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144 results on '"Cacciaguerra S"'

1. Turning Open Science and Open Innovation into reality

Author

Bassini S., Boccali T., Cacciaguerra S., Castelli D., Celino M., Cocco M., Di Giorgio S., Giorgetti A., Kourousias G., Locati M., Lucchesi D, Migliori S., Pappalardo G., Perini L., Petrillo C., Pugliese R., Rossi G., Ruggieri F., Smareglia R., and Tanlongo F.

Subjects
EOSC, FAIR Principles, EOSC Research and Innovation Agenda, ICDI, European Open Science Cloud
Abstract

This document summarises the views expressed by the Italian Computing and Data Initiative (ICDI) in response to the open consultation for the EOSC Strategic Research and Innovation Agenda (SRIA), closed on the 31st of August. It provides insightful input and suggestions about the current draft of the SRIA document shared with the wider EOSC community, with the aim of helping to shape the future vision of the European Open Science Cloud.

Published
2020

6. Tetraamines as lead compounds for the design of neurotransmitter receptor ligands:Focus on α-adrenergic and muscarinic receptors recognition

Author

Melchiorre, C., primary, Angeli, P., additional, Bolognesi, M.L., additional, Budriesi, R., additional, Cacciaguerra, S., additional, Chiarini, A., additional, Crucianelli, M., additional, Giardina, D., additional, Gulini, U., additional, Marucci, G., additional, Minarini, A., additional, Spampinato, S., additional, and Tumiatti, V., additional

Published
1996
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8. Abstracts of the 33rd International Austrian Winter Symposium : Zell am See, Austria. 24-27 January 2018

Author

Binzel, K, Adelaja, A, Wright, CL, Scharre, D, Zhang, J, Knopp, MV, Teoh, EJ, Bottomley, D, Scarsbrook, A, Payne, H, Afaq, A, Bomanji, J, van As, N, Chua, S, Hoskin, P, Chambers, A, Cook, GJ, Warbey, VS, Chau, A, Ward, P, Miller, MP, Stevens, DJ, Wilson, L, Gleeson, FV, Scheidhauer, K, Seidl, C, Autenrieth, M, Bruchertseifer, F, Apostolidis, C, Kurtz, F, Horn, T, Pfob, C, Schwaiger, M, Gschwend, J, D'Alessandria, C, Morgenstern, A, Uprimny, C, Kroiss, A, Decristoforo, C, von Guggenberg, E, Nilica, B, Horninger, W, Virgolini, I, Rasul, S, Poetsch, N, Woehrer, A, Preusser, M, Mitterhauser, M, Wadsak, W, Widhalm, G, Mischkulnig, M, Hacker, M, Traub-Weidinger, T, Wuthrick, EJ, Miller, ED, Maniawski, P, Rep, S, Hocevar, M, Vaupotic, J, Zdesar, U, Zaletel, K, Lezaic, L, Mairinger, S, Filip, T, Sauberer, M, Flunkert, S, Wanek, T, Stanek, J, Okamura, N, Langer, O, Kuntner, C, Fornito, MC, Balzano, R, Di Martino, V, Cacciaguerra, S, Russo, G, Seifert, D, Kleinova, M, Cepa, A, Ralis, J, Hanc, P, Lebeda, O, Mosa, M, Vandenberghe, S, Mikhaylova, E, Borys, D, Viswanath, V, Stockhoff, M, Efthimiou, N, Caribe, P, Van Holen, R, Karp, JS, Haller, PM, Farhan, C, Piackova, E, Jäger, B, Knoll, P, Kiss, A, Podesser, BK, Wojta, J, Huber, K, Mirzaei, S, Traxl, A, Komposch, K, Glitzner, E, Sibilia, M, Russello, M, Sorko, S, Gallowitsch, HJ, Kohlfuerst, S, Matschnig, S, Rieser, M, Sorschag, M, Lind, P, Ležaič, L, Žibert, J, Frelih, N, Šuštar, S, Baum, RP, Langbein, T, Singh, A, Shahinfar, M, Schuchardt, C, Volk, GF, Kulkarni, HR, Di Martino, GV, Thomson, WH, Kudlacek, M, Karik, M, Rieger, H, Pokieser, W, Glaser, K, Petz, V, Tugendsam, C, Buchinger, W, Schmoll-Hauer, B, Schenk, IP, Rudolph, K, Krebs, M, Zettinig, G, Zoufal, V, Krohn, M, Pahnke, J, Weitzer, F, Pernthaler, B, Salamon, S, Aigner, R, Koranda, P, Henzlová, L, Kamínek, M, Váchalová, M, Bachleda, P, Summer, D, Garousi, J, Oroujeni, M, Mitran, B, Andersson, KG, Vorobyeva, A, Löfblom, JN, Orlova, A, Tolmachev, V, Kaeopookum, P, Orasch, T, Lechner, B, Petrik, M, Novy, Z, Rangger, C, and Haas, H

