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21 results on '"Brizzi V"'

1. In vitro and in vivo pharmacology of synthetic olivetol- or resorcinol-derived cannabinoid receptor ligands

Author

CASCIO MG, BISOGNO T, PALAZZO, Enza, THOMAS A, VAN DER STELT M, BRIZZI A, DE NOVELLIS, Vito, NOVELLIS V, MARABESE, Ida, ROSS R, VAN DE DOELEN T, BRIZZI V, PERTWEE R, MAIONE, Sabatino, DI MARZO V., Cascio, Mg, Bisogno, T, Palazzo, Enza, Thomas, A, VAN DER STELT, M, Brizzi, A, DE NOVELLIS, Vito, Novellis, V, Marabese, Ida, Ross, R, VAN DE DOELEN, T, Brizzi, V, Pertwee, R, Maione, Sabatino, and DI MARZO, V.

Subjects
Male, Pain Threshold, Analgesics, Dose-Response Relationship, Drug, Action Potentials, Pain, CHO Cells, Resorcinols, Ligands, Transfection, Research Papers, Amides, Rats, Receptor, Cannabinoid, CB2, Mice, Cricetulus, Receptor, Cannabinoid, CB1, Guanosine 5'-O-(3-Thiotriphosphate), Cricetinae, Cyclic AMP, Animals, Rats, Wistar, Adenylyl Cyclases, Brain Stem, Pain Measurement
Abstract

We have previously reported the development of CB-25 and CB-52, two ligands of CB1 and CB2 cannabinoid receptors. We assessed here their functional activity.The effect of the two compounds on forskolin-induced cAMP formation in intact cells or GTP-gamma-S binding to cell membranes, and their action on nociception in vivo was determined.CB-25 enhanced forskolin-induced cAMP formation in N18TG2 cells (EC50 approximately 20 nM, max. stimulation = 48%), behaving as an inverse CB1 agonist, but it stimulated GTP-gamma-S binding to mouse brain membranes, behaving as a partial CB1 agonist (EC50 =100 nM, max. stimulation = 48%). At human CB1 receptors, CB-25 inhibited cAMP formation in hCB1-CHO cells (EC50 = 1600 nM, max. inhibition = 68% of CP-55,940 effect). CB-52 inhibited forskolin-induced cAMP formation by N18TG2 cells (IC50 = 450 nM, max. inhibition = 40%) and hCB1-CHO cells (EC50 = 2600 nM, max. inhibition = 62% of CP-55,940 effect), and stimulated GTP-gamma-S binding to mouse brain membranes (EC50 = 11 nM, max. stimulation approximately 16%). Both CB-25 and CB-52 showed no activity in all assays of CB2-coupled functional activity and antagonized CP55940-induced stimulation of GTP-gamma-S binding to hCB2-CHO cell membranes. In vivo, both compounds, administered i.p., produced dose-dependent nociception in the plantar test carried out in healthy rats, and antagonised the anti-nociceptive effect of i.p. WIN55,212-2. In the formalin test in mice, however, the compounds counteracted both phases of formalin-induced nociception.CB-25 and CB-52 behave in vitro mostly as CB1 partial agonists and CB2 neutral antagonists, whereas their activity in vivo might depend on the tonic activity of cannabinoid receptors.

Published
2006

2. Management of patients with infected aortic prosthesis. Analysis of 164 patients from the Italian Registry of Graft Infection (IRGI) [Modalità di trattamento nei pazienti con infezione di protesi aortica. Analisi di 164 pazienti dal R

Author

Speziale F, Rizzo L, Schioppa A, Brizzi V, Fiorani P, Cao P, Zannetti S, Parlani G, Agrifoglio G, Alagni G, Alberti D, Alò F, Bacciu P, Biglioli P, Bortolani E, Brotzu G, Caldarelli G, Canova G, Cavaliere P, Costarella S, Crescenzi B, D'Addato M, De Blasis G, De Donato G, Deriu G, Di Cintio V, Florena M, Franchi A, Mangialardi N, Moretti V, Muzj A, Odero A, Palombo D, Pedeferri G, Pistolere GR, Placida C, Ponzio E, Pratesi C, Puttini M, Rabitti C, Setacci C, Spartera C, Spigonardo F, Stancanelli V, Valitutti P, Vecchiati E, Vecchioni R., CHIESA , ROBERTO, Speziale, F, Rizzo, L, Schioppa, A, Brizzi, V, Fiorani, P, Cao, P, Zannetti, S, Parlani, G, Agrifoglio, G, Alagni, G, Alberti, D, Alò, F, Bacciu, P, Biglioli, P, Bortolani, E, Brotzu, G, Caldarelli, G, Canova, G, Cavaliere, P, Chiesa, Roberto, Costarella, S, Crescenzi, B, D'Addato, M, De Blasis, G, De Donato, G, Deriu, G, Di Cintio, V, Florena, M, Franchi, A, Mangialardi, N, Moretti, V, Muzj, A, Odero, A, Palombo, D, Pedeferri, G, Pistolere, Gr, Placida, C, Ponzio, E, Pratesi, C, Puttini, M, Rabitti, C, Setacci, C, Spartera, C, Spigonardo, F, Stancanelli, V, Valitutti, P, Vecchiati, E, and Vecchioni, R.

