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Items: 1 to 50 of 91

1.

Synergic stimulation of serotonin 5-HT1A receptor and α2-adrenoceptors for neuropathic pain relief: Preclinical effects of 2-substituted imidazoline derivatives.

Di Cesare Mannelli L, Ghelardini C, Micheli L, Del Bello F, Giannella M, Piergentili A, Pigini M, Quaglia W.

Eur J Pharmacol. 2017 Sep 5;810:128-133. doi: 10.1016/j.ejphar.2017.06.023. Epub 2017 Jun 17.

PMID:
28633926
2.

Combined Interactions with I1-, I2-Imidazoline Binding Sites and α2-Adrenoceptors To Manage Opioid Addiction.

Giusepponi ME, Cifani C, Micioni Di Bonaventura MV, Mattioli L, Hudson A, Diamanti E, Del Bello F, Giannella M, Mammoli V, Paoletti CD, Piergentili A, Pigini M, Quaglia W.

ACS Med Chem Lett. 2016 Sep 8;7(10):956-961. eCollection 2016 Oct 13.

3.

The Versatile 2-Substituted Imidazoline Nucleus as a Structural Motif of Ligands Directed to the Serotonin 5-HT1A Receptor.

Del Bello F, Cilia A, Carrieri A, Fasano DC, Ghelardini C, Di Cesare Mannelli L, Micheli L, Santini C, Diamanti E, Giannella M, Giorgioni G, Mammoli V, Paoletti CD, Petrelli R, Piergentili A, Quaglia W, Pigini M.

ChemMedChem. 2016 Oct 19;11(20):2287-2298. doi: 10.1002/cmdc.201600383. Epub 2016 Sep 30.

PMID:
27690321
4.

A Novel Class of Dopamine D4 Receptor Ligands Bearing an Imidazoline Nucleus.

Mammoli V, Bonifazi A, Dal Ben D, Giannella M, Giorgioni G, Piergentili A, Pigini M, Quaglia W, Thomas A, Newman AH, Ferré S, Sanchez-Soto M, Keck TM, Del Bello F.

ChemMedChem. 2016 Aug 19;11(16):1819-28. doi: 10.1002/cmdc.201600022. Epub 2016 Mar 15.

5.

Dual Alpha2C/5HT1A Receptor Agonist Allyphenyline Induces Gastroprotection and Inhibits Fundic and Colonic Contractility.

Zádori ZS, Fehér Á, Tóth VE, Al-Khrasani M, Köles L, Sipos S, Del Bello F, Pigini M, Gyires K.

Dig Dis Sci. 2016 Jun;61(6):1512-23. doi: 10.1007/s10620-015-4026-9. Epub 2016 Feb 10.

PMID:
26860509
6.

Biological profile and bioavailability of imidazoline compounds on morphine tolerance modulation.

Caprioli G, Mammoli V, Ricciutelli M, Sagratini G, Ubaldi M, Domi E, Mennuni L, Sabatini C, Galimberti C, Ferrari F, Milia C, Comi E, Lanza M, Giannella M, Pigini M, Del Bello F.

Eur J Pharmacol. 2015 Dec 15;769:219-24. doi: 10.1016/j.ejphar.2015.11.021. Epub 2015 Nov 24.

PMID:
26593429
7.

Antagonism/Agonism modulation to build novel antihypertensives selectively triggering i1-imidazoline receptor activation.

Del Bello F, Bargelli V, Cifani C, Gratteri P, Bazzicalupi C, Diamanti E, Giannella M, Mammoli V, Matucci R, Micioni Di Bonaventura MV, Piergentili A, Quaglia W, Pigini M.

ACS Med Chem Lett. 2015 Apr 3;6(5):496-501. doi: 10.1021/acsmedchemlett.5b00115. eCollection 2015 May 14.

8.

Investigation of allyphenyline efficacy in the treatment of alcohol withdrawal symptoms.

Ubaldi M, Del Bello F, Domi E, Pigini M, Nasuti C.

Eur J Pharmacol. 2015 Aug 5;760:122-8. doi: 10.1016/j.ejphar.2015.04.005. Epub 2015 Apr 17.

