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Items: 21

1.

╬│-secretase inhibitors and modulators for the treatment of Alzheimer's disease: disappointments and hopes.

Imbimbo BP, Giardina GA.

Curr Top Med Chem. 2011;11(12):1555-70. Review.

PMID:
21510832
2.

Accelerating the drug-discovery process: new tools and technologies available to medicinal chemists.

Raveglia LF, Giardina GA.

Future Med Chem. 2009 Sep;1(6):1019-23. doi: 10.4155/fmc.09.79. No abstract available.

3.

Creating effective medicinal chemistry collaborations in drug discovery.

Giardina GA, Raveglia LF.

Future Med Chem. 2009 Apr;1(1):3-6. doi: 10.4155/fmc.09.1. No abstract available.

4.

Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 2).

Peretto I, Fossati C, Giardina GA, Giardini A, Guala M, La Porta E, Petrillo P, Radaelli S, Radice L, Raveglia LF, Santoro E, Scudellaro R, Scarpitta F, Cerri A, Menegon S, Dondio GM, Rizzi A, Armani E, Amari G, Civelli M, Villetti G, Patacchini R, Bergamaschi M, Bassani F, Delcanale M, Imbimbo BP.

J Med Chem. 2007 Apr 5;50(7):1693-7. Epub 2007 Mar 13.

PMID:
17352463
5.

Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 1).

Peretto I, Forlani R, Fossati C, Giardina GA, Giardini A, Guala M, La Porta E, Petrillo P, Radaelli S, Radice L, Raveglia LF, Santoro E, Scudellaro R, Scarpitta F, Bigogno C, Misiano P, Dondio GM, Rizzi A, Armani E, Amari G, Civelli M, Villetti G, Patacchini R, Bergamaschi M, Delcanale M, Salcedo C, Fernández AG, Imbimbo BP.

J Med Chem. 2007 Apr 5;50(7):1571-83. Epub 2007 Mar 13.

PMID:
17352462
6.

Modification of nociception and morphine tolerance by the selective opiate receptor-like orphan receptor antagonist (-)-cis-1-methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111).

Zaratin PF, Petrone G, Sbacchi M, Garnier M, Fossati C, Petrillo P, Ronzoni S, Giardina GA, Scheideler MA.

J Pharmacol Exp Ther. 2004 Feb;308(2):454-61. Epub 2003 Oct 30.

PMID:
14593080
7.

Antagonists at the neurokinin receptors--recent patent literature.

Giardina GA, Gagliardi S, Martinelli M.

IDrugs. 2003 Aug;6(8):758-72. Review.

PMID:
12917772
8.

Morphinan derivatives--A review of the recent patent literature.

Gagliardi S, Dondio G, Giardina GA.

IDrugs. 2003 Feb;6(2):129-37. Review. Erratum in: IDrugs. 2003 Mar;6(3):276.

PMID:
12789616
9.

Nonpeptide tachykinin receptor antagonists. III. SB 235375, a low central nervous system-penetrant, potent and selective neurokinin-3 receptor antagonist, inhibits citric acid-induced cough and airways hyper-reactivity in guinea pigs.

Hay DW, Giardina GA, Griswold DE, Underwood DC, Kotzer CJ, Bush B, Potts W, Sandhu P, Lundberg D, Foley JJ, Schmidt DB, Martin LD, Kilian D, Legos JJ, Barone FC, Luttmann MA, Grugni M, Raveglia LF, Sarau HM.

J Pharmacol Exp Ther. 2002 Jan;300(1):314-23.

PMID:
11752131
10.
11.

Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists.

Blaney FE, Raveglia LF, Artico M, Cavagnera S, Dartois C, Farina C, Grugni M, Gagliardi S, Luttmann MA, Martinelli M, Nadler GM, Parini C, Petrillo P, Sarau HM, Scheideler MA, Hay DW, Giardina GA.

J Med Chem. 2001 May 24;44(11):1675-89.

PMID:
11356103
12.

Selective delta opioid receptor agonists for inflammatory and neuropathic pain.

Dondio G, Ronzoni S, Farina C, Graziani D, Parini C, Petrillo P, Giardina GA.

Farmaco. 2001 Jan-Feb;56(1-2):117-9.

PMID:
11347951
13.

Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.

Sarau HM, Feild JA, Ames RS, Foley JJ, Nuthulaganti P, Schmidt DB, Buckley PT, Elshourbagy NA, Brawner ME, Luttmann MA, Giardina GA, Hay DW.

Eur J Pharmacol. 2001 Feb 16;413(2-3):143-50.

PMID:
11226387
14.

Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist.

Sarau HM, Griswold DE, Bush B, Potts W, Sandhu P, Lundberg D, Foley JJ, Schmidt DB, Webb EF, Martin LD, Legos JJ, Whitmore RG, Barone FC, Medhurst AD, Luttmann MA, Giardina GA, Hay DW.

J Pharmacol Exp Ther. 2000 Oct;295(1):373-81.

PMID:
10992004
15.

Evidence that the proposed novel human "neurokinin-4" receptor is pharmacologically similar to the human neurokinin-3 receptor but is not of human origin.

Sarau HM, Mooney JL, Schmidt DB, Foley JJ, Buckley PT, Giardina GA, Wang DY, Lee JA, Hay DW.

Mol Pharmacol. 2000 Sep;58(3):552-9.

PMID:
10953048
16.

The opioid-receptor-like 1 (ORL-1) as a potential target for new analgesics.

Barlocco D, Cignarella G, Giardina GA, Toma L.

Eur J Med Chem. 2000 Mar;35(3):275-82. Review.

PMID:
10785553
17.

Replacement of the quinoline system in 2-phenyl-4-quinolinecarboxamide NK-3 receptor antagonists.

Giardina GA, Artico M, Cavagnera S, Cerri A, Consolandi E, Gagliardi S, Graziani D, Grugni M, Hay DW, Luttmann MA, Mena R, Raveglia LF, Rigolio R, Sarau HM, Schmidt DB, Zanoni G, Farina C.

Farmaco. 1999 Jun 30;54(6):364-74.

PMID:
10443017
18.

Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412).

Giardina GA, Raveglia LF, Grugni M, Sarau HM, Farina C, Medhurst AD, Graziani D, Schmidt DB, Rigolio R, Luttmann M, Cavagnera S, Foley JJ, Vecchietti V, Hay DW.

J Med Chem. 1999 Mar 25;42(6):1053-65.

PMID:
10090788
19.

Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework.

Giardina GA, Sarau HM, Farina C, Medhurst AD, Grugni M, Raveglia LF, Schmidt DB, Rigolio R, Luttmann M, Vecchietti V, Hay DW.

J Med Chem. 1997 Jun 6;40(12):1794-807.

PMID:
9191956
20.

Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.

Sarau HM, Griswold DE, Potts W, Foley JJ, Schmidt DB, Webb EF, Martin LD, Brawner ME, Elshourbagy NA, Medhurst AD, Giardina GA, Hay DW.

J Pharmacol Exp Ther. 1997 Jun;281(3):1303-11.

PMID:
9190866
21.

2-Phenyl-4-quinolinecarboxamides: a novel class of potent and selective non-peptide competitive antagonists for the human neurokinin-3 receptor.

Giardina GA, Sarau HM, Farina C, Medhurst AD, Grugni M, Foley JJ, Raveglia LF, Schmidt DB, Rigolio R, Vassallo M, Vecchietti V, Hay DW.

J Med Chem. 1996 Jun 7;39(12):2281-4. No abstract available.

PMID:
8691422

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