Published
2018

11. Italian experience of pediatric liver transplantation

Author

Guariso, G, Lodde, V, Visonà Dalla Pozza, L, Manea, S, Salmaso, L, Facchin, P, Alberti, D, Baldassarre, M, Baldi, M, Barbera, C, Balli, F, Viola, L, Brolese, A, D'Antiga, L, Zancan, L, Cacciaguerra, S, Campanozzi, A, Castellano, E, Di Cosmo, R, Iorio, R, Vajro, P, Vegnente, A, Frediani, T, Marcellini, M, Nobili, V, Pacifico, L, Gridelli, B, Sartorelli, M, Torre, G, Maggiore, G, Masseria, R, Nebbia, G, Pastore, M, Resti, M, Guariso G, Lodde V, Visonà Dalla Pozza L, Manea S, Salmaso L, Facchin P, Alberti D, Baldassarre M, Baldi M, Barbera C, Balli F, Viola L, Brolese A, D'Antiga L, Zancan L, Cacciaguerra S, Campanozzi A, Castellano E, Di Cosmo R, Iorio R, Vajro P, Vegnente A, Frediani T, Marcellini M, Nobili V, Pacifico L, Gridelli B, Sartorelli M, Torre G, Maggiore G, Masseria R, Nebbia G, Pastore M, Resti M, Guariso, G, Lodde, V, Visonà Dalla Pozza, L, Manea, S, Salmaso, L, Facchin, P, Alberti, D, Baldassarre, M, Baldi, M, Barbera, C, Balli, F, Viola, L, Brolese, A, D'Antiga, L, Zancan, L, Cacciaguerra, S, Campanozzi, A, Castellano, E, Di Cosmo, R, Iorio, R, Vajro, P, Vegnente, A, Frediani, T, Marcellini, M, Nobili, V, Pacifico, L, Gridelli, B, Sartorelli, M, Torre, G, Maggiore, G, Masseria, R, Nebbia, G, Pastore, M, Resti, M, Guariso G, Lodde V, Visonà Dalla Pozza L, Manea S, Salmaso L, Facchin P, Alberti D, Baldassarre M, Baldi M, Barbera C, Balli F, Viola L, Brolese A, D'Antiga L, Zancan L, Cacciaguerra S, Campanozzi A, Castellano E, Di Cosmo R, Iorio R, Vajro P, Vegnente A, Frediani T, Marcellini M, Nobili V, Pacifico L, Gridelli B, Sartorelli M, Torre G, Maggiore G, Masseria R, Nebbia G, Pastore M, and Resti M

Abstract

The SIGENP Group has created an Italian Liver Transplantation database. The study considers all patients under 18 yr of age on the waiting list or transplanted between 1984 and 2005. Demographic and clinical data were collected and a descriptive analysis was conducted. Kaplan-Meier survival curves were calculated and Cox's proportional-hazards regression analysis were performed to identify predictors of death after transplantation. Twenty-two Italian centers took part and data were collected on 622 cases: only 53.8% of the transplants performed up until 1998 were carried out in Italy, while this was true of 97.7% of the operations performed between 1999 and 2005. Recipient survival curve analysis revealed one-, two- and five-yr survival rates of 88, 87 and 84%, respectively, and a significant improvement in survival after 1998 (p = 0.0322). Cox's analysis identified the following risk factors for death after liver transplantation, i.e. transplantation before 1998, neoplasms or fulminant hepatic failure as indications, being in intensive care at the time of transplantation and retransplantation. The center where the transplant is performed also revealed an influence on patient survival. Thanks to a better patient follow-up and more cooperation between specialists, the mean survival after liver transplantation is improving and Italian children can be transplanted in Italy.

