G. Cignarella et al., SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF A NEW CLASS OF 2-OXO-8-AZASPIRO (4,5)DECAN-1-ONES AS ANALOGS OF THE MUSCARINIC AGONIST RS-86, Il Farmaco, 48(10), 1993, pp. 1439-1445
A new series of 8-substituted-2-oxo-8-azapsiro (4,5)decan-1-ones has b
een synthesized and compounds tested for their cholinergic properties
in comparison with the muscarinic agonist RS-86. Preliminary in vitro
and in vivo pharmacological data indicate that none of them is provide
d with significant cholinergic effects either at central or peripheral
level. A possible explanation for the lack of activity is given on th
e basis of conformational studies.