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The results of a pharmacological investigation on a series of 3-substituted benzyltrimethylammonium salts possessing muscarinic activity are reported. Correlative analysis shows that the pharmacodynamic activity is a function of the hydrophobic-lipophilic and steric parameters associated with the substituents. In particular, it is revealed that a lipophilic(More)
A series of chiral PAF agonists were synthesized. Modifications at the PAF structure were undertaken as far as the C2 substituents and the onium head groups are concerned. In parallel, molecular modelling studies including a MOPAC geometry optimization and the analysis of the electrostatic potential were performed on the newly synthesized and on already(More)
Two sets of substantial picolyl and furfuryltrimethylammonium salts have been synthesized and their affinities (expressed as pD2) have been studied with the aim of characterizing muscarinic receptor spaces to which the ligand structural features bind. The new data were combined with those relative to a set of substituted benzyltrimethylammonium salts(More)
The optical isomers of the well known alpha 1-antagonist WB4101 and of its derivatives with a methyl group in the oxyethyl moiety were prepared for the evaluation of their alpha-adrenoceptors binding affinity. By means of a detailed computational analysis, the present work shows that the introduction of a methyl group affects the behaviour of WB4101 in(More)
Stereoselective synthesis and biological properties of PAF-acether, its enantiomer and some analogues of both are reported. The results clearly indicate that the ONIUM SIZE and SHAPE of the various compounds tested are important in determining guinea-pig bronchoconstriction and human platelet aggregation.