86762-37-0Relevant academic research and scientific papers
Differential analgesic activity of the enantiomers of atropine derivatives does not correlate with their muscarinic subtype selectivity
Dei,Bartolini,Bellucci,Ghelardini,Gualtieri,Manetti,Romanelli,Scapecchi,Teodori
, p. 595 - 605 (2007/10/03)
The enantiomers of several tropic and p-substituted tropic acid esters related to atropine obtained by esterification under non-racemizing conditions after resolution of the corresponding racemic acids [(+)- and (-)-18, (+)- and (-)-19] are reported. They were tested in vitro on muscarinic subtype receptors and in vivo for their analgesic activity on mice. As in the case of the lead compound, R-(+)-hyoscyamine, these substances show enantioselectivity in analgesic tests, the eutomers being the R-(+) or R-(+)-p-substituted tropic acid derivatives. However, this property, which is a consequence of increased central release of ACh, seems unrelated to muscarinic subtype selectivity insofar as the compounds are unable to discriminate muscarinic subtype receptors. A possible explanation of these results which does not involve subtype selectivity is proposed, based on the recently developed concept of inverse agonism.
ESTERS OF 1-p-CHLOROBENZOYL-5-METHOXY-2-METHYL-3-INDOLYLACETIC ACID
Fisnerova, Ludmila,Rabek, Vlastimil,Nemecek, Oldrich
, p. 901 - 905 (2007/10/02)
Reactions of imidazolide of 1-p-chlorobenzoyl-5-methoxy-2-methyl-3-indolylacetic acid, prepared from the acid and N,N'-carbonyldiimidazole, with the optically active forms of 2-phenyl-3-hydroxypropane acid and with the inactive forms of p-chloro-, p-isopropyl- and p-isobutyl-2-phenyl-3-hydroxypropane acids gave the corresponding esters.The compounds were tested for antiinflammatory activity.
