Tricyclic thienopyridine–pyrimidones/thienopyrimidine–pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain

Autor: Larry Heimark, Duane A. Burnett, Birendra N. Pramanik, Thavalakulamgara K. Sasikumar, William J. Greenlee, Rosalia Bertorelli, Gianluca Lozza, Cheng Li, Mariagrazia Grilli, Li Qiang, Angelo Reggiani

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:3199-3203

Introduction of small unsaturated alkylamino groups at the 4-position of the A-ring of the tricyclic framework (triazafluorenone) afforded extremely potent and selective mGluR1 antagonists with desirable properties. Compounds 11q and 11s are active i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d45f3b03ac5aa2844ae38745eaaeecb8
https://doi.org/10.1016/j.bmcl.2009.04.104

Rapamycin, but not FK506 and GPI-1046, increases neurite outgrowth in PC12 cells by inhibiting cell cycle progression

Autor: Eric M. Parker, Carol M Babij, Ennio Ongini, Gianluca Lozza, Angela Monopoli

Publikováno v: Neuropharmacology. 39:1913-1919

Immunophilin ligands such as rapamycin, FK506 and GPI-1046 have been reported to increase neurite outgrowth in vitro and to have neuroprotective activity in vitro and in vivo. In this study, however, FK506 and GPI-1046 (0.1-1000 nM) had little effect

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ed3ece76c8336e7de4e18c96169b54f
https://doi.org/10.1016/s0028-3908(00)00028-9

Blockade of adenosine A2A receptors by SCH 58261 results in neuroprotective effects in cerebral ischaemia in rats

Autor: Ennio Ongini, Amanda Mattavelli, Angelo Forlani, Angela Monopoli, Gianluca Lozza

Publikováno v: NeuroReport. 9:3955-3958

Blockade of adenosine receptors can reduce cerebral infarct size in the model of global ischaemia. Using the potent and selective A2A adenosine receptor antagonist, SCH 58261, we assessed whether A2A receptors are involved in the neuronal damage foll

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2007726d040731d05bbf57a1f4382be7
https://doi.org/10.1097/00001756-199812010-00034

Cardiovascular pharmacology of SCH 59761, a highly potent, non-selective, adenosine receptor agonist

Autor: Ennio Ongini, C. Casati, Angela Monopoli, A. Conti, Gianluca Lozza

Publikováno v: Drug Development Research. 39:1-11

The therapeutic application of selective adenosine agonists is hampered by the difficulty of separating desirable actions from side effects. A non-selective agent, combining A 1 and A 2A properties, might have advantages in this regard. In the presen

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::528d7582e8b45d1904ea9dd58550c27a
https://doi.org/10.1002/(sici)1098-2299(19960901)39:1<1::aid-ddr1>3.0.co

Evaluation of cannabinoid receptor 2 and metabotropic glutamate receptor 1 functional responses using a cell impedance-based technology

Autor: Rossella Brusa, Isabella Mancini, Gianluca Lozza, Angelo Reggiani, Paola Scandroglio, Massimiliano Beltramo, Roberta Petrò

Publikováno v: Journal of Biomolecular Screening
Journal of Biomolecular Screening, SAGE Publications, 2010, 15 (10), pp.1238-1247. ⟨10.1177/1087057110375615⟩

Recently, new technologies based on biosensors and called label free have been developed. These technologies eliminate the need for using markers and dyes. The authors applied one of these technologies, based on measurement of cell impedance variatio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1409d9d55827f7853e9a0e0cf691893d
https://hal.archives-ouvertes.fr/hal-01129429