Published
2007

12. Italian experience of pediatric liver transplantation

Author

Guariso, Graziella, Visonà Dalla Pozza, Laura, Manea, Silvia, Salmaso, Laura, Lodde, Veronica, Facchin, Paola, Alberti, D., Baldassarre, M., Baldi, M., Balli, F., Barbera, C., Brolese, A., Cacciaguerra, S., Campanozzi, A., Castellano, E., D'Antiga, L., Di Cosmo, R., Frediani, T., Gridelli, B., Iorio, R., Maggiore, G., Marcellini, M., Masseria, R., Nebbia, G., Nobili, V., Pacifico, L., Pastore, M., Resti, M., Sartorelli, M., Torre, G., Vajro, P., Vegnente, A., Viola, L., Zancan, L., Guariso, G., Visonà Dalla Pozza, L., Manea, S., Salmaso, L., Lodde, V., Facchin, P., Alberti, D., Baldassarre, M., Baldi, M., Balli, F., Barbera, C., Brolese, A., Cacciaguerra, S., Campanozzi, A., Castellano, E., D'Antiga, L., Di Cosmo, R., Frediani, T., Gridelli, B., Iorio, Raffaele, Maggiore, G., Marcellini, M., Masseria, R., Nebbia, G., Nobili, V., Pacifico, L., Pastore, M., Resti, M., Sartorelli, M., Torre, G., Vajro, Pietro, Vegnente, Angela, Viola, L., and Zancan, L.

Subjects
medicine.medical_specialty, Time Factors, Databases, Factual, Adolescent, Waiting Lists, medicine.medical_treatment, Pediatric liver transplantation, Child, Follow-Up Studies, Humans, Italy, Liver Diseases, Liver Transplantation, Multivariate Analysis, Proportional Hazards Models, Retrospective Studies, Survival Analysis, Survivors, Pediatrics, Perinatology and Child Health, Transplantation, LIVER TRANPLANTATION, CHILDREN, Socio-culturale, Liver transplantation, Pediatrics, Databases, Fulminant hepatic failure, Internal medicine, Intensive care, medicine, Survival analysis, Factual, business.industry, Patient survival, Perinatology and Child Health, Surgery, El Niño, Waiting list, business
Abstract

The SIGENP Group has created an Italian Liver Transplantation database. The study considers all patients under 18 yr of age on the waiting list or transplanted between 1984 and 2005. Demographic and clinical data were collected and a descriptive analysis was conducted. Kaplan-Meier survival curves were calculated and Cox's proportional-hazards regression analysis were performed to identify predictors of death after transplantation. Twenty-two Italian centers took part and data were collected on 622 cases: only 53.8% of the transplants performed up until 1998 were carried out in Italy, while this was true of 97.7% of the operations performed between 1999 and 2005. Recipient survival curve analysis revealed one-, two- and five-yr survival rates of 88, 87 and 84%, respectively, and a significant improvement in survival after 1998 (p = 0.0322). Cox's analysis identified the following risk factors for death after liver transplantation, i.e. transplantation before 1998, neoplasms or fulminant hepatic failure as indications, being in intensive care at the time of transplantation and retransplantation. The center where the transplant is performed also revealed an influence on patient survival. Thanks to a better patient follow-up and more cooperation between specialists, the mean survival after liver transplantation is improving and Italian children can be transplanted in Italy.

