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Items: 1 to 50 of 68

1.

Discovery of a novel alpha-7 nicotinic acetylcholine receptor agonist series and characterization of the potent, selective, and orally efficacious agonist 5-(4-acetyl[1,4]diazepan-1-yl)pentanoic acid [5-(4-methoxyphenyl)-1H-pyrazol-3-yl] amide (SEN15924, WAY-361789).

Zanaletti R, Bettinetti L, Castaldo C, Cocconcelli G, Comery T, Dunlop J, Gaviraghi G, Ghiron C, Haydar SN, Jow F, Maccari L, Micco I, Nencini A, Scali C, Turlizzi E, Valacchi M.

J Med Chem. 2012 May 24;55(10):4806-23. doi: 10.1021/jm300247y. Epub 2012 May 3.

PMID:
22468936
2.

How to achieve confidence in drug discovery and development: managing risk (from a reductionist to a holistic approach).

Bakker A, Caricasole A, Gaviraghi G, Pollio G, Robertson G, Terstappen GC, Salerno M, Tunici P.

ChemMedChem. 2009 Jun;4(6):923-33. doi: 10.1002/cmdc.200900056.

PMID:
19434656
3.

Small molecule drug discovery for Huntington's Disease.

Fecke W, Gianfriddo M, Gaviraghi G, Terstappen GC, Heitz F.

Drug Discov Today. 2009 May;14(9-10):453-64. doi: 10.1016/j.drudis.2009.02.006. Epub 2009 Feb 25. Review.

PMID:
19429504
4.

Drug discovery and development for Huntington's disease - an orphan indication with high medical need.

Heitz F, La Rosa S, Gonzalez-Couto E, Gaviraghi G, Terstappen GC.

IDrugs. 2008 Sep;11(9):653-60. Review.

PMID:
18763216
5.

Aryl azoles with neuroprotective activity--parallel synthesis and attempts at target identification.

Cocconcelli G, Diodato E, Caricasole A, Gaviraghi G, Genesio E, Ghiron C, Magnoni L, Pecchioli E, Plazzi PV, Terstappen GC.

Bioorg Med Chem. 2008 Feb 15;16(4):2043-52. Epub 2007 Nov 4.

PMID:
18024137
6.

Target deconvolution strategies in drug discovery.

Terstappen GC, Schlüpen C, Raggiaschi R, Gaviraghi G.

Nat Rev Drug Discov. 2007 Nov;6(11):891-903. Review.

PMID:
17917669
7.

Inhibition of Wnt signaling, modulation of Tau phosphorylation and induction of neuronal cell death by DKK1.

Scali C, Caraci F, Gianfriddo M, Diodato E, Roncarati R, Pollio G, Gaviraghi G, Copani A, Nicoletti F, Terstappen GC, Caricasole A.

Neurobiol Dis. 2006 Nov;24(2):254-65. Epub 2006 Aug 17.

PMID:
16919965
8.

Inhibition of the canonical Wnt signaling pathway by apolipoprotein E4 in PC12 cells.

Caruso A, Motolese M, Iacovelli L, Caraci F, Copani A, Nicoletti F, Terstappen GC, Gaviraghi G, Caricasole A.

J Neurochem. 2006 Jul;98(2):364-71.

9.

The Wnt signaling pathway as a target for the treatment of neurodegenerative disorders.

Terstappen GC, Gaviraghi G, Caricasole A.

IDrugs. 2006 Jan;9(1):35-8.

PMID:
16374731
10.

Two sides of the same coin: Wnt signaling in neurodegeneration and neuro-oncology.

Caricasole A, Bakker A, Copani A, Nicoletti F, Gaviraghi G, Terstappen GC.

Biosci Rep. 2005 Oct-Dec;25(5-6):309-27. Review.

PMID:
16307379
11.

Induction of Dickkopf-1, a negative modulator of the Wnt pathway, is required for the development of ischemic neuronal death.

Cappuccio I, Calderone A, Busceti CL, Biagioni F, Pontarelli F, Bruno V, Storto M, Terstappen GT, Gaviraghi G, Fornai F, Battaglia G, Melchiorri D, Zukin RS, Nicoletti F, Caricasole A.

J Neurosci. 2005 Mar 9;25(10):2647-57. Erratum in: J Neurosci. 2005 Mar 23;25(12):table of contents. Zukin, Suzanne [corrected to Zukin, R Suzanne].