PMID:
25895641
9.

Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.

Del Bello F, Diamanti E, Giannella M, Mammoli V, Mattioli L, Titomanlio F, Piergentili A, Quaglia W, Lanza M, Sabatini C, Caselli G, Poggesi E, Pigini M.

ACS Med Chem Lett. 2013 Jul 22;4(9):875-9. doi: 10.1021/ml400232p. eCollection 2013 Sep 12.

10.

Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives in α1-adrenergic and 5-HT1A receptor binding sites recognition.

Bonifazi A, Piergentili A, Del Bello F, Farande Y, Giannella M, Pigini M, Amantini C, Nabissi M, Farfariello V, Santoni G, Poggesi E, Leonardi A, Menegon S, Quaglia W.

J Med Chem. 2013 Jan 24;56(2):584-8. doi: 10.1021/jm301525w. Epub 2013 Jan 8.

PMID:
23252794
11.

Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.

Del Bello F, Diamanti E, Giannella M, Mammoli V, Marchioro C, Mattioli L, Titomanlio F, Piergentili A, Quaglia W, Benedetti G, Varrone M, Pigini M.

ACS Med Chem Lett. 2012 Jun 8;3(7):535-9. doi: 10.1021/ml300064v. eCollection 2012 Jul 12.

12.

Favourable involvement of α2A-adrenoreceptor antagonism in the I₂-imidazoline binding sites-mediated morphine analgesia enhancement.

Mammoli V, Bonifazi A, Del Bello F, Diamanti E, Giannella M, Hudson AL, Mattioli L, Perfumi M, Piergentili A, Quaglia W, Titomanlio F, Pigini M.

Bioorg Med Chem. 2012 Apr 1;20(7):2259-65. doi: 10.1016/j.bmc.2012.02.016. Epub 2012 Feb 13.

PMID:
22370341
13.

Might the observed α(2A)-adrenoreceptor agonism or antagonism of allyphenyline analogues be ascribed to different molecular conformations?

Diamanti E, Del Bello F, Carbonara G, Carrieri A, Fracchiolla G, Giannella M, Mammoli V, Piergentili A, Pohjanoksa K, Quaglia W, Scheinin M, Pigini M.

Bioorg Med Chem. 2012 Mar 15;20(6):2082-90. doi: 10.1016/j.bmc.2012.01.035. Epub 2012 Jan 31.

PMID:
22341244
14.

Characterization of the hypothermic effects of imidazoline I₂ receptor agonists in rats.

Thorn DA, An XF, Zhang Y, Pigini M, Li JX.

Br J Pharmacol. 2012 Jul;166(6):1936-45. doi: 10.1111/j.1476-5381.2012.01894.x.

15.

1,4-dioxane, a suitable scaffold for the development of novel M₃ muscarinic receptor antagonists.

Del Bello F, Barocelli E, Bertoni S, Bonifazi A, Camalli M, Campi G, Giannella M, Matucci R, Nesi M, Pigini M, Quaglia W, Piergentili A.

J Med Chem. 2012 Feb 23;55(4):1783-7. doi: 10.1021/jm2013216. Epub 2012 Feb 2.

PMID:
22243489
16.

α2C-adrenoceptor modulators: a patent review.

Quaglia W, Del Bello F, Giannella M, Piergentili A, Pigini M.

Expert Opin Ther Pat. 2011 Apr;21(4):455-81. doi: 10.1517/13543776.2011.565333. Review.

PMID:
21413828
17.

Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.

Del Bello F, Mattioli L, Ghelfi F, Giannella M, Piergentili A, Quaglia W, Cardinaletti C, Perfumi M, Thomas RJ, Zanelli U, Marchioro C, Dal Cin M, Pigini M.

J Med Chem. 2010 Nov 11;53(21):7825-35. doi: 10.1021/jm100977d.

PMID:
20925410
18.

Structure-activity relationships in 1,4-benzodioxan-related compounds. 10. Novel α1-adrenoreceptor antagonists related to openphendioxan: synthesis, biological evaluation, and α1d computational study.

Carrieri A, Piergentili A, Del Bello F, Giannella M, Pigini M, Leonardi A, Fanelli F, Quaglia W.