Published
2007

13. Rapid response to the earthquake emergency of May 2012 in the Po Plain, northern Italy

Author

Moretti, M., Abruzzese, L., Abu Zeid, N., Augliera, P., Azzara, R. M., Barnaba, C., Benedetti, L., Bono, A., Bordoni, P., Boxberger, T., Bucci, A., Cacciaguerra, S., Calo, M., Cara, F., Carannante, S., Cardinale, V., Castagnozzi, A., Cattaneo, M., Cavaliere, A., Cecere, G., Chiarabba, C., Chiaraluce, L., Ciaccio, M. G., Cogliano, R., Colasanti, G., Colasanti, M., Cornou, Cécile, Courboulex, F., Criscuoli, F., Cultrera, G., D'Alema, E., D'Ambrosio, C., Danesi, S., De Gori, P., Delladio, A., De Luca, G., Demartin, M., Di Giulio, G., Dorbath, Catherine, Ercolani, E., Faenza, L., Falco, L., Fiaschi, A., Ficeli, P., Fodarella, A., Franceschi, D., Franceschina, G., Frapiccini, M., Frogneux, M., Giovani, L., Govoni, A., Improta, L., Jacques, E., Ladina, C., Langlaude, P., Lauciani, V., Lolli, B., Lovati, S., Lucente, F. P., Luzi, L., Mandiello, A., Marcocci, C., Margheriti, L., Marzorati, S., Massa, M., Mazza, S., Mercerat, D., Milana, G., Minichiello, F., Molli, G., Monachesi, G., Morelli, A., Moschillo, R., Pacor, F., Piccinini, D., Piccolini, U., Pignone, M., Pintore, S., Pondrelli, S., Priolo, E., Pucillo, S., Quintiliani, M., Riccio, G., Romanelli, M., Rovelli, A., Salimbeni, S., Sandri, L., Selvaggi, G., Serratore, A., Silvestri, M., Valoroso, L., Van der Woerd, J., Vannucci, G., Zaccarelli, L., Sismologie (IPGS) (IPGS-Sismologie), Institut de physique du globe de Strasbourg (IPGS), Université de Strasbourg (UNISTRA)-Centre National de la Recherche Scientifique (CNRS)-Institut national des sciences de l'Univers (INSU - CNRS)-Université de Strasbourg (UNISTRA)-Centre National de la Recherche Scientifique (CNRS)-Institut national des sciences de l'Univers (INSU - CNRS), Géosciences Environnement Toulouse (GET), Institut national des sciences de l'Univers (INSU - CNRS)-Centre National de la Recherche Scientifique (CNRS)-Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Observatoire Midi-Pyrénées (OMP), Météo France-Centre National d'Études Spatiales [Toulouse] (CNES)-Université Fédérale Toulouse Midi-Pyrénées-Centre National de la Recherche Scientifique (CNRS)-Institut de Recherche pour le Développement (IRD)-Météo France-Centre National d'Études Spatiales [Toulouse] (CNES)-Centre National de la Recherche Scientifique (CNRS)-Institut de Recherche pour le Développement (IRD), Université de Strasbourg (UNISTRA)-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National de la Recherche Scientifique (CNRS)-Université de Strasbourg (UNISTRA)-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National de la Recherche Scientifique (CNRS), Institut de Recherche pour le Développement (IRD)-Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Université de Toulouse (UT)-Institut national des sciences de l'Univers (INSU - CNRS)-Observatoire Midi-Pyrénées (OMP), and Université de Toulouse (UT)-Université de Toulouse (UT)-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National d'Études Spatiales [Toulouse] (CNES)-Centre National de la Recherche Scientifique (CNRS)-Météo-France -Institut de Recherche pour le Développement (IRD)-Institut national des sciences de l'Univers (INSU - CNRS)-Centre National d'Études Spatiales [Toulouse] (CNES)-Centre National de la Recherche Scientifique (CNRS)-Météo-France -Centre National de la Recherche Scientifique (CNRS)

Subjects
010504 meteorology & atmospheric sciences, [SDU.STU.GP]Sciences of the Universe [physics]/Earth Sciences/Geophysics [physics.geo-ph], [SDE.MCG]Environmental Sciences/Global Changes, Environmental Seismic Intensity scale, [PHYS.PHYS.PHYS-GEO-PH]Physics [physics]/Physics [physics]/Geophysics [physics.geo-ph], 550 - Earth sciences, lcsh:QC851-999, Surveys, 010502 geochemistry & geophysics, 01 natural sciences, Earthquake scenario, Earthquake simulation, Urban seismic risk, measurements and monitoring, Instruments and techniques, Seismological data, Emilia 2012 sequence, Sismiko, Seismic risk, 0105 earth and related environmental sciences, Seismic microzonation, lcsh:QC801-809, Mitigation of seismic motion, Rapid-response, Temporary Seismic Network, lcsh:Geophysics. Cosmic physics, Geophysics, Seismic hazard, 13. Climate action, lcsh:Meteorology. Climatology, Waveform data, Geology, Seismology
Abstract

