C Martini

Summary

Affiliation: University of Pisa
Country: Italy

Publications

  1. ncbi Regulation of A2B adenosine receptor functioning by tumour necrosis factor a in human astroglial cells
    Maria L Trincavelli
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Pisa, Italy
    J Neurochem 91:1180-90. 2004
  2. ncbi A2B adenosine receptor activity is reduced in neutrophils from patients with systemic sclerosis
    Laura Bazzichi
    Department of Internal Medicine, Division of Rheumatology, University of Pisa, Pisa, Italy
    Arthritis Res Ther 7:R189-95. 2005
  3. ncbi Upregulation of A2A adenosine receptors in platelets from patients affected by bipolar disorders under treatment with typical antipsychotics
    Claudia Martini
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Psychiatr Res 40:81-8. 2006
  4. ncbi Chemical modifications of striatal A2A adenosine receptors: a possible role for tyrosine at the ligand binding sites
    C Martini
    Istituto Policattedra di Discipline Biologiche, Universita di Pisa, Italy
    Biochim Biophys Acta 1326:67-74. 1997
  5. ncbi Serotonin-mediated phosphorylation of extracellular regulated kinases in platelets of patients with panic disorder versus controls
    Claudia Martini
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Neurochem Int 44:627-39. 2004
  6. ncbi A(2A) adenosine receptor binding parameters in platelets from patients affected by pathological gambling
    Claudia Martini
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Pisa, Italy
    Neuropsychobiology 63:154-9. 2011
  7. ncbi Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular modeling analysis of the structure-activity relationships
    G Primofiore
    Dipartimento di Scienze Farmaceutiche and Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 44:2286-97. 2001
  8. ncbi Regulation of A1 adenosine receptor functioning induced by P2Y1 purinergic receptor activation in human astroglial cells
    I Tonazzini
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Pisa, Italy
    J Neurosci Res 86:2857-66. 2008
  9. ncbi Peripheral-type benzodiazepine receptor ligands: mitochondrial permeability transition induction in rat cardiac tissue
    B Chelli
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, , Via Bonanno 6, I-56126, Pisa, Italy
    Biochem Pharmacol 61:695-705. 2001
  10. ncbi Norepinephrine-mediated regulation of 5HT1 receptor functioning in human platelets
    M L Trincavelli
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Neurochem Res 33:1292-300. 2008

Detail Information

Publications96

  1. ncbi Regulation of A2B adenosine receptor functioning by tumour necrosis factor a in human astroglial cells
    Maria L Trincavelli
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Pisa, Italy
    J Neurochem 91:1180-90. 2004
    ....
  2. ncbi A2B adenosine receptor activity is reduced in neutrophils from patients with systemic sclerosis
    Laura Bazzichi
    Department of Internal Medicine, Division of Rheumatology, University of Pisa, Pisa, Italy
    Arthritis Res Ther 7:R189-95. 2005
    ..Moreover, a decrease in A2B AR mediated adenylyl cyclase activity was observed in patients with SSc. Our findings demonstrate the occurrence of selective alterations in A2B AR density and signalling in SSc...
  3. ncbi Upregulation of A2A adenosine receptors in platelets from patients affected by bipolar disorders under treatment with typical antipsychotics
    Claudia Martini
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Psychiatr Res 40:81-8. 2006
    ....
  4. ncbi Chemical modifications of striatal A2A adenosine receptors: a possible role for tyrosine at the ligand binding sites
    C Martini
    Istituto Policattedra di Discipline Biologiche, Universita di Pisa, Italy
    Biochim Biophys Acta 1326:67-74. 1997
    ....
  5. ncbi Serotonin-mediated phosphorylation of extracellular regulated kinases in platelets of patients with panic disorder versus controls
    Claudia Martini
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Neurochem Int 44:627-39. 2004
    ....
  6. ncbi A(2A) adenosine receptor binding parameters in platelets from patients affected by pathological gambling
    Claudia Martini
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Pisa, Italy
    Neuropsychobiology 63:154-9. 2011
    ....
  7. ncbi Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular modeling analysis of the structure-activity relationships
    G Primofiore
    Dipartimento di Scienze Farmaceutiche and Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 44:2286-97. 2001
    ..The GABA ratios close to unity exhibited by all the tested compounds on each BzR subtype were predictive of an efficacy profile typical of antagonists...
  8. ncbi Regulation of A1 adenosine receptor functioning induced by P2Y1 purinergic receptor activation in human astroglial cells
    I Tonazzini
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Pisa, Italy
    J Neurosci Res 86:2857-66. 2008
    ....
  9. ncbi Peripheral-type benzodiazepine receptor ligands: mitochondrial permeability transition induction in rat cardiac tissue
    B Chelli
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, , Via Bonanno 6, I-56126, Pisa, Italy
    Biochem Pharmacol 61:695-705. 2001
    ....
