Search Results - "Sava, Anna"

Identification and characterization of novel NMDA receptor antagonists selective for NR2A- over NR2B-containing receptors by Bettini, Ezio, Sava, Anna, Griffante, Cristiana, Carignani, Corrado, Buson, Alberto, Capelli, Anna Maria, Negri, Michele, Andreetta, Filippo, Senar-Sancho, Sergio A, Guiral, Lorena, Cardullo, Francesca

“…NR1/NR2A is a subtype of N-methyl-d-aspartate receptors (NMDARs), which are glutamate and glycine-gated Ca(2+)-permeable channels highly expressed in the…”
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Affinity, potency, efficacy, and selectivity of neurokinin A analogs at human recombinant NK2 and NK1 receptors by Rupniak, Nadia M J, Perdona, Elisabetta, Griffante, Cristiana, Cavallini, Palmina, Sava, Anna, Ricca, Daniel J, Thor, Karl B, Burgard, Edward C, Corsi, Mauro

“…A series of peptide NK2 receptor agonists was evaluated for affinity, potency, efficacy, and selectivity at human recombinant NK2 and NK1 receptors expressed…”
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Novel Spirotetracyclic Zwitterionic Dual H1/5-HT2A Receptor Antagonists for the Treatment of Sleep Disorders by Gianotti, Massimo, Botta, Maurizio, Brough, Stephen, Carletti, Renzo, Castiglioni, Emiliano, Corti, Corrado, Dal-Cin, Michele, Delle Fratte, Sonia, Korajac, Denana, Lovric, Marija, Merlo, Giancarlo, Mesic, Milan, Pavone, Francesca, Piccoli, Laura, Rast, Slavko, Roscic, Maja, Sava, Anna, Smehil, Mario, Stasi, Luigi, Togninelli, Andrea, Wigglesworth, Mark J

“…Histamine H1 and serotonin 5-HT2A receptors mediate two different mechanisms involved in sleep regulation: H1 antagonists are sleep inducers, while 5-HT2A…”
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Modulation of nicotinic acetylcholine receptor turnover by tyrosine phosphorylation in rat myotubes by Sava, Anna, Barisone, Ilaria, Di Mauro, Debora, Fumagalli, Guido, Sala, Carlo

“…The muscle nicotinic acetylcholine receptor (AChR) turns over at different rates depending on stage of synaptogenesis and innervation. Tyrosine phosphorylation…”
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Brain-penetrant cyanoindane and cyanotetralin inhibitors of G2019S-LRRK2 kinase activity by Garofalo, Albert W., Schwarz, Jacob, Zobel, Kerry, Beato, Claudia, Bernardi, Silvia, Budassi, Federica, Caberlotto, Laura, Gao, Peng, Griffante, Cristiana, Liu, Xinying, Migliore, Marco, Qiao, Feifei, Sabbatini, Fabio Maria, Sava, Anna, Zhang, Mingliang, Carlisle, Holly J.

“…[Display omitted] The G2019S variant of LRRK2, which causes an increase in kinase activity, is associated with the occurrence of Parkinson’s disease (PD)…”
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Selective Inhibitors of G2019S-LRRK2 Kinase Activity by Garofalo, Albert W, Bright, Jessica, De Lombaert, Stéphane, Toda, Alyssa M. A, Zobel, Kerry, Andreotti, Daniele, Beato, Claudia, Bernardi, Silvia, Budassi, Federica, Caberlotto, Laura, Gao, Peng, Griffante, Cristiana, Liu, Xinying, Mengatto, Luisa, Migliore, Marco, Sabbatini, Fabio Maria, Sava, Anna, Serra, Elena, Vincetti, Paolo, Zhang, Mingliang, Carlisle, Holly J

“…Pathogenic variants in the leucine-rich repeat kinase 2 (LRRK2) gene have been identified that increase the risk for developing Parkinson’s disease in a…”
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Potency, efficacy, and selectivity of GR64349 at human recombinant neurokinin NK2 and NK1 receptors by Perdona, Elisabetta, Cavallini, Palmina, Sava, Anna, Griffante, Cristiana, Ricca, Daniel J., Thor, Karl B., Rupniak, Nadia M.J., Corsi, Mauro

“…•The affinity and potency of GR64349 for NK2 and NK1 receptors was examined.•Binding affinity was ˜1200-fold higher for NK2 than NK1 receptors.•Potency was…”
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Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists by Micheli, Fabrizio, Cremonesi, Susanna, Semeraro, Teresa, Tarsi, Luca, Tomelleri, Silvia, Cavanni, Paolo, Oliosi, Beatrice, Perdonà, Elisabetta, Sava, Anna, Zonzini, Laura, Feriani, Aldo, Braggio, Simone, Heidbreder, Christian

“…[Display omitted] A new series of morpholine derivatives has been identified as selective DA D3 receptor antagonists; their in vitro profile and…”
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NMDA-induced ERK signalling is mediated by NR2B subunit in rat cortical neurons and switches from positive to negative depending on stage of development by Sava, Anna, Formaggio, Elena, Carignani, Corrado, Andreetta, Filippo, Bettini, Ezio, Griffante, Cristiana

“…It is known that NMDA receptor stimulation can activate or inhibit the extracellular signal-regulated kinase (ERK) signalling cascade, a key pathway involved…”
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1,2,4-Triazolyl 5‑Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists by Micheli, Fabrizio, Bacchi, Alessia, Braggio, Simone, Castelletti, Laura, Cavallini, Palmina, Cavanni, Paolo, Cremonesi, Susanna, Dal Cin, Michele, Feriani, Aldo, Gehanne, Sylvie, Kajbaf, Mahmud, Marchió, Luciano, Nola, Selena, Oliosi, Beatrice, Pellacani, Annalisa, Perdonà, Elisabetta, Sava, Anna, Semeraro, Teresa, Tarsi, Luca, Tomelleri, Silvia, Wong, Andrea, Visentini, Filippo, Zonzini, Laura, Heidbreder, Christian

