Premium
Reduced Flexibility Analogs of Analgesic and Cognition Enhancing α‐Tropanyl Esters
Author(s) -
Manetti Dina,
Romanelli Maria Novella,
Bartolini Alessandro,
Dei Silvia,
Ghelardini Carla,
Gualtieri Fulvio,
Matucci Rosanna,
Scapecchi Serena,
Teodori Elisabetta
Publication year - 1996
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19963290208
Subject(s) - analgesic , chemistry , muscarinic acetylcholine receptor , antagonist , nociception , pharmacology , muscarinic acetylcholine receptor m1 , receptor , stereochemistry , biochemistry , medicine
A series of semirigid analogs of compounds 1 and 2 , two potent analgesics and cognition enhancers, have been synthesized and tested for antinociceptive activity (hot plate test) and for muscarinic affinity (binding in rat cerebral cortex). They were found to be in general less potent than the reference compounds; only one of them ( 22 ) shows a good affinity for the muscarinic receptor and an antinociceptive efficacy comparable with those of the reference compounds. At a dose of 30 mg/kg 22 is also able to reverse the amnesic effect of dicyclomine. Since the analgesic effect of these compounds is affected by the 5‐HT 4 antagonist SDZ 205557, the possible role of this receptor is discussed.