  10. ncbi Norepinephrine-mediated regulation of 5HT1 receptor functioning in human platelets
    M L Trincavelli
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Neurochem Res 33:1292-300. 2008
    ..These results suggest that high NE levels (released i.e. during stress disorders) may play an important role in regulating the 5HT1 responsiveness and in controlling effectiveness of drugs acting on these neurotransmitter systems...
  11. ncbi Translocator protein ligands as promising therapeutic tools for anxiety disorders
    S Taliani
    Department of Pharmaceutical Science, University of Pisa, Italy
    Curr Med Chem 16:3359-80. 2009
    ....
  12. ncbi 3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists
    F Da Settimo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Italy
    J Med Chem 44:316-27. 2001
    ....
  13. ncbi N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor
    Giampaolo Primofiore
    Dipartimento di Scienze Farmaceutiche, , Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 47:1852-5. 2004
    ..The most potent ligands (4-7, 9, 13-27) stimulated steroid biosynthesis in rat C6 glioma cells with a potency similar to or higher than that of classical ligands. The SARs of this new class of compounds are discussed...
  14. ncbi Role of translocator protein (18 kDa) in adult separation anxiety and attachment style in patients with depression
    B Costa
    Department of Human Morphology and Applied Biology, University of Pisa, Via Volta, 4 56126 Pisa, Italy
    Curr Mol Med 12:483-7. 2012
    ..A further aim was to confirm the genetic association of Ala147Thr SNP with ASAD in an extended case-control sample and to investigate whether this SNP was related to an anxious attachment style that is thought to be connected to ASAD...
  15. ncbi Modulation of PAR(1) signalling by benzimidazole compounds
    S Asteriti
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Italy
    Br J Pharmacol 167:80-94. 2012
    ..Q109 presents a modest variation from Q94 in the substituent group at the 2-position, while Q89 has quite different groups at the 1- and 2-positions...
  16. ncbi 7-Nitrobenzofurazan (NBD) derivatives of 5'-N-ethylcarboxamidoadenosine (NECA) as new fluorescent probes for human A(3) adenosine receptors
    M Macchia
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Bioorg Med Chem Lett 11:3023-6. 2001
    ....
  17. ncbi Agonist-induced desensitization/resensitization of human G protein-coupled receptor 17: a functional cross-talk between purinergic and cysteinyl-leukotriene ligands
    S Daniele
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Pharmacol Exp Ther 338:559-67. 2011
    ....
  18. ncbi Novel, highly potent adenosine deaminase inhibitors containing the pyrazolo[3,4-d]pyrimidine ring system. Synthesis, structure-activity relationships, and molecular modeling studies
    Federico Da Settimo
    Dipartimento di Scienze Farmaceutiche, , Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 48:5162-74. 2005
    ..14 nM), which was taken as the reference standard. Docking simulations of aminopyrazolopyrimidines into the ADA binding site were also performed, to rationalize the structure-activity relationships of this class of inhibitors...
  19. ncbi Design, synthesis and biological evaluation of novel N-alkyl- and N-acyl-(7-substituted-2-phenylimidazo[1,2-a][1,3,5]triazin-4-yl)amines (ITAs) as novel A(1) adenosine receptor antagonists
    Ettore Novellino
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Universita di Pisa, Via Bonanno 6, Italy
    J Med Chem 45:5030-6. 2002
    ....
  20. ncbi Refinement of the benzodiazepine receptor site topology by structure-activity relationships of new N-(heteroarylmethyl)indol-3-ylglyoxylamides
    Giampaolo Primofiore
    Dipartimento di Scienze Farmaceutiche, , Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 49:2489-95. 2006
    ..On the basis of published mutagenesis studies and the present SARs, we speculate that the S(1) HBA/D group might be identified as the hydroxyl of alpha(1)-Tyr209 or of other neighboring amino acids...
  21. ncbi Anxiolytic-like effects of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides by modulation of translocator protein promoting neurosteroid biosynthesis
    Federico Da Settimo
    Dipartimento di Scienze Farmaceutiche and Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 51:5798-806. 2008
    ..The results of this study suggested that the novel N,N-disubstituted indol-3-ylglyoxylamides may represent a promising class of compounds potentially suited for the treatment of anxiety disorders...
  22. ncbi Novel N2-substituted pyrazolo[3,4-d]pyrimidine adenosine A3 receptor antagonists: inhibition of A3-mediated human glioblastoma cell proliferation
    Sabrina Taliani
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Pisa, Italy
    J Med Chem 53:3954-63. 2010
    ..Furthermore, the antiproliferative activity of the new compounds was demonstrated to be mediated by the block of A(3) AR agonist activation of intracellular kinases ERK 1/2...
  23. ncbi 5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists
    Federico Da Settimo
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 50:5676-84. 2007
    ..Docking simulations on selected ligands into a model of the A3 AR allowed us to rationalize the structure-activity relationships of phenyltriazolobenzotriazindiones VIII and aminophenyltriazolobenzotriazinones IX at the molecular level...
