Targeting group II Metabotropic Glutamate (mGlu) receptors for the treatment of psychosis associated with alzheimer's disease: Selective activation of mGlu2 receptors amplifies β-amyloid toxicity in cultured neurons, whereas dual activation of mGlu2 and mGlu3 receptors is neuroprotective (747 views)
Mol Pharmacol (ISSN: 0026-895x), 2011 Mar; 79(3): 618-626.
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Paper type: Journal Article, Research Support, Non-U. S. Gov'T,
Impact factor: 4.883, 5-year impact factor: 4.58
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-79951975389&partnerID=40&md5=4d22666774d7ce51cae97a212cc9b001
Keywords: 1 (5 Bromopyrimidin 2 Yl) N (2, 4 Dichlorobenzyl)pyrrolidin 3 Amine Methanesulfonate Hydrate, 2 Amino 2 (2 Carboxycyclopropyl) 3 (xanthen 9 Yl)propionic Acid, 4 Amino 2 Oxabicyclo[3 1 0]hexane 4, 6 Dicarboxylic Acid, Amyloid Beta Protein, Ly 2389575, Ly 566332, Metabotropic Receptor 2, Metabotropic Receptor Agonist, Metabotropic Receptor Antagonist, Cyano Biphenyl 3 Yl) N (3 Pyridinylmethyl)ethanesulfonamide, Transforming Growth Factor Beta1, Unclassified Drug, Alzheimer Disease, Animal Cell, Animal Experiment, Animal Model, Article, Astrocyte, Cell Viability, Drug Antagonism, Drug Targeting, Gene Expression, Mouse, Nerve Cell Culture, Nerve Degeneration, Neuroprotection, Neurotoxicity, Nonhuman, Priority Journal, Psychosis, Amino Acids, Amyloid Beta-Peptides, Antipsychotic Agents, Bicyclo Compounds, Heterocyclic, Knockout, Neuroprotective Agents, Psychotic Disorders, Sprague-Dawley, Metabotropic Glutamate, Reverse Transcriptase Polymerase Chain Reaction, Alzheimer Disease Complications Drug Therapy Metabolism, Amino Acids Pharmacology, Amyloid Beta-Peptides Drug Effects Metabolism, Antipsychotic Agents Pharmacology, Astrocytes Drug Effects Metabolism, Heterocyclic Pharmacology, Neurons Drug Effects Metabolism, Neuroprotective Agents Pharmacology, Psychotic Disorders Drug Therapy Etiology Metabolism, Pyridines Pharmacology, Metabotropic Glutamate Drug Effects Metabolism Physiology, Sulfonamides Pharmacology, Transforming Growth Factor Beta1 Pharmacology, Xanthenes Pharmacology, 4 Dichlorobenzyl) Pyrrolidin 3 Amine Methanesulfonate Hydrate, 2 Amino 2 (2 Carboxycyclopropyl) 3 (xanthen 9 Yl) Propionic Acid, 4 Amino 2 Oxabicyclo [3 1 0] Hexane 4, Cyano Biphenyl 3 Yl) N (3 Pyridinylmethyl) Ethanesulfonamide,
Affiliations:
*** IBB - CNR ***
Department of Pharmaceutical Sciences, University of Catania, Catania, Italy
Experimental and Clinical Pharmacology, University of Catania, Catania, Italy
Istituto Neurologico Mediterraneo Neuromed, Pozzilli, Italy
Istituto Nazionale Biostrutture e Biosistemi, Rome, Italy
Institute of Biostructure and Bioimaging, National Research Council, Catania, Italy
Department of Physiology and Pharmacology, University of Rome Sapienza, Piazzale Aldo Moro 6, 00185, Rome, Italy
Neuroscience Discovery Research, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN, United States
References:
Arosio, B., Bergamaschini, L., Galimberti, L., La, P.C., Zanetti, M., Calabresi, C., Scarpini, E., Vergani, C., +10 T/C polymorphisms in the gene of transforming growth factor-β1 are associated with neurodegeneration and its clinical evolution (2007) Mechanisms of Ageing and Development, 128 (10), pp. 553-557. , DOI 10.1016/j.mad.2007.07.006, PII S004763740700122