Rapid-response seismic networks are an important element in the response to seismic crises. They temporarily improve the detection performance of permanent monitoring systems during seismic sequences. The improvement in earthquake detection and location capabilities can be important for decision makers to assess the current situation, and can provide invaluable data for scientific studies related to hazard, tectonics and earthquake physics. Aftershocks and the clustering of the locations of seismic events help to characterize the dimensions of the causative fault. Knowing the number, size and timing of the aftershocks or the clustering seismic events can help in the foreseeing of the characteristics of future seismic sequences in the same tectonic environment. Instrumental rapid response requires a high degree of preparedness. A mission in response to a magnitude (Ml) 6 event with a rupture length of a few tens of kilometers might involve the deployment within hours to days of 30-50 seismic stations in the middle of a disaster area of some hundreds of square kilometers, and the installation of an operational center to help in the logistics and communications. When an earthquake strikes in a populated area, which is almost always the case in Italy, driving the relevant seismic response is more difficult. […]

Published
2012

14. A cross-sectional nationwide survey on esophageal atresia and tracheoesophageal fistula

Author

Pini Prato, A., primary, Carlucci, M., additional, Bagolan, P., additional, Gamba, P.G., additional, Bernardi, M., additional, Leva, E., additional, Paradies, G., additional, Manzoni, C., additional, Noccioli, B., additional, Tramontano, A., additional, Jasonni, V., additional, Vaccarella, F., additional, De Pascale, S., additional, Alberti, D., additional, Riccipetitoni, G., additional, Falchetti, D., additional, Caccia, F., additional, Pelizzo, G., additional, Schleef, J., additional, Lima, M., additional, Andriolo, P., additional, Franchella, A., additional, Cacciari, A., additional, Caravaggi, F., additional, Federici, S., additional, Andermarcher, M., additional, Perrino, G., additional, Codrich, D., additional, Camoglio, F.S., additional, Chiarenza, F.S., additional, Martino, A., additional, Appignani, A., additional, Briganti, V., additional, Caterino, S., additional, Cozzi, D., additional, Messina, M., additional, Rizzo, A., additional, Liotta, L., additional, Salerno, D., additional, Aceti, M.G.R., additional, Bartoli, F., additional, Romeo, C., additional, Esposito, C., additional, Lelli Chiesa, P.L., additional, Clemente, E., additional, Mascia, L., additional, Cacciaguerra, S., additional, Di Benedetto, V., additional, Licciardi, S., additional, De Grazia, E., additional, Ubertazzi, M., additional, Piazza, G., additional, Mattioli, G., additional, Rossi, F., additional, and Nobili, M., additional

Published
2015
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18. Analysis of the muscarinic receptor subtype mediating inhibition of the neurogenic contractions in rabbit isolated vas deferens by a series of polymethylene tetra-amines

Author

Budriesi, R, Cacciaguerra, S, Di Toro, R, Bolognesi, M L, Chiarini, A, Minarini, A, Rosini, M, Spampinato, S, Tumiatti, V, and Melchiorre, C

Subjects
Male, Receptor, Muscarinic M3, Receptor, Muscarinic M2, Dose-Response Relationship, Drug, Receptor, Muscarinic M4, Receptor, Muscarinic M1, (4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium Chloride, Muscarinic Antagonists, Muscarinic Agonists, Receptors, Muscarinic, Rats, Benzodiazepines, Vas Deferens, Papers, Polyamines, Animals, Humans, Rabbits, Rats, Wistar, Muscle Contraction
Abstract

The pharmacological characteristics of the presynaptic muscarinic receptor subtype, which mediates inhibition of the neurogenic contractions in the prostatic portion of rabbit vas deferens, have been investigated by using a series of polymethylene tetra-amines, which were selected for their ability to differentiate among muscarinic receptor subtypes. It was found that all tetra-amines antagonized McN-A-343-induced inhibition in electrically stimulated rabbit vas deferens in a competitive manner and with affinity values (pA:(2)) ranging between 6.27+/-0.09 (spirotramine) and 8.51+/-0.02 (AM170). Competition radioligand binding studies, using native muscarinic receptors from rat tissues (M(1), cortex; M(2), heart; M(3), submaxillary gland) or from NG 108-15 cells (M(4)) and human cloned muscarinic M(1)-M(4) receptors expressed in CHO-K1 cells, were undertaken with the same tetra-amines employed in functional assays. All antagonists indicated a one-site fit. The affinity estimates (pK:(i)) of tetra-amines calculated in binding assays using native receptors were similar to those obtained using cloned receptors. Among these compounds some displayed selectivity between muscarinic receptor subtypes, indicating that they may be valuable tools in receptor characterization. Spirotramine was selective for M(1) receptors versus all other subtypes (pK:(i) native: M(1), 7.32+/-0.10; M(2), 6.50+/-0.11; M(3), 6.02+/-0.13; M(4), 6.28+/-0.16; pK:(i) cloned: M(1), 7.69+/-0.08; M(2), 6.22+/-0.14; M(3), 6.11+/-0.16; 6.35+/-0.11) whereas CC8 is highly selective for M(2) receptors versus the other subtypes (pK:(i) native: M(1), 7.50+/-0.04; M(2), 9.01+/-0.12; M(3), 6.70+/-0.08; M(4), 7.56+/-0.04; pK:(i) cloned: M(1), 7.90+/-0.20; M(2), 9.04+/-0.08; M(3), 6.40+/-0.07; M(4), 7.40+/-0.04). Furthermore, particularly relevant for this investigation were tetra-amines dipitramine and AM172 for their ability to significantly differentiate M(1) and M(4) receptors. The apparent affinity values (pA:(2)) obtained for tetra-amines in functional studies using the prostatic portion of rabbit vas deferens correlated most closely with the values (pK:(i)) obtained at either native or human recombinant muscarinic M(4) receptors. This supports the view that the muscarinic receptor mediating inhibition of neurogenic contractions of rabbit vas deferens may not belong to the M(1) type but rather appears to be of the M(4) subtype.