  24. ncbi A3 adenosine receptors in human astrocytoma cells: agonist-mediated desensitization, internalization, and down-regulation
    M L Trincavelli
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Università Pisa, Pisa, Italy
    Mol Pharmacol 62:1373-84. 2002
    ..In conclusion, our results demonstrated that A(3) receptors, in astrocytoma cells, are regulated after short- and long-term agonist exposure...
  25. ncbi A(1) adenosine receptors in human neutrophils: direct binding and electron microscope visualization
    A Falleni
    Dipartimento di Morfologia Umana e Biologia Applicata, Universita di Pisa, Pisa, Italy
    J Cell Biochem 75:235-44. 1999
    ..These data suggest that the CHA-biotin XX-streptavidin-gold complex is a useful marker for the specific labelling of A(1) binding sites and to follow the intracellular trafficking of these receptors...
  26. ncbi Adenosine receptors: what we know and what we are learning
    M L Trincavelli
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno 6, Pisa, Italy
    Curr Top Med Chem 10:860-77. 2010
    ..In addition, to dissect the potential therapeutic application of adenosine receptor ligands, the pathophysiological role of the receptor subtypes in different tissues are discussed...
  27. ncbi Fluorescent probes for adenosine receptors: synthesis and biology of N6-dansylaminoalkyl-substituted NECA derivatives
    M Macchia
    GlaxoWellcome Medicines Research Center, Verona, Italy
    Bioorg Med Chem Lett 8:3223-8. 1998
    ....
  28. ncbi Spirotetrahydronaphthalene analogues of sympathomimetic catecholamines. Synthesis and adrenergic activity of 5,6- and 6,7-dihydroxy-3,4-dihydrospiro[naphthalen-1 (2H)-3'-piperidines]
    Bruno Macchia
    Dipartimento di Scienze Farmaceutiche, Facolta di Farmacia, Universita di Pisa, Italy
    J Pharm Pharmacol 54:649-60. 2002
    ..Comparison of the affinity and activity data of novel derivatives with those of reference compounds 2, 3 and 4 shows a general low ability of DDSNPs 5 and 6 to interact with both alpha and beta- adrenoceptors...
  29. ncbi Synthesis and benzodiazepine receptor affinity of derivatives of the new tricyclic heteroaromatic system pyrido[3',2':5,6]thiopyrano[4,3-c]pyridazin-3(2H,5H)-one
    Giampaolo Primofiore
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Pisa, Italy
    Arch Pharm (Weinheim) 338:126-32. 2005
    ..A hypothesis is presented to rationalize these results...
  30. ncbi Geometrically constrained analogues of N-benzylindolylglyoxylylamides: [1, 2, 4]triazino[4, 3-a]benzimidazol-4(10H)-one derivatives as potential new ligands at the benzodiazepine receptor
    Giampaolo Primofiore
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Pisa, Italy
    Arch Pharm (Weinheim) 336:413-21. 2003
    ..Attempts were made to rationalize these results taking into account the possible tautomeric equilibria involving these ligands...
  31. ncbi Plasma and serum brain-derived neurotrophic factor (BDNF) in depressed patients during 1 year of antidepressant treatments
    Armando Piccinni
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, University of Pisa, Pisa, Italy
    J Affect Disord 105:279-83. 2008
    ..The aim of this study was to assess the possible relationships between depressive symptoms and serum and/or plasma BDNF levels during 1 year of antidepressant treatment...
  32. ncbi Reductions in platelet 18-kDa translocator protein density are associated with adult separation anxiety in patients with bipolar disorder
    Marianna Abelli
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Pisa, Italy
    Neuropsychobiology 62:98-103. 2010
    ..The aim of this study was to explore whether adult separation anxiety might be a factor differentiating TSPO expression in a sample of patients with bipolar disorder...
  33. ncbi Short-term effects of 3,4-methylen-dioxy-metamphetamine (MDMA) on 5-HT(1A) receptors in the rat hippocampus
    Gino Giannaccini
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno 6, Pisa 56126, Italy
    Neurochem Int 51:496-506. 2007
    ..Therefore, our results encourage at extending the study of MDMA biochemical profiles, in the attempt to elucidate those amphetamine-induced pathways with a potential for neurotoxicity or psycho-stimulant activity...
  34. ncbi Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands
    Giampaolo Primofiore
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 50:1627-34. 2007
    ....
  35. ncbi Novel irreversible fluorescent probes targeting the 18 kDa translocator protein: synthesis and biological characterization
    Sabrina Taliani
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Pisa, Italy
    J Med Chem 53:4085-93. 2010
    ..Further biological characterization of the fluorescent irreversible TSPO probe 18 was carried out by using fluorescent spectroscopy in human glioma cells...
  36. ncbi New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation
    Sabrina Taliani
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 50:404-7. 2007
    ..Results from fluorescence microscopy showed that these probes specifically labeled the PBR at the mitochondrial level in C6 glioma cells...
  37. ncbi 4-[6-(Dansylamino)hexylamino]-7-methyl-2-phenyl-1,8-naphthyridine as a new potential fluorescent probe for studying A1-adenosine receptor
    Marco Macchia
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Italy
    Farmaco 57:783-6. 2002
    ....