12.

Induction of Dickkopf-1, a negative modulator of the Wnt pathway, is associated with neuronal degeneration in Alzheimer's brain.

Caricasole A, Copani A, Caraci F, Aronica E, Rozemuller AJ, Caruso A, Storto M, Gaviraghi G, Terstappen GC, Nicoletti F.

J Neurosci. 2004 Jun 30;24(26):6021-7.

13.

Evidence that lacidipine at nonsustained antihypertensive doses activates nitrogen monoxide system in the endothelium of salt-loaded Dahl-S rats.

Crespi F, Vecchiato E, Lazzarini C, Andreoli M, Gaviraghi G.

J Cardiovasc Pharmacol. 2002 Apr;39(4):471-7.

PMID:
11904520
14.

Can voltammetry measure nitrogen monoxide (NO) and/or nitrites?

Crespi F, Campagnola M, Neudeck A, McMillan K, Rossetti Z, Pastorino A, Garbin U, Fratta-Pasini A, Reggiani A, Gaviraghi G, Cominacini L.

J Neurosci Methods. 2001 Aug 15;109(1):59-70.

PMID:
11489301
15.

Successful xenografting of cryopreserved primary pancreatic cancers.

Sorio C, Bonora A, Orlandini S, Moore PS, Capelli P, Cristofori P, Dal Negro G, Marchiori P, Gaviraghi G, Falconi M, Pederzoli P, Zamboni G, Scarpa A.

Virchows Arch. 2001 Feb;438(2):154-8.

PMID:
11253117
16.

Lacidipine [correction of Lalsoacidipine] modulates the secretion of matrix metalloproteinase-9 by human macrophages.

Bellosta S, Canavesi M, Favari E, Cominacini L, Gaviraghi G, Fumagalli R, Paoletti R, Bernini F.

J Pharmacol Exp Ther. 2001 Mar;296(3):736-43. Erratum in: J Pharmacol Exp Ther 2001 May;297(2):827.

17.

Electrochemical evidence that lacidipine stimulates release of nitrogen monoxide in rat aorta.

Crespi F, Vecchiato E, Lazzarini C, Gaviraghi G.

Neurosci Lett. 2001 Feb 9;298(3):171-4.

PMID:
11165434
18.

Involvement of cholecystokinin within craving for cocaine: role of cholecystokinin receptor ligands.

Crespi F, Corsi M, Reggiani A, Ratti E, Gaviraghi G.

Expert Opin Investig Drugs. 2000 Oct;9(10):2249-58. Review.

PMID:
11060804
19.

The calcium-channel blocker lacidipine reduces the development of atherosclerotic lesions in the apoE-deficient mouse.

Cristofori P, Lanzoni A, Quartaroli M, Pastorino AM, Zancanaro C, Cominacini L, Gaviraghi G, Turton J.

J Hypertens. 2000 Oct;18(10):1429-36.

PMID:
11057430
20.

Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.

Ursini A, Capelli AM, Carr RA, Cassarà P, Corsi M, Curcuruto O, Curotto G, Dal Cin M, Davalli S, Donati D, Feriani A, Finch H, Finizia G, Gaviraghi G, Marien M, Pentassuglia G, Polinelli S, Ratti E, Reggiani AM, Tarzia G, Tedesco G, Tranquillini ME, Trist DG, Van Amsterdam FT.

J Med Chem. 2000 Oct 5;43(20):3596-613. Erratum in: J Med Chem 2000 Dec 28;43(26):5057. Reggiani A [corrected to Reggiani AM].

PMID:
11020274
21.

Excitatory amino acid receptors.

Gaviraghi G.

Pharm Acta Helv. 2000 Mar;74(2-3):219-20. No abstract available.

PMID:
10812961
22.

Anti-atherosclerotic activity of the calcium antagonist lacidipine in cholesterol-fed hamsters.

Cristofori P, Lanzoni A, Gaviraghi G, Turton J, Sbarbati A.

Biomed Pharmacother. 2000 Mar;54(2):93-9.

PMID:
10759293
23.

Comparative effects of different dihydropyridines on the expression of adhesion molecules induced by TNF-alpha on endothelial cells.

Cominacini L, Pasini AF, Pastorino AM, Garbin U, Davoli A, Rigoni A, Campagnola M, Tosetti ML, Rossato P, Gaviraghi G.

J Hypertens. 1999 Dec;17(12 Pt 2):1837-41.