Published
2001

24. Smoking, polyuria and impaired vision

Author

Granata, A., primary, Viola, G., additional, Privitera, C., additional, Romeo, G., additional, Cacciaguerra, S., additional, Gaeta, M., additional, Sicurezza, E., additional, and Figuera, M., additional

Published
2007
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26. Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives.

Author

UCL - MD/FARM - Ecole de pharmacie, Ucar, H, Van derpoorten, K, Cacciaguerra, S, Spampinato, S, Stables, J P, Depovere, Paul, Isa, M., Masereel, Bernard, Delarge, J., Poupaert, Jacques, UCL - MD/FARM - Ecole de pharmacie, Ucar, H, Van derpoorten, K, Cacciaguerra, S, Spampinato, S, Stables, J P, Depovere, Paul, Isa, M., Masereel, Bernard, Delarge, J., and Poupaert, Jacques

Abstract

A series of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives were synthesized and evaluated for anticonvulsant activity. The compounds were assayed, intraperitoneally in mice and per os in rats, against seizures induced by maximal electroshock (MES) and pentylenetetrazole (scMet). Neurologic deficit was evaluated by the rotarod test. The compounds were prepared to determine the relationship between the 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives' structures and anticonvulsant activity. Several of these compounds showed significant anticonvulsant activity. Compounds 43 and 45 were the most active of the series against MES-induced seizures with ED50 values of 8.7 and 7.6 mg/kg, respectively. Compound 45 displayed good protection against MES-induced seizures and low toxicity in rats with an oral ED50 of 18.6 mg/kg and a protective index (PI = TD50/ED50) of < 26.9. In vitro receptor binding studies revealed that compounds 43 and 45 bind to sigma 1 receptors with nanomolar affinities.

Published
1998

27. 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives: novel, potent and selective sigma1 receptor ligands.

Author

UCL, Ucar, H, Cacciaguerra, S, Spampinato, S, Van derpoorten, K, Isa, M., Kanyonyo, M, Poupaert, Jacques, UCL, Ucar, H, Cacciaguerra, S, Spampinato, S, Van derpoorten, K, Isa, M., Kanyonyo, M, and Poupaert, Jacques

Abstract

A series of original 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives were evaluated for their affinity at sigma1 and sigma2 receptor subtypes in competition binding experiments, using [3H](+)-pentazocine or [3H]1,3-di-o-tolyl-guanidine (DTG) in the presence of 100 nM (+)-N-allylnormetazocine (NANM) in guinea-pig brain membranes. Several of these derivatives showed preferential selectivity for sigma1 binding sites. Compound 1 [3-(1-piperidinoethyl)-6-propylbenzothiazolin-2-one] emerged as a potent sigma1 receptor ligand (Ki = 0.6 nM) and displayed a moderate selectivity over the sigma2 receptor subtype (Ki for sigma2/Ki for sigma1 = 29). Compounds 2 [3-(1-piperidinopropyl)-6-propanoylbenzothiazolin-2-one] and 3 [3-(1-piperidinopropyl)-6-propanoylbenzoxazolin-2-one] still showed rather high affinities for sigma1 binding sites with Ki values of 2.3 and 8.5 nM, respectively. On the contrary, they had 87- and 58-fold less affinity at sigma2 receptors, respectively. Unlike their potent affinity for sigma binding sites, these compounds had negligible affinity for mu-, delta- and kappa-opioid receptors, 5-HT2, dopamine D2, and muscarinic M2 receptors. Sigma receptor ligands may affect neuronal transmission and display, in animal models, antipsychotic, cognitive, motor, neuroprotective and anticonvulsant activity. Therefore, on the basis of these findings, these novel sigma receptor ligands were assayed, in mice, in three tests: maximal electroshock, subcutaneous pentylenetetrazol and rotarod neurotoxicity. Compound 1, administered intraperitoneally, was the most effective against maximal electroshock-induced seizures and was devoid of significant neurotoxic effects.