“…A novel series of 1,2,4-triazolyl 5-azaspiro[2.4]­heptanes with high affinity and selectivity at the dopamine (DA) D3 receptor (D3R) is described. Some of…”
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The opioid receptor pharmacology of GSK1521498 compared to other ligands with differential effects on compulsive reward-related behaviours by Kelly, Eamonn, Mundell, Stuart J., Sava, Anna, Roth, Adelheid L., Felici, Antonio, Maltby, Kay, Nathan, Pradeep J., Bullmore, Edward T., Henderson, Graeme

“…Rationale The novel opioid receptor antagonist, GSK1421498, has been shown to attenuate reward-driven compulsive behaviours, such as stimulant drug seeking or…”
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Design and Synthesis of Novel Tricyclic Benzoxazines as Potent 5-HT1A/B/D Receptor Antagonists Leading to the Discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045) by Bromidge, Steven M, Arban, Roberto, Bertani, Barbara, Bison, Silvia, Borriello, Manuela, Cavanni, Paolo, Dal Forno, Giovanna, Di-Fabio, Romano, Donati, Daniele, Fontana, Stefano, Gianotti, Massimo, Gordon, Laurie J, Granci, Enrica, Leslie, Colin P, Moccia, Luca, Pasquarello, Alessandra, Sartori, Ilaria, Sava, Anna, Watson, Jeannette M, Worby, Angela, Zonzini, Laura, Zucchelli, Valeria

“…Bioisoteric replacement of the metabolically labile N-methyl amide group of a series of benzoxazinones with small heterocyclic rings has led to novel series of…”
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Design and Synthesis of Novel Tricyclic Benzoxazines as Potent 5-HT 1A/B/D Receptor Antagonists Leading to the Discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4 H -imidazo[5,1- c ][1,4]benzoxazine-3-carboxamide (GSK588045) by Bromidge, Steven M., Arban, Roberto, Bertani, Barbara, Bison, Silvia, Borriello, Manuela, Cavanni, Paolo, Dal Forno, Giovanna, Di-Fabio, Romano, Donati, Daniele, Fontana, Stefano, Gianotti, Massimo, Gordon, Laurie J., Granci, Enrica, Leslie, Colin P., Moccia, Luca, Pasquarello, Alessandra, Sartori, Ilaria, Sava, Anna, Watson, Jeannette M., Worby, Angela, Zonzini, Laura, Zucchelli, Valeria

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The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2 by D’Alessandro, Pier L., Corti, Corrado, Roth, Adelheid, Ugolini, Annarosa, Sava, Anna, Montanari, Dino, Bianchi, Federica, Garland, Stephen L., Powney, Ben, Koppe, Emma L., Rocheville, Magalie, Osborne, Greg, Perez, Paloma, de la Fuente, Jesús, De Los Frailes, Maite, Smith, Paul W., Branch, Clive, Nash, David, Watson, Stephen P.

“…The optimisation of an HTS hit series ( 1) leading to the identification of structurally novel, selective, orally bioavailable mGluR2 positive modulators…”
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Novel Spirotetracyclic Zwitterionic Dual H 1 /5-HT 2A Receptor Antagonists for the Treatment of Sleep Disorders by Gianotti, Massimo, Botta, Maurizio, Brough, Stephen, Carletti, Renzo, Castiglioni, Emiliano, Corti, Corrado, Dal-Cin, Michele, Delle Fratte, Sonia, Korajac, Denana, Lovric, Marija, Merlo, Giancarlo, Mesic, Milan, Pavone, Francesca, Piccoli, Laura, Rast, Slavko, Roscic, Maja, Sava, Anna, Smehil, Mario, Stasi, Luigi, Togninelli, Andrea, Wigglesworth, Mark J.

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Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders by Gianotti, Massimo, Botta, Maurizio, Brough, Stephen, Carletti, Renzo, Castiglioni, Emiliano, Corti, Corrado, Dal-Cin, Michele, Delle Fratte, Sonia, Korajac, Denana, Lovric, Marija, Merlo, Giancarlo, Mesic, Milan, Pavone, Francesca, Piccoli, Laura, Rast, Slavko, Roscic, Maja, Sava, Anna, Smehil, Mario, Stasi, Luigi, Togninelli, Andrea, Wigglesworth, Mark J

“…Histamine H(1) and serotonin 5-HT(2A) receptors mediate two different mechanisms involved in sleep regulation: H(1) antagonists are sleep inducers, while…”
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Design and synthesis of novel tricyclic benzoxazines as potent 5-HT(1A/B/D) receptor antagonists leading to the discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045) by Bromidge, Steven M, Arban, Roberto, Bertani, Barbara, Bison, Silvia, Borriello, Manuela, Cavanni, Paolo, Dal Forno, Giovanna, Di-Fabio, Romano, Donati, Daniele, Fontana, Stefano, Gianotti, Massimo, Gordon, Laurie J, Granci, Enrica, Leslie, Colin P, Moccia, Luca, Pasquarello, Alessandra, Sartori, Ilaria, Sava, Anna, Watson, Jeannette M, Worby, Angela, Zonzini, Laura, Zucchelli, Valeria

“…Bioisoteric replacement of the metabolically labile N-methyl amide group of a series of benzoxazinones with small heterocyclic rings has led to novel series of…”
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