Ashe, K.H., Zahs, K.R., Probing the biology of Alzheimer's disease in mice (2010) Neuron, 66, pp. 631-645
Bruno, V., Battaglia, G., Casabona, G., Copani, A., Caciagli, F., Nicoletti, F., Neuroprotection by glial metabotropic glutamate receptors is mediated by transforming growth factor-β (1998) Journal of Neuroscience, 18 (23), pp. 9594-9600
Bullock, R., Treatment of behavioural and psychiatric symptoms in dementia: Implications of recent safety warnings (2005) Curr Med Res Opin, 21, pp. 1-10
Caraci, F., Battaglia, G., Bruno, V., Bosco, P., Carbonaro, V., Giuffrida, M.L., Drago, F., Copani, A., TGF-β1 pathway as a new target for neuroprotection in Alzheimer's disease (2009) CNS Neurosci Ther, , doi:10.1111/j.1755-5949.2009.00115.x
Carter, K., Dickerson, J., Schoepp, D.D., Reilly, M., Herring, N., Williams, J., Sallee, F.R., Sharp, F.R., The mGlu2/3 receptor agonist LY379268 injected into cortex or thalamus decreases neuronal injury in retrosplenial cortex produced by NMDA receptor antagonist MK-801: Possible implications for psychosis (2004) Neuropharmacology, 47 (8), pp. 1135-1145. , DOI 10.1016/j.neuropharm.2004.08.018, PII S0028390804002461
Cartmell, J., Monn, J.A., Schoepp, D.D., Attenuation of specific PCP-evoked behaviors by the potent mGlu2/3 receptor agonist, LY379268 and comparison with the atypical antipsychotic, clozapine (2000) Psychopharmacology, 148 (4), pp. 423-429
Ciceroni, C., Mosillo, P., Mastrantoni, E., Sale, P., Ricci-Vitiani, L., Biagioni, F., Stocchi, F., Melchiorri, D., MGLU3 metabotropic glutamate receptors modulate the differentiation of SVZ-derived neural stem cells towards the astrocytic lineage (2010) Glia, 58, pp. 813-822
Conn, P.J., Lindsley, C.W., Jones, C.K., Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia (2009) Trends Pharmacol Sci, 30, pp. 25-31
Copani, A., Condorelli, F., Caruso, A., Vancheri, C., Sala, A., Giuffrida Stella, A.M., Canonico, P.L., Sortino, M.A., Mitotic signaling by β-amyloid causes neuronal death (1999) FASEB J, 13, pp. 2225-2234
Copani, A., Koh, J.Y., Cotman, C.W., Beta-amyloid increases neuronal susceptibility to injury by glucose deprivation (1991) Neuroreport, 2, pp. 763-765
Corti, C., Battaglia, G., Molinaro, G., Riozzi, B., Pittaluga, A., Corsi, M., Mugnaini, M., Bruno, V., The use of knock-out mice unravels distinct roles for mGlu2 and mGlu3 metabotropic glutamate receptors in mechanisms of neurodegeneration/ neuroprotection (2007) Journal of Neuroscience, 27 (31), pp. 8297-8308. , http://www.jneurosci.org/cgi/reprint/27/31/8297, DOI 10.1523/JNEUROSCI.1889-07.2007
D'Onofrio, M., Cuomo, L., Battaglia, G., Ngomba, R.T., Storto, M., Kingston, A.E., Orzi, F., Bruno, V., Neuroprotection mediated by glial group-II metabotropic glutamate receptors requires the activation of the MAP kinase and the phosphatidylinositol-3-kinase pathways (2001) Journal of Neurochemistry, 78 (3), pp. 435-445. , DOI 10.1046/j.1471-4159.2001.00435.x
Fell, M.J., Svensson, K.A., Johnson, B.G., Schoepp, D.D., Evidence for the role of metabotropic glutamate (mGlu)2 not mGlu3 receptors in the preclinical antipsychotic pharmacology of the mGlu2/3 receptor agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]hexane-4,6- dicarboxylic acid (LY404039) (2008) Journal of Pharmacology and Experimental Therapeutics, 326 (1), pp. 209-217. , http://jpet.aspetjournals.org/cgi/reprint/326/1/209, DOI 10.1124/jpet.108.136861