Bioorg Med Chem. 2010 Oct 1;18(19):7065-77. doi: 10.1016/j.bmc.2010.08.002. Epub 2010 Aug 6.

PMID:
20801662
19.

Novel imidazoline compounds as partial or full agonists of D2-like dopamine receptors inspired by I2-imidazoline binding sites ligand 2-BFI.

Giorgioni G, Ambrosini D, Vesprini C, Hudson A, Nasuti C, Di Stefano A, Sozio P, Ciampi O, Costa B, Martini C, Carrieri A, Carbonara G, Enzensperger C, Pigini M.

Bioorg Med Chem. 2010 Oct 1;18(19):7085-91. doi: 10.1016/j.bmc.2010.08.005. Epub 2010 Aug 6.

PMID:
20801048
20.

Novel highly potent and selective sigma 1 receptor antagonists related to spipethiane.

Piergentili A, Amantini C, Del Bello F, Giannella M, Mattioli L, Palmery M, Perfumi M, Pigini M, Santoni G, Tucci P, Zotti M, Quaglia W.

J Med Chem. 2010 Feb 11;53(3):1261-9. doi: 10.1021/jm901542q.

PMID:
20067271
21.

Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation.

Piergentili A, Quaglia W, Del Bello F, Giannella M, Pigini M, Barocelli E, Bertoni S, Matucci R, Nesi M, Bruni B, Di Vaira M.

Bioorg Med Chem. 2009 Dec 15;17(24):8174-85. doi: 10.1016/j.bmc.2009.10.027. Epub 2009 Oct 20.

PMID:
19896386
22.

Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine?

Cardinaletti C, Mattioli L, Ghelfi F, Del Bello F, Giannella M, Bruzzone A, Paris H, Perfumi M, Piergentili A, Quaglia W, Pigini M.

J Med Chem. 2009 Nov 26;52(22):7319-22. doi: 10.1021/jm901262f.

PMID:
19886609
23.

[Effects of 2% ibopamine eye drops on the results of computerized visual field].

Pigini MA, Avila MP, Magacho L.

Arq Bras Oftalmol. 2009 May-Jun;72(3):365-9. Portuguese.

24.

Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents.

Quaglia W, Piergentili A, Del Bello F, Farande Y, Giannella M, Pigini M, Rafaiani G, Carrieri A, Amantini C, Lucciarini R, Santoni G, Poggesi E, Leonardi A.

J Med Chem. 2008 Oct 23;51(20):6359-70. doi: 10.1021/jm800461k. Epub 2008 Sep 26.

PMID:
18817363
25.

[2% ibopamine vs. water-drinking test as a provocative test for glaucoma].

Magacho L, Reis R, Pigini MA, Avila MP.

Arq Bras Oftalmol. 2008 Jul-Aug;71(4):499-503. Portuguese.

26.

Novel ligands rationally designed for characterizing I2-imidazoline binding sites nature and functions.

Gentili F, Cardinaletti C, Vesprini C, Ghelfi F, Farande A, Giannella M, Piergentili A, Quaglia W, Mattioli L, Perfumi M, Hudson A, Pigini M.

J Med Chem. 2008 Aug 28;51(16):5130-4. doi: 10.1021/jm800400k. Epub 2008 Jul 29.

PMID:
18661965
27.

Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.

Gentili F, Cardinaletti C, Vesprini C, Carrieri A, Ghelfi F, Farande A, Giannella M, Piergentili A, Quaglia W, Laurila JM, Huhtinen A, Scheinin M, Pigini M.

J Med Chem. 2008 Jul 24;51(14):4289-99. doi: 10.1021/jm800250z. Epub 2008 Jun 25.

PMID:
18578476
28.

Alpha2-adrenoreceptors profile modulation. 3.1 (R)-(+)-m-nitrobiphenyline, a new efficient and alpha2C-subtype selective agonist.

Crassous PA, Cardinaletti C, Carrieri A, Bruni B, Di Vaira M, Gentili F, Ghelfi F, Giannella M, Paris H, Piergentili A, Quaglia W, Schaak S, Vesprini C, Pigini M.