  38. ncbi A virtual screening study of the 18 kDa translocator protein using pharmacophore models combined with 3D-QSAR studies
    Tiziano Tuccinardi
    Dipartimento di Scienze Farmaceutiche, Università di Pisa via Bonanno 6, 56126 Pisa Italy
    ChemMedChem 4:1686-94. 2009
    ..These results validated our applied methodologies, and the two compounds with sub-micromolar affinity could be used as interesting leads for the development of new active TSPO ligands...
  39. ncbi High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives
    Giampaolo Primofiore
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 48:2936-43. 2005
    ..Moreover, compounds 45 and 49 were found to display a full agonist efficacy profile at alpha1 and alpha2 receptor subtypes, and an antagonist efficacy at alpha5-containing receptors...
  40. ncbi Translocator protein (TSPO) and neurosteroids: implications in psychiatric disorders
    E Da Pozzo
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno, 6 56126 Pisa, Italy
    Curr Mol Med 12:426-42. 2012
    ..The focus of this review is to illustrate the currently available literature regarding the role of TSPO in psychiatric disorders...
  41. ncbi Inhibition of metalloproteinases derived from tumours: new insights in the treatment of human glioblastoma
    P Gabelloni
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno, 6 56126 Pisa, Italy
    Neuroscience 168:514-22. 2010
    ....
  42. ncbi GABA A/Bz receptor subtypes as targets for selective drugs
    F Da Settimo
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Curr Med Chem 14:2680-701. 2007
    ..The status of BzR ligands, subdivided on the basis of their main chemical structural features, is reviewed in relation to structure-activity relationships which determine their affinity or efficacy selectivity for a certain BzR subtype...
  43. ncbi Regulation of A(2A) adenosine receptor expression and functioning following permanent focal ischemia in rat brain
    Maria L Trincavelli
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Pisa, Italy
    J Neurochem 104:479-90. 2008
    ..Modifications of ARs may play a significant role in determining adenosine effects during ischemia and therefore should be taken into account when evaluating time-dependent protective effects of specific A(2A) active compounds...
  44. ncbi Short-term TNF-Alpha treatment induced A2B adenosine receptor desensitization in human astroglial cells
    Maria Letizia Trincavelli
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Pisa, Italy
    J Cell Biochem 104:150-61. 2008
    ....
  45. ncbi Platelet 18 kDa Translocator Protein density is reduced in depressed patients with adult separation anxiety
    Beatrice Chelli
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno 6, 56100 Pisa, Italy
    Eur Neuropsychopharmacol 18:249-54. 2008
    ....
  46. ncbi TSPO over-expression increases motility, transmigration and proliferation properties of C6 rat glioma cells
    Mariarosa Rechichi
    Dipartimento di Morfologia Umana e Biologia Applicata, University of Pisa, Via Volta 4, Pisa, Italy
    Biochim Biophys Acta 1782:118-25. 2008
    ..These findings suggest that the use of TSPO ligands as chemotherapeutic agents could be effective on aggressive tumor cells with a high TSPO expression level...
  47. ncbi Serotonin-mediated cyclic AMP inhibitory pathway in platelets of patients affected by panic disorder
    Claudia Carmassi
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Pisa, Italy
    Neuropsychobiology 50:28-36. 2004
    ....
  48. ncbi Substituted pyrazolo[3,4-b]pyridines as potent A1 adenosine antagonists: synthesis, biological evaluation, and development of an A1 bovine receptor model
    Tiziano Tuccinardi
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    ChemMedChem 3:898-913. 2008
    ..Analysis of the bovine/human A(1)AR affinity profile of ligands supported the hypothesis that such receptors should be characterized by a different size of their binding site, responsible for the different affinity of the antagonists...
  49. ncbi Lifetime manic-hypomanic symptoms in post-traumatic stress disorder: relationship with the 18 kDa mitochondrial translocator protein density
    Liliana Dell'Osso
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnologies, Pisa University, Pisa, Italy
    Psychiatry Res 177:139-43. 2010
    ....
  50. ncbi Identification of anxiolytic/nonsedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the gamma-aminobutyric acid-A (GABAA) alpha2 benzodiazepine receptor
    Sabrina Taliani
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    J Med Chem 52:3723-34. 2009
    ....
  51. ncbi Peripheral benzodiazepine receptor: characterization in human T-lymphoma Jurkat cells
    Barbara Costa
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno, 6 56126 Pisa, Italy
    Mol Pharmacol 69:37-44. 2006
    ....
  52. ncbi Peripheral benzodiazepine binding sites in platelets of patients affected by mitochondrial diseases and large scale mitochondrial DNA rearrangements
    Claudia Martini
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Italy
    Mol Med 8:841-6. 2002
    ..06 nM versus 5.63 +/- 0.46 nM, p< 0.05). CONCLUSIONS: These data suggest that the kinetic binding parameters of PBR are altered in MD and that the observed changes might be related to the mitochondrial dysfunction associated with MD...