Fraley, M.E., Positive allosteric modulators of the metabotropic glutamate receptor 2 for the treatment of schizophrenia (2009) Expert Opin Ther Pat, 19, pp. 1259-1275
Gill, S.S., Rochon, P.A., Herrmann, N., Lee, P.E., Sykora, K., Gunraj, N., Normand, S.L., Wodchis, W.P., Atypical antipsychotic drugs and risk of ischaemic stroke: Population based retrospective cohort study (2005) BMJ, 330, p. 445
Giuffrida, M.L., Caraci, F., Pignataro, B., Cataldo, S., De Bona, P., Bruno, V., Molinaro, G., Palmigiano, A., Beta-amyloid monomers are neuroprotective (2009) J Neurosci, 29, pp. 10582-10587
Giuffrida, M.L., Grasso, G., Ruvo, M., Pedone, C., Saporito, A., Marasco, D., Pignataro, B., Rizzarelli, E., Aβ(25-35) and its C- And/or N-blocked derivatives: Copper driven structural features and neurotoxicity (2007) J Neurosci Res, 85, pp. 623-633
Hardy, J., The amyloid hypothesis for Alzheimer's disease: A critical reappraisal (2009) J Neurochem, 110, pp. 1129-1134
Herrmann, N., Lanctot, K.L., Do atypical antipsychotics cause stroke? (2005) CNS Drugs, 19 (2), pp. 91-103. , DOI 10.2165/00023210-200519020-00001
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Johnson, M.P., Barda, D., Britton, T.C., Emkey, R., Hornback, W.J., Jagdmann, G.E., McKinzie, D.L., Schoepp, D.D., Metabotropic glutamate 2 receptor potentiators: Receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and psychosis model(s) (2005) Psychopharmacology, 179 (1), pp. 271-283. , DOI 10.1007/s00213-004-2099-9
Kim, S.H., Fraser, P.E., Westaway, D., St George-Hyslop, P.H., Ehrlich, M.E., Gandy, S., Group II metabotropic glutamate receptor stimulation triggers production and release of Alzheimer's amyloid(β)42 from isolated intact nerve terminals (2010) J Neurosci, 30, pp. 3870-3875
Koh, J.-Y., Yang, L.L., Cotman, C.W., Beta-Amyloid protein increases the vulnerability of cultured cortical neurons to excitotoxic damage (1990) Brain Research, 533 (2), pp. 315-320. , DOI 10.1016/0006-8993(90)91355-K
Lambert, M.P., Barlow, A.K., Chromy, B.A., Edwards, C., Freed, R., Liosatos, M., Morgan, T.E., Viola, K.L., Diffusible, nonfibrillar ligands derived from Aβ1-42 are potent central nervous system neurotoxins (1998) Proc Natl Acad Sci USA, 95, pp. 6448-6453
Lee, H.-G., Ogawa, O., Zhu, X., O'Neil, M.J., Petersen, R.B., Castellani, R.J., Ghanbari, H., Smith, M.A., Aberrant expression of metabotropic glutamate receptor 2 in the vulnerable neurons of Alzheimer's disease (2004) Acta Neuropathologica, 107 (4), pp. 365-371. , DOI 10.1007/s00401-004-0820-8
Lee, H.G., Zhu, X., Casadesus, G., Pallàs, M., Camins, A., O'Neill, M.J., Nakanishi, S., Smith, M.A., The effect of mGluR2 activation on signal transduction pathways and neuronal cell survival (2009) Brain Res, 1249, pp. 244-250
Leucht, S., Corves, C., Arbter, D., Engel, R.R., Li, C., Davis, J.M., Secondgeneration versus first-generation antipsychotic drugs for schizophrenia: A meta-analysis (2009) Lancet, 373, pp. 31-41
Lieberman, J.A., Is schizophrenia a neurodegenerative disorder? A clinical and neurobiological perspective (1999) Biol Psychiatry, 46, pp. 729-739