Published
2002

8. Modalità di trattamento nei pazienti con infezione di protesi aortica. Analisi di 164 pazienti dal Registro Italiano delle Infezioni Protesiche (IRGI)

Author

Speziale, F., Rizzo, L., Schioppa, A., Brizzi, V., Fiorani, P., Cao, P., Zannetti, S., Parlani, G., Agrifoglio, G., Alagni, G., Alberti, D., Alò, F., Bacciu, P., Biglioli, P., Bortolani, E., Brotzu, G., Caldarelli, G., Canova, G., Cavaliere, P., Chiesa, R., Costarella, S., Crescenzi, B., D'Addato, M., De Blasis, G., De Donato, G., Deriu, G., Di Cintio, V., Florena, M., Franchi, A., Mangialardi, N., Moretti, V., Muzj, A., Odero, A., Palombo, Domenico, Pedeferri, G., Pistolere, G. R., Placida, C., Ponzio, E., Pratesi, C., Puttini, M., Rabitti, C., Setacci, C., Spartera, C., Spigonardo, F., Stancanelli, V., Valitutti, P., Vecchiati, E., and Vecchioni, R.

Subjects
Postoperative complications, Prosthesis related infections, diagnosis, Aortic diseases, diagnosis, Intestinal fistula, diagnosis, Prosthesis related infections, diagnosis, Cardiology and Cardiovascular Medicine, Aortic diseases, Intestinal fistula
Published
2002

12. Rifamycins as inhibitors of HIV-1

Author

Bartolucci, C., Cellai, L., DI FILIPPO, P., Iannelli, M. A., Segre, A. L., Brufani, Mario, Filocamo, Luigi, Bianco, Armandodoriano, Guiso, Marcella, Brizzi, V., Benedetto, A., and DI CARO, A.

Published
1993

18. Management of patients with infected aortic prosthesis. Analysis of 164 patients from the Italian Registry of Graft Infection (IRGI) | Modalità di trattamento nei pazienti con infezione di protesi aortica. Analisi di 164 pazienti dal Registro Italiano delle Infezioni Protesiche (IRGI)

Author

Speziale, F., Rizzo, L., Schioppa, A., Brizzi, V., Fiorani, P., Cao, P., Zannetti, S., Parlani, G., Agrifoglio, G., Alagni, G., Alberti, D., Alò, F., Bacciu, P., Biglioli, P., Bortolani, E., Brotzu, G., Caldarelli, G., Canova, G., Cavaliere, P., Chiesa, R., Costarella, S., Crescenzi, B., D Addato, M., Blasis, G., Donato, G., Deriu, G., Di Cintio, V., Florena, M., Franchi, A., Mangialardi, N., Moretti, V., Muzj, A., Odero, A., Palombo, D., Pedeferri, G., Pistolere, G. R., Placida, C., Ponzio, E., Pratesi, C., Puttini, M., Rabitti, C., Setacci, C., Carlo SPARTERA, Spigonardo, F., Stancanelli, V., Valitutti, P., Vecchiati, E., and Vecchioni, R.

19. Thirty-day Outcome of Delayed Versus Early Management of Symptomatic Carotid Stenosis

Author

Gérard Sassoust, Sandro Lepidi, Vincenzo Brizzi, Xavier Berard, Eric Ducasse, Stéphanie Roullet, Dominique Midy, Emilie Charmoille, Charmoille, E., Brizzi, V., Lepidi, S., Sassoust, G., Roullet, S., Ducasse, E., Midy, D., and Berard, X.

Subjects
Male, medicine.medical_specialty, Time Factors, SURGERY, medicine.medical_treatment, Myocardial Infarction, MULTICENTER, Time-to-Treatment, RETROSPECTIVE ANALYSIS, Risk Factors, THIRTY-DAY, medicine, Humans, Carotid Stenosis, Symptom onset, Myocardial infarction, NONDISABLING STROKE, Stroke, EARLY ENDARTERECTOMY, Aged, Retrospective Studies, Endarterectomy, Aged, 80 and over, Endarterectomy, Carotid, business.industry, Mortality rate, ARTERY STENOSIS, Retrospective cohort study, General Medicine, Middle Aged, medicine.disease, TRANSIENT ISCHEMIC ATTACK, PROCEDURAL RISK, NEUROLOGIC DEFICITS, SAFE, Surgery, Stenosis, Treatment Outcome, Practice Guidelines as Topic, Female, Guideline Adherence, Cardiology and Cardiovascular Medicine, business
Abstract

Background: The aim of this study was to compare outcomes of early (

Published
2015

20. Structure-affinity relationships and pharmacological characterization of new alkyl-resorcinol cannabinoid receptor ligands: Identification of a dual cannabinoid receptor/TRPA1 channel agonist

Author

Antonella Brizzi, Vincenzo Di Marzo, Federico Corelli, Livio Luongo, Roger G. Pertwee, Vittorio Brizzi, Francesca Aiello, Pietro Marini, Sabatino Maione, Maria Grazia Cascio, Stefania Lamponi, Luciano De Petrocellis, Alessia Ligresti, Brizzi, A, Aiello, F, Marini, P, Cascio, Mg, Corelli, F, Brizzi, V, De Petrocellis, L, Ligresti, A, Luongo, Livio, Lamponi, S, Maione, Sabatino, Pertwee, Rg, and Di Marzo, V.

