1,3-OXATHIOLANE MUSCARINIC LIGANDS MODIFIED AT THE CATIONIC HEAD

Citation
E. Teodori et al., 1,3-OXATHIOLANE MUSCARINIC LIGANDS MODIFIED AT THE CATIONIC HEAD, Il Farmaco, 49(5), 1994, pp. 305-312
Citations number
20
Categorie Soggetti
Pharmacology & Pharmacy
Journal title
ISSN journal
0014827X
Volume
49
Issue
5
Year of publication
1994
Pages
305 - 312
Database
ISI
SICI code
0014-827X(1994)49:5<305:1MLMAT>2.0.ZU;2-8
Abstract
In order to develop compounds which may be useful in the treatment of memory and cognitive disorders we have synthesized and tested some 1,3 -oxathiolane derivatives bearing an amidine function instead of the cl assical ammonium head, with the aim of improving brain penetration. Th e compounds were tested on peripheral and central models of muscarinic receptors. The results show that, unlike for other series of muscarin ic ligands, this modification results in the reduced potency of antago nists, shifts the activity of agonists toward weak antagonism and does not introduce any noteworthy subtype selectivity.