  53. ncbi PIGA (N,N-Di-n-butyl-5-chloro-2-(4-chlorophenyl)indol-3-ylglyoxylamide), a new mitochondrial benzodiazepine-receptor ligand, induces apoptosis in C6 glioma cells
    Beatrice Chelli
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Chembiochem 6:1082-8. 2005
    ....
  54. ncbi Up-regulation of A(2A) adenosine receptors by proinflammatory cytokines in rat PC12 cells
    Maria L Trincavelli
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, Universita di Pisa, Via Bonanno 6, Italy
    Biochem Pharmacol 64:625-31. 2002
    ..The biological significance of this regulation might be associated with modulating cellular activity in response to tissue damage associated with inflammatory mediator production...
  55. ncbi Involvement of mitogen protein kinase cascade in agonist-mediated human A(3) adenosine receptor regulation
    M Letizia Trincavelli
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, , Via Bonanno 6, 56126 Pisa, Italy
    Biochim Biophys Acta 1591:55-62. 2002
    ..These results suggested that the MAPK cascade is involved in A(3) AR regulation by a feedback mechanism which controls GRK(2) activity and probably involves a direct receptor phosphorylation...
  56. ncbi Characterization of a cloned xenopus laevis serotonin 5-HT1A receptor expressed in the NIH-3T3 cell line
    C Cappellini
    Laboratori di Biologia Cellulare e dello Sviluppo, Dipartimento di Fisiologia e Biochimica, Universita di Pisa, Via Carducci 13, 56010 Ghezzano, Pisa, Italy
    Brain Res Mol Brain Res 63:380-3. 1999
    ..The effects of X5-HT1A receptor activation on cell growth were also investigated in stably transfected NIH-3T3 cells. The 5-HT1A agonist 8-OH-DPAT was found to increase DNA synthesis and accelerated cell growth...
  57. ncbi Peripheral benzodiazepine receptors in isolated human pancreatic islets
    L Giusti
    Istituto Policattedra di Discipline Biologiche, Universita di Pisa, Italy
    J Cell Biochem 64:273-7. 1997
    ..3 mM glucose. These results show the presence of peripheral benzodiazepine receptors in purified human pancreatic islets and suggest their role in the mechanisms of insulin release...
  58. ncbi Co-localization and functional cross-talk between A1 and P2Y1 purine receptors in rat hippocampus
    I Tonazzini
    Department of Psychiatry Neurobiology Pharmacology and Biotechnology, University of Pisa, 56126, Pisa, Italy
    Eur J Neurosci 26:890-902. 2007
    ..This may be particularly important during pathological conditions, when large amounts of these mediators are released...
  59. ncbi Upregulation of mitochondrial peripheral benzodiazepine receptor expression by cytokine-induced damage of human pancreatic islets
    M Letizia Trincavelli
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, , Via Bonnanno 6, 56126 Pisa, Italy
    J Cell Biochem 84:636-44. 2002
    ..These results suggest a possible role of peripheral benzodiazepine receptors in the organism response to tissue damage associated with inflammatory mediator production...
  60. ncbi PK 11195 differentially affects cell survival in human wild-type and 18 kDa translocator protein-silenced ADF astrocytoma cells
    Beatrice Chelli
    Department of Psychiatry, Pharmacology, Neurobiology and Biotechnology, University of Pisa, Pisa, Italy
    J Cell Biochem 105:712-23. 2008
    ..These results encourage the development of specific-cell strategies for the treatment of gliomas, in which TSPO is highly expressed respect to normal cells...
  61. ncbi Peripheral benzodiazepine receptor ligands: mitochondrial transmembrane potential depolarization and apoptosis induction in rat C6 glioma cells
    Beatrice Chelli
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Pisa, Italy
    Biochem Pharmacol 68:125-34. 2004
    ..Moreover, PK 11195 and Ro5-4864 induced a decrease of DeltaPsi(m), as evidenced by JC-1 flow cytometry analysis. Our data demonstrate the pro-apoptotic effects of specific PBR ligands on rat C6 glioma cells...
  62. ncbi The spontaneous Ala147Thr amino acid substitution within the translocator protein influences pregnenolone production in lymphomonocytes of healthy individuals
    Barbara Costa
    Department of Human Morphology and Applied Biology, University of Pisa, 4 56126 Pisa, Italy
    Endocrinology 150:5438-45. 2009
    ....
  63. ncbi Oxytocin receptor polymorphisms and adult attachment style in patients with depression
    Barbara Costa
    Department of Human Morphology and Applied Biology, University of Pisa, Via Volta, 4 56126 Pisa, Italy
    Psychoneuroendocrinology 34:1506-14. 2009
    ..These findings support the involvement of the oxytocinergic system in the mechanisms that underlie depression and specific adult attachment styles...