Subjects
Structure-affinity relationships, Male, Nociception, Cannabinoid receptor, Clinical Biochemistry, Pharmaceutical Science, Pharmacology, Ligands, Biochemistry, Alkyl-resorcinol derivatives, Receptor, Cannabinoid, CB2, Mice, Transient Receptor Potential Channels, Receptor, Cannabinoid, CB1, Fatty acid amide hydrolase, Cannabinoid ligands, Drug Discovery, Cannabinoid receptor type 2, Transient receptor potential ankyrin type-1 channel, Receptor, TRPA1 Cation Channel, Cells, Cultured, Pain Measurement, Analgesics, Molecular Structure, Chemistry, Endocannabinoid system, Molecular Medicine, lipids (amino acids, peptides, and proteins), psychological phenomena and processes, Agonist, medicine.drug_class, Stereochemistry, Cell Survival, Pain, Nerve Tissue Proteins, CHO Cells, Structure-Activity Relationship, Cricetulus, medicine, Inverse agonist, Animals, Humans, Molecular Biology, Lipid modulators, Dose-Response Relationship, Drug, Organic Chemistry, Anandamide, Resorcinols, Monoacylglycerol lipase, NIH 3T3 Cells, Calcium Channels, Endocannabinoids
Abstract

In our ongoing program aimed at deeply investigating the endocannabinoid system (ES), a set of new alkyl-resorcinol derivatives was prepared focusing on the nature and the importance of the carboxamide functionality. Binding studies on CB 1 and CB 2 receptors, monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH) showed that some of the newly developed compounds behaved as very potent cannabinoid receptor ligands ( K i in the nanomolar range) while, however, none of them was able to inhibit MAGL and/or FAAH. Derivative 11 was a potent CB 1 and CB 2 ligand, with K i values similar to WIN 55,212, exhibiting a CB 1 and CB 2 agonist profile in vitro. In the formalin test of peripheral acute and inflammatory pain in mice, this compound showed a weak and delayed antinociceptive effect against the second phase of the nocifensive response, exhibiting, interestingly, a quite potent transient receptor potential ankyrin type-1 (TRPA1) channel agonist activity. Moreover, derivative 14 , characterized by lower affinity but higher CB 2 selectivity than 11 , proved to behave as a weak CB 2 competitive inverse agonist.

Published
2014
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21. Synthesis of nucleosidyl rifamycins as inhibitors of human immunodeficiency virus type 1

Author

C. Bartolucci, Vittorio Brizzi, L. Cellai, Luisa Mannina, Luigi Filocamo, A. Di Caro, M. Marzano, Arrigo Benedetto, Mario Brufani, Samantha Messina, Bartolucci, C, Cellai, L, Mannina, L, Marzano, M, Brufani, M, Filocamo, L, Messina, S, Brizzi, V, and Benedetto, A AND DI CARO A

Subjects
0301 basic medicine, Stereochemistry, 030106 microbiology, Rifamycins, Biology, 01 natural sciences, 03 medical and health sciences, Zidovudine, chemistry.chemical_compound, HIV, non-nucleoside reverse transcriptase inhibitors, rifamycins, medicine, chemistry.chemical_classification, virus diseases, Rifamycin, General Medicine, Prodrug, Reverse transcriptase, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, Enzyme, chemistry, Biochemistry, Thymidine, Nucleoside, medicine.drug
Abstract

In the search for potential nucleoside/non-nucleoside mixed type inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase, we synthesized a new set of rifamycin S derivatives, containing AZT connected via its hydroxyl at 5′ C, through a spacer, to the third C of rifamycin S. The length of the spacer was eight, nine or 14 atoms. Rifamycin S was also used in its 21, 23-O, O-isopropylidene derivative form, and in one case thymidine replaced AZT. These nucleosidyl rifamycins were weak inhibitors of isolated HIV-1 reverse transcriptase. The inhibitory power was weak most probably because their large molecular volume hindered the inhibition process. With the exception of the thymidine derivative, the AZT derivatives, at concentrations in the range 0.04–0.07 μM, proved non-toxic and inhibited the replication of HIV-1 in C8166 T lymphocytes. This activity appears to be owing to AZT released by the derivatives upon hydrolysis in solution. The present compounds require further development as mixed type reverse transcriptase inhibitors and can be considered non-toxic lipophilic prodrugs of AZT.

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