Published
1997

44. (+)-cis-N-Ethyleneamino-N-normetazocine Derivatives. Novel and Selective σ Ligands with Antagonist Properties

Author

Ronsisvalle, G., Marrazzo, A., Prezzavento, O., Pasquinucci, L., Vittorio, F., Pittala, V., Pappalardo, M. S., Cacciaguerra, S., and Spampinato, S.

Abstract

A series of (+)-cis-N-normetazocine derivatives has been described, and their affinities for σ1, σ2, and phencyclidine (PCP) sites and opioid, muscarinic (M2), dopamine (D2), and serotonin (5-HT2) receptors were evaluated. The effect of the N-substitution with a substituted ethylamino spacer was investigated. Compounds 8c−11c displayed high affinities for σ1 sites and for opioid receptors. Substitution of the second basic nitrogen either with alkyl or cycloalkyl substituents give compounds (1a−6a) with high affinity and selectivity for σ1 binding sites. Compounds 1a−5a were further characterized in vivo, and their agonist/antagonist activity was evaluated. In mouse, compound 1a and 2a as well as haloperidol suppressed in a dose-related manner the stereotyped behavior induced by (+)-SKF 10,047. Compounds 3a−5a and (+)-pentazocine do not affect the stereotyped behavior induced by ip injection of (+)-SKF 10,047. Therefore, from this series of compounds we identified potent and selective σ1 ligands which might prove useful to unveil the functional role of σ1 sites.

Published
1998

45. Synthesis and Anticonvulsant Activity of 2(3H)-Benzoxazolone and 2(3H)-Benzothiazolone Derivatives

Author

Ucar, H., derpoorten, K. Van, Cacciaguerra, S., Spampinato, S., Stables, J. P., Depovere, P., Isa, M., Masereel, B., Delarge, J., and Poupaert, J. H.

Abstract

A series of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives were synthesized and evaluated for anticonvulsant activity. The compounds were assayed, intraperitoneally in mice and per os in rats, against seizures induced by maximal electroshock (MES) and pentylenetetrazole (scMet). Neurologic deficit was evaluated by the rotarod test. The compounds were prepared to determine the relationship between the 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives' structures and anticonvulsant activity. Several of these compounds showed significant anticonvulsant activity. Compounds 43 and 45 were the most active of the series against MES-induced seizures with ED50 values of 8.7 and 7.6 mg/kg, respectively. Compound 45 displayed good protection against MES-induced seizures and low toxicity in rats with an oral ED50 of 18.6 mg/kg and a protective index (PI = TD50/ED50) of &lt;26.9. In vitro receptor binding studies revealed that compounds 43 and 45 bind to σ1 receptors with nanomolar affinities.

Published
1998

46. Universal Template Approach to Drug Design:  Polyamines as Selective Muscarinic Receptor Antagonists

Author

Bolognesi, M. L., Minarini, A., Budriesi, R., Cacciaguerra, S., Chiarini, A., Spampinato, S., Tumiatti, V., and Melchiorre, C.