J Med Chem. 2007 Aug 9;50(16):3964-8. Epub 2007 Jul 14.

PMID:
17630725
29.

Agonists and antagonists targeting the different alpha2-adrenoceptor subtypes.

Gentili F, Pigini M, Piergentili A, Giannella M.

Curr Top Med Chem. 2007;7(2):163-86. Review.

PMID:
17266604
30.

Involvement of I2-imidazoline binding sites in positive and negative morphine analgesia modulatory effects.

Gentili F, Cardinaletti C, Carrieri A, Ghelfi F, Mattioli L, Perfumi M, Vesprini C, Pigini M.

Eur J Pharmacol. 2006 Dec 28;553(1-3):73-81. Epub 2006 Sep 26.

PMID:
17081513
31.

3-[5-(4,5-dihydro-1H-imidazol-2-yl)-furan-2-yl]phenylamine (Amifuraline), a promising reversible and selective peripheral MAO-A inhibitor.

Gentili F, Pizzinat N, Ordener C, Marchal-Victorion S, Maurel A, Hofmann R, Renard P, Delagrange P, Pigini M, Parini A, Giannella M.

J Med Chem. 2006 Sep 7;49(18):5578-86.

PMID:
16942031
32.
33.

alpha 2-adrenoreceptors profile modulation. 2. Biphenyline analogues as tools for selective activation of the alpha 2C-subtype.

Gentili F, Ghelfi F, Giannella M, Piergentili A, Pigini M, Quaglia W, Vesprini C, Crassous PA, Paris H, Carrieri A.

J Med Chem. 2004 Dec 2;47(25):6160-73.

PMID:
15566287
34.

I1 imidazoline receptor-mediated effects on apoptotic processes in PC12 cells.

Dupuy L, Urosevic D, Greney H, Quaglia W, Pigini M, Brasili L, Dontenwill M, Bousquet P.

Cell Death Differ. 2004 Sep;11(9):1049-52. No abstract available.

35.

Muscarinic subtypes profile modulation within a series of new antagonists, bridged bicyclic derivatives of 2,2-diphenyl-[1,3]-dioxolan-4-ylmethyl-dimethylamine.

Piergentili A, Gentili F, Ghelfi F, Marucci G, Pigini M, Quaglia W, Giannella M.

Bioorg Med Chem. 2003 Sep 1;11(18):3901-11.

PMID:
12927850
36.

Imidazoline binding sites (IBS) profile modulation: key role of the bridge in determining I1-IBS or I2-IBS selectivity within a series of 2-phenoxymethylimidazoline analogues.

Gentili F, Bousquet P, Brasili L, Dontenwill M, Feldman J, Ghelfi F, Giannella M, Piergentili A, Quaglia W, Pigini M.

J Med Chem. 2003 May 22;46(11):2169-76.

PMID:
12747788
37.

Binding of nicotine and homoazanicotine analogues at neuronal nicotinic acetylcholinergic (nACh) receptors.

Ferretti G, Dukat M, Giannella M, Piergentili A, Pigini M, Quaglia W, Damaj MI, Martin BR, Glennon RA.

Bioorg Med Chem Lett. 2003 Feb 24;13(4):733-5.

PMID:
12639569
38.

Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.

Ferretti G, Dukat M, Giannella M, Piergentili A, Pigini M, Quaglia W, Damaj MI, Martin BR, Glennon RA.

J Med Chem. 2002 Oct 10;45(21):4724-31.

PMID:
12361399
39.

Structure-activity relationships in 1,4-benzodioxan-related compounds. 7. Selectivity of 4-phenylchroman analogues for alpha(1)-adrenoreceptor subtypes.

Quaglia W, Pigini M, Piergentili A, Giannella M, Gentili F, Marucci G, Carrieri A, Carotti A, Poggesi E, Leonardi A, Melchiorre C.

J Med Chem. 2002 Apr 11;45(8):1633-43.

PMID:
11931617
40.

Deoxamuscaroneoxime derivatives as useful muscarinic agonists to explore the muscarinic subsite: demox, a modulator of orthosteric and allosteric sites at cardiac muscarinic M2 receptors.

