444339-86-0Relevant academic research and scientific papers
2-Phenyl-3-(quinolizidin-1-yl)-5-substituted indoles as platelet antiaggregating agents
Ercoli, Marcella,Mina, Lorenzo,Boido, Caterina Canu,Boido, Vito,Sparatore, Fabio,Armani, Ugo,Piana, Antonietta
, p. 101 - 109 (2007/10/03)
A set of ten 2-phenyl-3-(quinolizidin-1-yl)-5-substituted indoles was prepared through the Fischer cyclization of lupinyl- and epi- lupinylphenylketone 4-substituted phenylhydrazones.Compounds were tested for antiaggregating activity on human platelets activated by adenosine diphosphate (ADP), collagen and adrenaline. At 2.5 × 10-4 M concentration most compounds strongly inhibited the aggregation induced by all the agonists considered and many of them still displayed good activity at 0.625 × 10-4 M concentration. The least active (1c) and one of the most active (1d) compounds were also tested for antiaggregating activity on rabbit platelets activated by ADP, PAF and sodium arachidonate. Both the compounds were active against ADP and PAF, but only 1d inhibited the arachidonate-induced aggregation (100% at 8 × 10-6 M concentration) and increased the bleeding time in mice. The same compounds were subjected to a general pharmacological screening and found to display several activities; of particular interest was the dose dependent reduction of serum cholesterol and heparin precipitating betalipoproteins in hypercholesterolemic mice exerted by 1c, which was still significant at the oral dose of 10 mg/kg.
Quinolizidine derivatives as ligands for sigma receptors
Sparatore, Anna,Novelli, Federica,Sparatore, Fabio
, p. 1 - 11 (2007/10/03)
A set of 1α/1β-[(4-R-phenyl)ethyl]quinolizidines was synthetized and together with selected intermediates was tested for affinity to sigma-1 receptor. Some compounds displayed good affinity for the relevant receptor, with Ki in the nanomolar range, and good selectivity versus σ2, 5-HT2A and D2 receptor subtypes.