Abstract

The concept that polyamines may represent a universal template in the receptor recognition process is embodied in the design of new selective muscarinic ligands. Tetraamines 4−7 and 16−20 and diamine diamides 8−15 were synthesized, and their pharmacological profiles at muscarinic receptor subtypes were assessed by functional experiments in isolated guinea pig left atrium (M2) and ileum (M3) and by binding assays in rat cortex (M1), heart (M2), submaxillary gland (M3), and NG 108-15 cells (M4). It has been confirmed that appropriate substituents on the terminal nitrogens of a tetraamine template can tune both affinity and selectivity for muscarinic receptors. The novel tetraamine C-tripitramine (17) was able to discriminate significantly M1 and M2 receptors versus the other subtypes, and in addition it was 100-fold more lipophilic than the lead compound tripitramine. Compound 14 (tripinamide), in which the tetraamine backbone was transformed into a diamine diamide one, retained high affinity for muscarinic subtypes, displaying a binding affinity profile (M2 > M1 > M4 > M3) qualitatively similar to that of tripitramine. Both these ligands, owing to their improved lipophilicity relative to tripitramine and methoctramine, could serve as tools in investigating cholinergic functions in the central nervous system. Furthermore, notwithstanding the fact that the highest affinity was always associated with muscarinic M2 receptors, for the first time polyamines were shown to display high pA2 values also toward muscarinic M3 receptors.

Published
1998

48. Emergency structure activities perfomed after Emilia Romagna earthquake: Report on first month | Terremoto in Emilia Romagna: le attività del Pronto Intervento Sismico durante il primo mese di emergenza. Modalità e tempistica

Author

Moretti, M., Abruzzese, L., Augliera, P., Azzara, R., Bono, A., Bordoni, P., Bucci, A., Cacciaguerra, S., Cara, F., Carannante, S., Cardinale, V., Castagnozzi, A., Cattaneo, M., Cavaliere, A., Cecere, G., Chiarabba, C., Chiaraluce, L., Ciaccio, M. G., Cogliano, R., Colasanti, G., Colasanti, M., Criscuoli, F., Cultrera, G., D Alema, E., D Ambrosio, C., Danesi, S., Gori, P., Luca, G., Delladio, A., Demartin, M., Di Giulio, G., Ercolani, E., Faenza, L., Falco, L., Fiaschi, A., Ficeli, P., Fodarella, A., Franceschi, D., Franceschina, G., Frapiccini, M., Giovani, L., Govoni, A., Improta, L., Ladina, C., Lauciani, V., Lolli, B., Lovati, S., Lucente, F. P., Luzi, L., Mandiello, A., Marcocci, C., Margheriti, L., Marzorati, S., Massa, M., Mazza, S., Giuliano Milana, Minichiello, F., Monachesi, G., Morelli, A., Moschillo, R., Pacor, F., Piccinini, D., Piccolini, U., Pignone, M., Pintore, S., Pondrelli, S., Pucillo, S., Quintiliani, M., Riccio, G., Rovelli, A., Salimbeni, S., Sandri, L., Selvaggi, G., Serratore, A., Silvestri, M., Valoroso, L., Vannucci, G., and Zaccarelli, L.

50. Emergency structure activities perfomed after Emilia Romagna earthquake: Report on first month,Terremoto in Emilia Romagna: le attività del Pronto Intervento Sismico durante il primo mese di emergenza. Modalità e tempistica

Author

Moretti, M., Abruzzese, L., Augliera, P., Azzara, R., Bono, A., Bordoni, P., Bucci, A., Cacciaguerra, S., Cara, F., Carannante, S., Cardinale, V., Castagnozzi, A., Cattaneo, M., Cavaliere, A., Cecere, G., Chiarabba, C., Chiaraluce, L., Maria Grazia CIACCIO, Cogliano, R., Colasanti, G., Colasanti, M., Criscuoli, F., Cultrera, G., D Alema, E., D Ambrosio, C., Danesi, S., Gori, P., Luca, G., Delladio, A., Demartin, M., Di Giulio, G., Ercolani, E., Faenza, L., Falco, L., Fiaschi, A., Ficeli, P., Fodarella, A., Franceschi, D., Franceschina, G., Frapiccini, M., Giovani, L., Govoni, A., Improta, L., Ladina, C., Lauciani, V., Lolli, B., Lovati, S., Lucente, F. P., Luzi, L., Mandiello, A., Marcocci, C., Margheriti, L., Marzorati, S., Massa, M., Mazza, S., Milana, G., Minichiello, F., Monachesi, G., Morelli, A., Moschillo, R., Pacor, F., Piccinini, D., Piccolini, U., Pignone, M., Pintore, S., Pondrelli, S., Pucillo, S., Quintiliani, M., Riccio, G., Rovelli, A., Salimbeni, S., Sandri, L., Selvaggi, G., Serratore, A., Silvestri, M., Valoroso, L., Vannucci, G., and Zaccarelli, L.

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