Angeli P, Marucci G, Buccioni M, Piergentili A, Giannella M, Quaglia W, Pigini M, Cantalamessa F, Nasuti C, Novi F, Maggio R, Qasem AR, Spampinato S.

Life Sci. 2002 Feb 8;70(12):1427-46.

PMID:
11883718
41.

Alpha2-adrenoreceptors profile modulation and high antinociceptive activity of (S)-(-)-2-[1-(biphenyl-2-yloxy)ethyl]-4,5-dihydro-1H-imidazole.

Gentili F, Bousquet P, Brasili L, Caretto M, Carrieri A, Dontenwill M, Giannella M, Marucci G, Perfumi M, Piergentili A, Quaglia W, Rascente C, Pigini M.

J Med Chem. 2002 Jan 3;45(1):32-40.

PMID:
11754577
42.

Chain-lengthened and imidazoline analogues of nicotine.

Ferretti G, Dukat M, Giannella M, Piergentili A, Pigini M, Quaglia W, Damaj MI, Martin BR, Glennon RA.

Bioorg Med Chem Lett. 2000 Dec 4;10(23):2665-8.

PMID:
11128647
43.

Structure-activity relationship at alpha-adrenergic receptors within a series of imidazoline analogues of cirazoline.

Pigini M, Quaglia W, Gentili F, Marucci G, Cantalamessa F, Franchini S, Sorbi C, Brasili L.

Bioorg Med Chem. 2000 May;8(5):883-8.

PMID:
10882000
44.

Coupling of I(1) imidazoline receptors to the cAMP pathway: studies with a highly selective ligand, benazoline.

Greney H, Ronde P, Magnier C, Maranca F, Rascente C, Quaglia W, Giannella M, Pigini M, Brasili L, Lugnier C, Bousquet P, Dontenwill M.

Mol Pharmacol. 2000 Jun;57(6):1142-51.

PMID:
10825384
45.

Alpha 1-adrenoreceptor antagonists bearing a quinazoline or a benzodioxane moiety.

Melchiorre C, Angeli P, Bolognesi ML, Chiarini A, Giardinà D, Gulini U, Leonardi A, Marucci G, Minarini A, Pigini M, Quaglia W, Rosini M, Tumiatti V.

Pharm Acta Helv. 2000 Mar;74(2-3):181-90. Review. No abstract available.

PMID:
10812956
46.

Hyperphagic effect of novel compounds with high affinity for imidazoline I(2) binding sites.

Polidori C, Gentili F, Pigini M, Quaglia W, Panocka I, Massi M.

Eur J Pharmacol. 2000 Mar 24;392(1-2):41-9.

PMID:
10748271
47.

Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.

Quaglia W, Pigini M, Piergentili A, Giannella M, Marucci G, Poggesi E, Leonardi A, Melchiorre C.

J Med Chem. 1999 Jul 29;42(15):2961-8.

PMID:
10425105
48.

2-(2-Phenylcyclopropyl)imidazolines: reversed enantioselective interaction at I(1) and I(2) imidazoline receptors.

Quaglia W, Bousquet P, Pigini M, Carotti A, Carrieri A, Dontenwill M, Gentili F, Giannella M, Maranca F, Piergentili A, Brasili L.

J Med Chem. 1999 Jul 29;42(15):2737-40. No abstract available.

PMID:
10425083
49.

Binding of tracizolines to the imidazoline receptor. Role of lipophilicity in quantitative structure-activity relationship models.

Pigini M, Bousquet P, Brasili L, Carrieri A, Dontenwill M, Gentili F, Giannella M, Leonetti F, Piergentili A, Quaglia W, Carotti A.

Ann N Y Acad Sci. 1999 Jun 21;881:118-22. No abstract available.

PMID:
10415907
50.

An unexpected central hypertensive effect of the new imidazoline compound benazoline.

Bruban V, Feldman J, Dontenwill M, Greney H, Brasili L, Giannella M, Pigini M, Bousquet P.

Ann N Y Acad Sci. 1999 Jun 21;881:102-5. No abstract available.

PMID:
10415903

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