PMID:
10703877
24.

Extracellular matrix gene expression in the left ventricular tissue of spontaneously hypertensive rats.

Seccia TM, Bettini E, Vulpis V, Quartaroli M, Trist DG, Gaviraghi G, Pirrelli A.

Blood Press. 1999;8(1):57-64.

PMID:
10412884
25.

Cycloalkyl indole-2-carboxylates as useful tools for mapping the "north-eastern" region of the glycine binding site associated with the NMDA receptor.

Micheli F, Di Fabio R, Capelli AM, Cugola A, Curcuruto O, Feriani A, Gastaldi P, Gaviraghi G, Marchioro C, Orlandi A, Pozzan A, Quaglia AM, Reggiani A, van Amsterdam F.

Arch Pharm (Weinheim). 1999 Mar;332(3):73-80.

PMID:
10228452
26.

Oxidized low-density lipoprotein increases the production of intracellular reactive oxygen species in endothelial cells: inhibitory effect of lacidipine.

Cominacini L, Garbin U, Pasini AF, Davoli A, Campagnola M, Pastorino AM, Gaviraghi G, Lo Cascio V.

J Hypertens. 1998 Dec;16(12 Pt 2):1913-9.

PMID:
9886877
27.

Lacidipine inhibits the activation of the transcription factor NF-kappaB and the expression of adhesion molecules induced by pro-oxidant signals on endothelial cells.

Cominacini L, Garbin U, Fratta Pasini A, Paulon T, Davoli A, Campagnola M, Marchi E, Pastorino AM, Gaviraghi G, Lo Cascio V.

J Hypertens. 1997 Dec;15(12 Pt 2):1633-40.

PMID:
9488215
28.

Spontaneous preference for ethanol in naive rats is influenced by cholecystokinin A receptor antagonism.

Crespi F, Corsi M, England T, Ratti E, Trist DG, Gaviraghi G.

Alcohol. 1997 Jul-Aug;14(4):327-32.

PMID:
9209547
29.

Structural changes of small resistance arteries in spontaneously hypertensive rats after treatment with various doses of lacidipine.

Porteri E, Rizzoni D, Castellano M, Bettoni G, Muiesan ML, Salvetti M, Quartaroli M, Gaviraghi G, Rosei EA.

J Hypertens. 1997 Jun;15(6):619-25.

PMID:
9218181
30.

Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site.

Di Fabio R, Capelli AM, Conti N, Cugola A, Donati D, Feriani A, Gastaldi P, Gaviraghi G, Hewkin CT, Micheli F, Missio A, Mugnaini M, Pecunioso A, Quaglia AM, Ratti E, Rossi L, Tedesco G, Trist DG, Reggiani A.

J Med Chem. 1997 Mar 14;40(6):841-50.

PMID:
9083472
31.

Synthesis and antimicrobial evaluation of 2 beta-chloromethyl-6 beta-carbamoylmethyl-penam-1,1-dioxide-3-carboxylic acid.

Gaviraghi G, Perboni A, Tamburini B, Xerri L, Salvatori A, Spadoni G, Tarzia G.

Farmaco. 1996 Jul;51(7):535-8.

PMID:
8765676
32.

Synthesis of novel 6-alpha and 6-beta-alkylcarbonylmethyl substituted penems.

Pentassuglia G, Tarzia G, Andreotti D, Bismara C, Carlesso R, Donati D, Gaviraghi G, Perboni A, Pezzoli A, Rossi T, et al.

J Antibiot (Tokyo). 1995 May;48(5):399-407.

33.

Recent developments in the use of calcium antagonists in myocardial protection.

Gaviraghi G, Micheli D, Trist DG.

Pharmacol Res. 1995 Mar-Apr;31(3-4):251-4. Review.

PMID:
7630866
34.

Cholinergic agents structurally related to furtrethonium. 2. Synthesis and antimuscarinic activity of a series of N-[5-[(1'-substituted-acetoxy) methyl]-2-furfuryl]dialkylamines.

Feriani A, Gaviraghi G, Toson G, Mor M, Barbieri A, Grana E, Boselli C, Guarneri M, Simoni D, Manfredini S.

J Med Chem. 1994 Dec 9;37(25):4278-87.

PMID:
7996539
35.

A further analysis of the contraction induced by activation of cholecystokinin A receptors in guinea pig isolated ileum longitudinal muscle-myenteric plexus.