Lieberman, J.A., Neuroprotection: A new strategy in the treatment of schizophrenia. Neurobiological basis of neurodegeneration and neuroprotection (2007) CNS Spectr, 12 (SUPPL. 18), pp. 4-6
Mazzucco, S., Cipriani, A., Barbui, C., Monaco, S., Antipsychotic drugs and cerebrovascular events in elderly patients with dementia: A systematic review (2008) Mini Rev Med Chem, 8, pp. 776-783
Niswender, C.M., Conn, P.J., Metabotropic glutamate receptors: Physiology, pharmacology, and disease (2010) Annu Rev Pharmacol Toxicol, 50, pp. 295-322
Patil, S.T., Zhang, L., Martenyi, F., Lowe, S.L., Jackson, K.A., Andreev, B.V., Avedisova, A.S., Schoepp, D.D., Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: A randomized Phase 2 clinical trial (2007) Nature Medicine, 13 (9), pp. 1102-1107. , DOI 10.1038/nm1632, PII NM1632
Pérez-Neri, I., Ramírez-Bermúdez, J., Montes, S., Ríos, C., Possible mechanisms of neurodegeneration in schizophrenia (2006) Neurochem Res, 31, pp. 1279-1294
Querfurth, H.W., LaFerla, F.M., Alzheimer's disease (2010) N Engl J Med, 362, pp. 329-344
Recupero, P.R., Rainey, S.E., Managing risk when considering the use of atypical antipsychotics for elderly patients with dementia-related psychosis (2007) Journal of Psychiatric Practice, 13 (3), pp. 143-152. , DOI 10.1097/01.pra.0000271655.02093.49, PII 0013174620070500000002
Rorick-Kehn, L.M., Hart, J.C., McKinzie, D.L., Pharmacological characterization of stress-induced hyperthermia in DBA/2 mice using metabotropic and ionotropic glutamate receptor ligands (2005) Psychopharmacology, 183 (2), pp. 226-240. , DOI 10.1007/s00213-005-0169-2
Rund, B.R., Is schizophrenia a neurodegenerative disorder? (2009) Nord J Psychiatry, 63, pp. 196-201
Schoepp, D.D., Jane, D.E., Monn, J.A., Pharmacological agents acting at subtypes of metabotropic glutamate receptors (1999) Neuropharmacology, 38 (10), pp. 1431-1476. , DOI 10.1016/S0028-3908(99)00092-1, PII S0028390899000921
Swanson, C.J., Schoepp, D.D., A Role for Noradrenergic Transmission in the Actions of Phencyclidine and the Antipsychotic and Antistress Effects of mGlu2/3 Receptor Agonists (2003) Annals of the New York Academy of Sciences, 1003, pp. 309-317. , DOI 10.1196/annals.1300.019
Tesseur, I., Zou, K., Esposito, L., Bard, F., Berber, E., Van, C.J., Lin, A.H., Wyss-Coray, T., Deficiency in neuronal TGF-β signaling promotes neurodegeneration and Alzheimer's pathology (2006) Journal of Clinical Investigation, 116 (11), pp. 3060-3069. , http://www.jci.org/cgi/reprint/116/11/3060.pdf, DOI 10.1172/JCI27341
Trifirò, G., Spina, E., Gambassi, G., Use of antipsychotics in elderly patients with dementia: Do atypical and conventional agents have a similar safety profile? (2009) Pharmacol Res, 59, pp. 1-12
Ashe, K. H., Zahs, K. R., Probing the biology of Alzheimer's disease in mice (2010) Neuron, 66, pp. 631-645
Conn, P. J., Lindsley, C. W., Jones, C. K., Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia (2009) Trends Pharmacol Sci, 30, pp. 25-31
