- Analgesic, antimuscarinic activity and enantioselectivity of the four isomers of 3-quinuclidinyl tropate as compared with the enantiomers of hyoscyamine
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The four stereoisomers of 3-quinuclidinyl tropate (2) were synthesized and their absolute configuration established. The analgesic activity of the four isomers on the hot-plate test and their muscarinic antagonism on rabbit vas deferens (M1), g
- Dei,Bellucci,Gualtieri,Romanelli,Scapecchi,Teodori,Bartolini,Ghelardini
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p. 303 - 309
(2007/10/02)
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- Parasympatholytic (Anticholinergic) Esters of the Isomeric 2-Tropanols. 2. Non-Glycolates
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The 19 esters in Table I were prepared from (+)-2α-tropanol, (-)-2β-tropanol, (+/-)-3-quinuclidinol, and a variety of non-glycolic acids in order to compare their central and pheripheral activities with those of the glycolates reported in the previous paper.The results (Table II) showed that esters 6 and 17 were approximately equivalent to one another and the atropine, that 8 was equal in both central and peripheral activity to reference glycolates, that 9 and 19 were less active than 8 but 9 had a substantially reduced central activity, and that 10 and 11 weremore active than the methoxy analogue reported earlier.
- Atkinson, Edward R.,McRitchie-Ticknor, Donna D.,Harris, Louis S.,Archer, Sydney,Aceto, Mario D.,et al.
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p. 1772 - 1775
(2007/10/02)
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