Corsi M, Palea S, Pietra C, Oliosi B, Gaviraghi G, Sugg E, Van Amsterdam FT, Trist DG.

J Pharmacol Exp Ther. 1994 Aug;270(2):734-40.

PMID:
7520941
36.

Quantification of the calcium antagonism of lacidipine by kinetic analysis.

Giacometti A, Micheli D, Gaviraghi G, Trist DG.

J Pharmacol Exp Ther. 1994 Apr;269(1):424-9.

PMID:
8169848
37.

ADP beta S induces contraction of the human isolated urinary bladder through a purinoceptor subtype different from P2X and P2Y.

Palea S, Corsi M, Pietra C, Artibani W, Calpista A, Gaviraghi G, Trist DG.

J Pharmacol Exp Ther. 1994 Apr;269(1):193-7.

PMID:
8169824
38.
39.

Lacidipine: experimental evidence of vasculoprotective properties.

Cristofori P, Micheli D, Terron A, Gaviraghi G.

J Cardiovasc Pharmacol. 1994;23 Suppl 5:S90-3.

PMID:
7609515
40.

The molecular basis for lacidipine's unique pharmacokinetics: optimal hydrophobicity results in membrane interactions that may facilitate the treatment of atherosclerosis.

Herbette LG, Mason PE, Gaviraghi G, Tulenko TN, Mason RP.

J Cardiovasc Pharmacol. 1994;23 Suppl 5:S16-25. Review.

PMID:
7609501
41.

In-vivo binding of (+)-[3H]PN 200-110 to peripheral tissues and brain of spontaneously hypertensive rats: effect of lacidipine.

Mennini T, Taddei C, Uslenghi A, Cagnotto A, Micheli D, Trist D, Gaviraghi G, Ratti E.

J Pharm Pharmacol. 1993 May;45(5):430-3.

PMID:
8099961
43.

Analysis of the CCKB receptor antagonism of virginiamycin in guinea-pig ileum longitudinal myenteric plexus.

Corsi M, Pojani G, Dal Forno G, Pietra C, Gaviraghi G, Trist D.

Br J Pharmacol. 1993 Apr;108(4):1164-8.

44.

Molecular interaction between lacidipine and biological membranes.

Herbette LG, Gaviraghi G, Tulenko T, Mason RP.

J Hypertens Suppl. 1993 Mar;11(1):S13-9.

PMID:
8387105
45.

Inhibition of [3H]-(+)-MK 801 binding to rat brain sections by CPP and 7-chlorokynurenic acid: an autoradiographic analysis.

Tacconi S, Ratti E, Marien MR, Gaviraghi G, Bowery NG.

Br J Pharmacol. 1993 Mar;108(3):577-82.

46.

Synthesis and antimicrobial activity of DNA-gyrase inhibiting derivatives of 4-oxo-1,4-dihydro-3-pyridinecarboxylic acid.

Bassini C, Bismara C, Carlesso R, Feriani A, Gaviraghi G, Marchioro C, Perboni A, Shaw RE, Tamburini B, Tarzia G, et al.

Farmaco. 1993 Feb;48(2):159-89.

PMID:
8388214
47.

Analysis of the interaction between lacidipine and BAY K 8644 in two isolated rabbit arteries.

Giacometti A, Quartaroli M, Gaviraghi G, Micheli D, Trist D.

J Pharmacol Exp Ther. 1992 Dec;263(3):1241-7.

PMID:
1281877
48.

Evidence for two cholecystokinin receptors mediating the contraction of the guinea pig isolated ileum longitudinal muscle myenteric plexus.

Dal Forno G, Pietra C, Urciuoli M, van Amsterdam FT, Toson G, Gaviraghi G, Trist D.

J Pharmacol Exp Ther. 1992 Jun;261(3):1056-63.

PMID:
1602372
49.

A novel class of cholinergic agents structurally related to 2-morpholinol.

Feriani A, Gaviraghi G, Toson G, Valsecchi B, Caldirola P, Ravasi M, Merlini L, Redaelli C, Grana E, Zonta F, et al.

Farmaco. 1992 Jan;47(1):3-20.

PMID:
1616575
50.

A comparative study on the vascular selectivity of lacidipine in the pithed rat.

Micheli D, Massagrande M, Giacometti A, Collodel A, Gaviraghi G.

Pharmacology. 1992;44(3):150-7.

PMID:
1579596

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