Fell, M. J., Svensson, K. A., Johnson, B. G., Schoepp, D. D., Evidence for the role of metabotropic glutamate (mGlu) 2 not mGlu3 receptors in the preclinical antipsychotic pharmacology of the mGlu2/3 receptor agonist (-) - (1R, 4S, 5S, 6S) -4-amino-2-sulfonylbicyclo [3. 1. 0] hexane-4, 6- dicarboxylic acid (LY404039) (2008) Journal of Pharmacology and Experimental Therapeutics, 326 (1), pp. 209-217. , http: //jpet. aspetjournals. org/cgi/reprint/326/1/209, DOI 10. 1124/jpet. 108. 136861
Fraley, M. E., Positive allosteric modulators of the metabotropic glutamate receptor 2 for the treatment of schizophrenia (2009) Expert Opin Ther Pat, 19, pp. 1259-1275
Gill, S. S., Rochon, P. A., Herrmann, N., Lee, P. E., Sykora, K., Gunraj, N., Normand, S. L., Wodchis, W. P., Atypical antipsychotic drugs and risk of ischaemic stroke: Population based retrospective cohort study (2005) BMJ, 330, p. 445
Giuffrida, M. L., Caraci, F., Pignataro, B., Cataldo, S., De Bona, P., Bruno, V., Molinaro, G., Palmigiano, A., Beta-amyloid monomers are neuroprotective (2009) J Neurosci, 29, pp. 10582-10587
Giuffrida, M. L., Grasso, G., Ruvo, M., Pedone, C., Saporito, A., Marasco, D., Pignataro, B., Rizzarelli, E., A (25-35) and its C- And/or N-blocked derivatives: Copper driven structural features and neurotoxicity (2007) J Neurosci Res, 85, pp. 623-633
Johnson, M. P., Barda, D., Britton, T. C., Emkey, R., Hornback, W. J., Jagdmann, G. E., McKinzie, D. L., Schoepp, D. D., Metabotropic glutamate 2 receptor potentiators: Receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and psychosis model (s) (2005) Psychopharmacology, 179 (1), pp. 271-283. , DOI 10. 1007/s00213-004-2099-9
Kim, S. H., Fraser, P. E., Westaway, D., St George-Hyslop, P. H., Ehrlich, M. E., Gandy, S., Group II metabotropic glutamate receptor stimulation triggers production and release of Alzheimer's amyloid () 42 from isolated intact nerve terminals (2010) J Neurosci, 30, pp. 3870-3875
Koh, J. -Y., Yang, L. L., Cotman, C. W., Beta-Amyloid protein increases the vulnerability of cultured cortical neurons to excitotoxic damage (1990) Brain Research, 533 (2), pp. 315-320. , DOI 10. 1016/0006-8993 (90) 91355-K
Lambert, M. P., Barlow, A. K., Chromy, B. A., Edwards, C., Freed, R., Liosatos, M., Morgan, T. E., Viola, K. L., Diffusible, nonfibrillar ligands derived from A 1-42 are potent central nervous system neurotoxins (1998) Proc Natl Acad Sci USA, 95, pp. 6448-6453
Lee, H. -G., Ogawa, O., Zhu, X., O'Neil, M. J., Petersen, R. B., Castellani, R. J., Ghanbari, H., Smith, M. A., Aberrant expression of metabotropic glutamate receptor 2 in the vulnerable neurons of Alzheimer's disease (2004) Acta Neuropathologica, 107 (4), pp. 365-371. , DOI 10. 1007/s00401-004-0820-8
Lee, H. G., Zhu, X., Casadesus, G., Pall s, M., Camins, A., O'Neill, M. J., Nakanishi, S., Smith, M. A., The effect of mGluR2 activation on signal transduction pathways and neuronal cell survival (2009) Brain Res, 1249, pp. 244-250
Lieberman, J. A., Is schizophrenia a neurodegenerative disorder? A clinical and neurobiological perspective (1999) Biol Psychiatry, 46, pp. 729-739
Lieberman, J. A., Neuroprotection: A new strategy in the treatment of schizophrenia. Neurobiological basis of neurodegeneration and neuroprotection (2007) CNS Spectr, 12 (SUPPL. 18), pp. 4-6
Niswender, C. M., Conn, P. J., Metabotropic glutamate receptors: Physiology, pharmacology, and disease (2010) Annu Rev Pharmacol Toxicol, 50, pp. 295-322
