Evaluation of three quinoline-carboxamide derivatives as potential radioligands for the in vivo pet imaging of neurodegeneration
- S. Belloli, R. Moresco, F. Fazio
- Biology, ChemistryNeurochemistry International
- 1 May 2004
Aromatase and 5-alpha reductase gene expression: modulation by pain and morphine treatment in male rats
- A. Aloisi, I. Ceccarelli, A. Giordano
- Biology, MedicineMolecular Pain
- 1 January 2010
It appears that morphine administration can induce long-lasting genomic effects in different body areas which contribute to the strong central and peripheral testosterone levels.
Mapping and fitting the peripheral benzodiazepine receptor binding site by carboxamide derivatives. Comparison of different approaches to quantitative ligand-receptor interaction modeling.
- M. Anzini, A. Cappelli, J. Bourguignon
- Chemistry, BiologyJournal of Medicinal Chemistry
- 20 March 2001
The ligand-receptor complexes obtained provided a detailed description of the modalities of the interaction and interesting suggestions for further experiments and several computational methods were used to furnish descriptors of the isolated ligands able to rationalize the variation in the binding affinity of the enlarged series of compounds.
Synthesis and biological evaluation of amidine, guanidine, and thiourea derivatives of 2-amino(6-trifluoromethoxy)benzothiazole as neuroprotective agents potentially useful in brain diseases.
- M. Anzini, Alessia Chelini, S. Vomero
- Chemistry, BiologyJournal of Medicinal Chemistry
- 28 January 2010
A series of amidine, thiourea, and guanidine derivatives of 2-amino-6-(trifluoromethoxy)benzothiazole termed 2, 3, and 4, respectively, and structurally related to riluzole, a neuroprotective drug in…
Further studies on the interaction of the 5-hydroxytryptamine3 (5-HT3) receptor with arylpiperazine ligands. development of a new 5-HT3 receptor ligand showing potent acetylcholinesterase inhibitory…
- A. Cappelli, A. Gallelli, S. Vomero
- Biology, ChemistryJournal of Medicinal Chemistry
- 16 April 2005
The tacrine-related heterobivalent ligand 6o was designed in an attempt to capitalize on the evidence of a certain degree of conformational freedom of the amino acid residues interacting with the substituents in positions 3 and 4 of the quipazine quinoline nucleus, and represents the first example of a rationally designed high-affinity 5-HT(3) receptor ligand showing nanomolar AChE inhibitory activity.
Labeling and evaluation of N-[11C]methylated quinoline-2-carboxamides as potential radioligands for visualization of peripheral benzodiazepine receptors.
- M. Matarrese, R. Moresco, F. Fazio
- Chemistry, BiologyJournal of Medicinal Chemistry
- 16 January 2001
Inhibition studies in rats following intravenous pre-administration of 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide (PK 11195, 1) showed high specific binding to PBR of [11C]4, [11 c]5, and [11 C]6 in heart, lung, kidney, adrenal gland, spleen, and brain.
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
- A. Cappelli, M. Anzini, T. Langer
- Biology, ChemistryJournal of Medicinal Chemistry
- 5 February 1998
Qualitative and quantitative structure-affinity relationship studies carried out by making use of theoretical molecular descriptors allowed to elucidate the role of the main pharmacophoric components and to develop a model for the interaction of the 5-HT3 ligands related to quipazine with their receptor.
New insight into the central benzodiazepine receptor-ligand interactions: design, synthesis, biological evaluation, and molecular modeling of 3-substituted…
- M. Anzini, S. Valenti, G. Biggio
- Biology, ChemistryJournal of Medicinal Chemistry
- 25 August 2011
3-Substituted 6-phenyl-4H-imidazo[1,5-a][1,4]benzodiazepines and related compounds were synthesized as central benzodiazepine receptor (CBR) ligands. Most of the compounds showed high affinity for…
Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity.
- M. Anzini, L. Canullo, N. Galeotti
- Biology, ChemistryJournal of Medicinal Chemistry
- 6 August 2003
The synthesis and biological evaluation of a series of new derivatives of 2-substituted 5-phenyl-1,4-benzodiazepines, structurally related to tifluadom, and the interaction with the homology model of the human kappa-opioid receptor, built on the recently solved crystal structure of rhodopsin are reported.
PEG-benzofulvene copolymer hydrogels for antibody delivery.
- M. Licciardi, M. Grassi, G. Giammona
- Biology, Materials ScienceInternational journal of pharmaceutics
- 10 May 2010
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