  64. ncbi A(2A) adenosine receptor ligands and proinflammatory cytokines induce PC 12 cell death through apoptosis
    Maria L Trincavelli
    Dipartimento di Psichiatria, Neurobiologia, Farmacologia e Biotecnologie, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Biochem Pharmacol 66:1953-62. 2003
    ....
  65. ncbi The role of newer antiglutamatergic agents as mood-stabilizers in bipolar disorder
    Marianna Abelli
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnologies, University of Pisa, Pisa, Italy
    Curr Drug Targets 6:607-14. 2005
    ..These agents have widely varying mechanisms of action. Some of these medications focus on the current understanding of antiglutamatergic mechanisms of action and their treatment implications for bipolar disorders...
  66. ncbi Regulation of PC12 cell survival and differentiation by the new P2Y-like receptor GPR17
    Simona Daniele
    Department of Psychiatry, Neurobiology, Pharmacology and Biotechnology, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Cell Signal 22:697-706. 2010
    ..They also represent the first direct demonstration, in a native system, that GPR17 can indeed be activated by uracil nucleotides and cysLTs, in line with what previously demonstrated in recombinant expression systems...
  67. ncbi Ribose-modified nucleosides as ligands for adenosine receptors: synthesis, conformational analysis, and biological evaluation of 1'-C-methyl adenosine analogues
    Loredana Cappellacci
    Dipartimento di Scienze Chimiche, , 62032 Camerino, Italy
    J Med Chem 45:1196-202. 2002
    ....
  68. ncbi Synthesis and benzodiazepine receptor binding activity of 2, 9-disubstituted quinolino[2', 3'-5, 4](3-pyrazolino)[3, 2-b]purin-4-ones
    Ola A El-Sayed
    Pharmaceutical Chemistry Department, Faculty of Pharmacy, University of Alexandria, Egypt
    Arch Pharm (Weinheim) 335:207-12. 2002
    ..Compound 5c caused 83 +/- 8 %inhibition in [(3)H]R015-1788 specific benzodiazepine receptor binding followed by compounds 5f, 5h, and 5i while other analogs were inactive at 10 microM concentration...
  69. ncbi Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists
    Loredana Cappellacci
    Dipartimento di Scienze Chimiche, , 62032 Camerino, Italy
    J Med Chem 48:1550-62. 2005
    ....
  70. ncbi Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists
    Barbara Cosimelli
    Departimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, via D Montesano 49, Naples, Italy
    J Med Chem 51:1764-70. 2008
    ..This compound binds to the A 3 AR with a K i of 3.5 nM and is devoid of appreciable affinity for the A 1, A 2A, and A 2B ARs...
  71. ncbi Synthesis, molecular modeling studies, and pharmacological activity of selective A(1) receptor antagonists
    Francesco Bondavalli
    Dipartimento di Scienze Farmaceutiche, , Viale Benedetto XV n.3, I-16132 Genova, Italy
    J Med Chem 45:4875-87. 2002
    ..All of the new compounds were tested for their affinity toward A(1), A(2a), and A(3) AR, showing interesting antagonistic activity and A(1) selectivity...
  72. ncbi Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents
    Annarella Costanzo
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Firenze, Via Gino Capponi 9, 50121 Firenze Italy
    J Med Chem 45:5710-20. 2002
    ....
  73. ncbi Synthesis and structure-activity relationships of a new set of 1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives as adenosine receptor antagonists
    Vittoria Colotta
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via G Capponi, 9, 50121, Florence, Italy
    Bioorg Med Chem 11:3541-50. 2003
    ..Finally, the SAR studies provide some new insights about the steric and lipophilic requirements of the hA(3) receptor binding pocket which accommodates the benzofused moiety of our 4-amino-triazoloquinoxalin-1-one derivatives...
  74. ncbi Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands
    Silvia Selleri
    Department of Pharmaceutical Sciences, University of Firenze, Via G Capponi 9, 50121 Firenze, Italy
    J Med Chem 46:310-3. 2003
    ..Some of the synthesized compounds are tested in vivo to explore their pharmacological effect as a consequence of their high alpha 1 beta 2 gamma 2 subtype selectivity observed in vitro...
  75. ncbi Synthesis and preliminary pharmacological evaluation of trans-2-amino-5(6)-chloro-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes as dopamine receptor ligands
    Antonio Di Stefano
    Dipartimento di Scienze del Farmaco, Universita G D Annunzio, Chieti, Italy
    Farmaco 57:303-13. 2002
    ..The results suggest that introduction of chlorine substituent in five or six position of previously synthesized trans-2-amino-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes decreases both D1-like and D2-like receptor affinity...
  76. ncbi Synthesis of 4-amino-6-(hetero)arylalkylamino-1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives as potent A(2A) adenosine receptor antagonists
    Vittoria Colotta
    Dipartimento di Scienze Farmaceutiche, Polo Scientifico, Universita di Firenze, Via Ugo Schiff, 6, 50019 Sesto FJ, Fiorentino, Italy
    Bioorg Med Chem 11:5509-18. 2003
    ..Thus, the SAR studies provided us some new insights about the structural requirements of the bA(2A) AR recognition site...
