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A series of bivalent ligands (2-8) derived from 2,2-diphenyl-[1,3]-dioxolan-4-ylmethyl-dimethylamine methiodide 1 has been synthesized and tested to evaluate affinity and selectivity for M1, M2 and M3 muscarinic receptor subtypes. In order to study the contribution of the spacer and of a second cationic head to the binding process, unsymmetrical ligands (9,10) have also been prepared. The results, expressed in terms of pA2 values, show that, although the spacer negatively affects the interaction of the bivalent ligands with the three receptor subtypes, affinity and selectivity are modulated by its length; this indicates that the pharmacophore binding sites are organized differently with respect to their mutual proximity and orientation, in each receptor subtype.
A Piergentili, and
W Quaglia, and
S K Tayebati, and
F Paparelli, and
L Malmusi, and
L Brasili
March 1977,
British journal of pharmacology,
A Piergentili, and
W Quaglia, and
S K Tayebati, and
F Paparelli, and
L Malmusi, and
L Brasili
May 2011,
Bioorganic & medicinal chemistry,
A Piergentili, and
W Quaglia, and
S K Tayebati, and
F Paparelli, and
L Malmusi, and
L Brasili
May 1993,
Biochemical pharmacology,
A Piergentili, and
W Quaglia, and
S K Tayebati, and
F Paparelli, and
L Malmusi, and
L Brasili
September 1986,
Journal of medicinal chemistry,
A Piergentili, and
W Quaglia, and
S K Tayebati, and
F Paparelli, and
L Malmusi, and
L Brasili
July 2003,
The Journal of organic chemistry,
A Piergentili, and
W Quaglia, and
S K Tayebati, and
F Paparelli, and
L Malmusi, and
L Brasili
January 1982,
Proceedings of the National Academy of Sciences of the United States of America,
A Piergentili, and
W Quaglia, and
S K Tayebati, and
F Paparelli, and
L Malmusi, and
L Brasili
April 2013,
Bioorganic & medicinal chemistry letters,
A Piergentili, and
W Quaglia, and
S K Tayebati, and
F Paparelli, and
L Malmusi, and
L Brasili
October 2011,
Bioorganic & medicinal chemistry,
A Piergentili, and
W Quaglia, and
S K Tayebati, and
F Paparelli, and
L Malmusi, and
L Brasili
March 1993,
Farmaco (Societa chimica italiana : 1989),
A Piergentili, and
W Quaglia, and
S K Tayebati, and
F Paparelli, and
L Malmusi, and
L Brasili
July 1996,
Chemistry & biology,
