the active sites of thecholinergic receptors XVII. 1,3-oxathiolane nucleus as a carrier of the active moeties
BRASILI, Livio;
1981
Abstract
In order to get infolmation on the molecular requirements of the cholinergic receptor, pure cis and, trans 2-methyl-5-dimethylaminomethyl-1,3-oxathiolane methiodide 2a-b and the corresponding sulfoxides 3a-b and sulfones 4a-b have synthesized and tested. Compound 2a was found to be very active, being 2 times more potent than muscarone and some 20 times more potent than Ach on Guinea Pig lleum, while 3a is equipotent with ACh on he same pràparation. The results of the pharmacological screening seem to suggest that 2a-b and 3a-d-interact with different subsite of the receptor.
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