  77. ncbi Synthesis, ligand-receptor modeling studies and pharmacological evaluation of novel 4-modified-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives as potent and selective human A3 adenosine receptor antagonists
    Vittoria Colotta
    Dipartimento di Scienze Farmaceutiche, Laboratorio di Progettazione, Sintesi e Studio di Eterocicli Biologicamente Attivi, Universita di Firenze, Polo Scientifico, Via Ugo Schiff, 6, 50019 Sesto Fiorentino, FI, Italy
    Bioorg Med Chem 16:6086-102. 2008
    ....
  78. ncbi 2-aryl-8-chloro-1,2,4-triazolo[1,5-a]quinoxalin-4-amines as highly potent A1 and A3 adenosine receptor antagonists
    Daniela Catarzi
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Firenze, Polo Scientifico, Via U Schiff, 6, 50019 Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem 13:705-15. 2005
    ..Structure-activity relationships have been explained analyzing the three-dimensional structure of the antagonist-receptor models obtained by molecular docking simulation...
  79. ncbi Differences in the neurotoxicity profile induced by ATP and ATPgammaS in cultured cerebellar granule neurons
    Susanna Amadio
    Santa Lucia Foundation/CERC, Rome, Italy
    Neurochem Int 47:334-42. 2005
    ..Among several P2 receptor antagonists, only pyridoxal-phosphate-6-azophenyl-2',4'-disulphonic acid 4-sodium promotes 80-100% neuroprotection...
  80. ncbi Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage
    Gabriella Guerrini
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Firenze, Via U Schiff, 6, 50019 Polo Scientifico, Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem 15:2573-86. 2007
    ..These compounds were evaluated also for their binding at Benzodiazepine site on GABA(A) receptor complex (GABA(A)/BzR complex) subtype to evaluate their subtype selectivity...
  81. ncbi 4-amido-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-ones as new potent and selective human A3 adenosine receptor antagonists. synthesis, pharmacological evaluation, and ligand-receptor modeling studies
    Ombretta Lenzi
    Dipartimento di Scienze Farmaceutiche, Laboratorio di Progettazione, Sintesi e Studio di Eterocicli Biologicamente Attivi, , Polo Scientifico, Via Ugo Schiff, 6, 50019 Sesto Fiorentino, Italy
    J Med Chem 49:3916-25. 2006
    ..In contrast, the 6-nitro substituent exerted a variable effect. An intensive molecular modeling investigation was performed to rationalize the experimental SAR findings...
  82. ncbi A novel selective GABA(A) alpha1 receptor agonist displaying sedative and anxiolytic-like properties in rodents
    Silvia Selleri
    Department of Pharmaceutical Sciences, University of Firenze, via U Schiff 6, 50019 Sesto Fiorentino, Italy
    J Med Chem 48:6756-60. 2005
    ..Compound 4 displayed affinity only for alpha1beta2gamma2 subtype (K(i) = 31 nM), and in an in-depth, in vivo study it revealed sedative and anxiolytic-like properties without any amnesic and myorelaxant effects in rodents...
  83. ncbi Benzodiazepine receptor ligands. 8: synthesis and pharmacological evaluation of new pyrazolo[5,1-c] [1,2,4]benzotriazine 5-oxide 3- and 8-disubstituted: high affinity ligands endowed with inverse-agonist pharmacological efficacy
    Gabriella Guerrini
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Firenze, Via U Schiff, 6, 50019 Polo Scientifico, Sesto Fiorentino, Florence, Italy
    Bioorg Med Chem 14:758-75. 2006
    ..Compounds 4d and 6d showed an inverse-agonist profile. These compounds were evaluated also for their binding at benzodiazepine site on GABAA receptor complex (GABAA/BzR complex) subtype to evaluate their subtype selectivity...
  84. ncbi 2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database searching
    Ettore Novellino
    Dipartimento di Chimica Farmaceutica e Tossicologica, , Via D. Montesano, 49, 80131 Napoli, Italy. novellin.unima.it
    J Med Chem 48:8253-60. 2005
    ..5, 3440, and 955 nM, respectively, whereas 2-(4-methylbenzimidazol-2-yl)quinoxaline (3b) displayed at the same ARs K(i) values of 8000, 833, and 26 nM, respectively...
  85. ncbi 1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation, and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives
    Daniela Catarzi
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Firenze, Polo Scientifico, Via U Schiff, 6 50019 Sesto Fiorentino, Firenze, Italy
    J Med Chem 48:7932-45. 2005
    ....
  86. ncbi Insight into 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamides as peripheral benzodiazepine receptor ligands: synthesis, biological evaluation and 3D-QSAR investigation
    Silvia Selleri
    Dipartimento di Scienze Farmaceutiche, , Via U. Schiff, 6, 50019 Sesto F.no Firenze, Italy
    Bioorg Med Chem 13:4821-34. 2005
    ..In addition, a subset of the novel compounds showing high affinity for PBR was tested for their ability to modulate the steroid biosynthesis in C6 glioma cells...
  87. ncbi New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies
    Vittoria Colotta
    Dipartimento di Scienze Farmaceutiche, Laboratorio di Progettazione, Sintesi e Studio di Eterocicli Biologicamente Attivi, Universita di Firenze, Polo Scientifico, Via Ugo Schiff, 6, 50019 Sesto Fiorentino, Italy
    J Med Chem 50:4061-74. 2007
    ..The observed structure-affinity relationships of this class of antagonists were also exhaustively rationalized using the recently published ligand-based homology modeling (LBHM) approach...
  88. ncbi Synthesis and structure-activity relationships of 4-cycloalkylamino-1, 2, 4-triazolo[4, 3-a]quinoxalin-1- one derivatives as A1 and A3 adenosine receptor antagonists
    Vittoria Colotta
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Firenze, Italy
    Arch Pharm (Weinheim) 337:35-41. 2004
    ..Finally, SAR studies provide some new insights about the steric requirements of the A(3) receptor pocket, which accommodates the benzofused moiety of our 4-amino-triazoloquinoxalin-1-one derivatives...
  89. ncbi Novel 3-aroylpyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides 8-substituted, ligands at GABAA/benzodiazepine receptor complex: synthesis, pharmacological and molecular modeling studies
    Gabriella Guerrini
    Dipartimento di Scienze Farmaceutiche, Laboratorio di Progettazione, Sintesi e Studio di Eterocicli Biologicamente attivi HeteroBioLab Università degli Studi di Firenze, Via U Schiff, Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem 16:4471-89. 2008
    ..To rationalize and qualitatively interpret the GABA(A)/Bz binding affinities of compounds 8a and 11, a dynamic molecular modeling study has been performed, with the aim of assessing the preferred geometry of protein-ligand complex...
  90. ncbi 1,2,4-Triazolo[1,5-a]quinoxaline derivatives: synthesis and biological evaluation as adenosine receptor antagonists
    Daniela Catarzi
    Dipartimento di Scienze Farmaceutiche, Polo Scientifico, Universita degli Studi di Firenze, Via U Schiff, 6, Sesto Fiorentino FZ, 50019, Italy
    Farmaco 59:71-81. 2004
    ....
  91. ncbi 1,2,4-triazolo[4,3-a]quinoxalin-1-one moiety as an attractive scaffold to develop new potent and selective human A3 adenosine receptor antagonists: synthesis, pharmacological, and ligand-receptor modeling studies
    Vittoria Colotta
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Firenze, Polo Scientifico, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy
    J Med Chem 47:3580-90. 2004
    ..Structure-activity relationships have been explained analyzing the three-dimensional structure of the antagonist-receptor models obtained by molecular docking simulation...
  92. ncbi Preparation and pharmacological characterization of trans-2-amino-5(6)-fluoro-6(5)-hydroxy-1-phenyl-2,3-dihydro-1H-indenes as D2-like dopamine receptor agonists
    Antonio Di Stefano
    Dipartimento di Scienze del Farmaco, , Via dei Vestini 31, 66100 Chieti, Italy
    J Med Chem 48:2646-54. 2005
    ..The selective D(2)-like agonism of compounds 20 and 5e was proved by their effects on basal striatal adenylyl cyclase activity...
  93. ncbi Peripheral-type benzodiazepine receptor binding sites in platelets of patients with panic disorder associated to separation anxiety symptoms
    Stefano Pini
    Psychopharmacology (Berl) 181:407-11. 2005
    ..CONCLUSIONS: Patients with SA symptoms had significantly lower densities of PBRs. PBR expression might become a useful biological marker of these two associated conditions...
  94. ncbi Synthesis and 3D QSAR of new pyrazolo[3,4-b]pyridines: potent and selective inhibitors of A1 adenosine receptors
    Fabrizio Manetti
    Dipartimento Farmaco Chimico Tecnologico, , Via Aldo Moro, I-53100 Siena, Italy
    J Med Chem 48:7172-85. 2005
    ..To rationalize the relationships between structure and affinity of the novel compounds, a 3D QSAR model was also generated starting from compounds belonging to different classes of known A1AR antagonists...
  95. ncbi The role of peripheral benzodiazepine receptors on the function and survival of isolated human pancreatic islets
    Lorella Marselli
    Dipartimento di Endocrinologia e Metabolismo, Sezione Metabolismo, Universita di Pisa, Via Paradisa 2, Ospedale Cisanello, 56100 Pisa, Italy
    Eur J Endocrinol 151:207-14. 2004
    ..We hypothesized that PBRs can have a role in human islet physiopathology, and evaluated the effects of prolonged exposure to two specific PBR ligands, PK11195 and Ro5-4864 on the function and survival of isolated human islets...
  96. ncbi 5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species
    Loredana Cappellacci
    Dipartimento di Scienze Chimiche, Universita di Camerino, 62032 Camerino, Italy
    Bioorg Med Chem 16:336-53. 2008
    ....