Patil, S. T., Zhang, L., Martenyi, F., Lowe, S. L., Jackson, K. A., Andreev, B. V., Avedisova, A. S., Schoepp, D. D., Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: A randomized Phase 2 clinical trial (2007) Nature Medicine, 13 (9), pp. 1102-1107. , DOI 10. 1038/nm1632, PII NM1632
P rez-Neri, I., Ram rez-Berm dez, J., Montes, S., R os, C., Possible mechanisms of neurodegeneration in schizophrenia (2006) Neurochem Res, 31, pp. 1279-1294
Querfurth, H. W., LaFerla, F. M., Alzheimer's disease (2010) N Engl J Med, 362, pp. 329-344
Recupero, P. R., Rainey, S. E., Managing risk when considering the use of atypical antipsychotics for elderly patients with dementia-related psychosis (2007) Journal of Psychiatric Practice, 13 (3), pp. 143-152. , DOI 10. 1097/01. pra. 0000271655. 02093. 49, PII 0013174620070500000002
Rorick-Kehn, L. M., Hart, J. C., McKinzie, D. L., Pharmacological characterization of stress-induced hyperthermia in DBA/2 mice using metabotropic and ionotropic glutamate receptor ligands (2005) Psychopharmacology, 183 (2), pp. 226-240. , DOI 10. 1007/s00213-005-0169-2
Rund, B. R., Is schizophrenia a neurodegenerative disorder? (2009) Nord J Psychiatry, 63, pp. 196-201
Schoepp, D. D., Jane, D. E., Monn, J. A., Pharmacological agents acting at subtypes of metabotropic glutamate receptors (1999) Neuropharmacology, 38 (10), pp. 1431-1476. , DOI 10. 1016/S0028-3908 (99) 00092-1, PII S0028390899000921
Swanson, C. J., Schoepp, D. D., A Role for Noradrenergic Transmission in the Actions of Phencyclidine and the Antipsychotic and Antistress Effects of mGlu2/3 Receptor Agonists (2003) Annals of the New York Academy of Sciences, 1003, pp. 309-317. , DOI 10. 1196/annals. 1300. 019
Trifir, G., Spina, E., Gambassi, G., Use of antipsychotics in elderly patients with dementia: Do atypical and conventional agents have a similar safety profile? (2009) Pharmacol Res, 59, pp. 1-12
Mol Pharmacol (ISSN: 0026-895x), 2011 Mar; 79(3): 618-626.
Export to BibTeX Export to EndNote
Paper type: Journal Article, Research Support, Non-U. S. Gov'T,
Impact factor: 4.883, 5-year impact factor: 4.58
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-79951975389&partnerID=40&md5=4d22666774d7ce51cae97a212cc9b001
Keywords: 1 (5 Bromopyrimidin 2 Yl) N (2, 4 Dichlorobenzyl)pyrrolidin 3 Amine Methanesulfonate Hydrate, 2 Amino 2 (2 Carboxycyclopropyl) 3 (xanthen 9 Yl)propionic Acid, 4 Amino 2 Oxabicyclo[3 1 0]hexane 4, 6 Dicarboxylic Acid, Amyloid Beta Protein, Ly 2389575, Ly 566332, Metabotropic Receptor 2, Metabotropic Receptor Agonist, Metabotropic Receptor Antagonist, Cyano Biphenyl 3 Yl) N (3 Pyridinylmethyl)ethanesulfonamide, Transforming Growth Factor Beta1, Unclassified Drug, Alzheimer Disease, Animal Cell, Animal Experiment, Animal Model, Article, Astrocyte, Cell Viability, Drug Antagonism, Drug Targeting, Gene Expression, Mouse, Nerve Cell Culture, Nerve Degeneration, Neuroprotection, Neurotoxicity, Nonhuman, Priority Journal, Psychosis, Amino Acids, Amyloid Beta-Peptides, Antipsychotic Agents, Bicyclo Compounds, Heterocyclic, Knockout, Neuroprotective Agents, Psychotic Disorders, Sprague-Dawley, Metabotropic Glutamate, Reverse Transcriptase Polymerase Chain Reaction, Alzheimer Disease Complications Drug Therapy Metabolism, Amino Acids Pharmacology, Amyloid Beta-Peptides Drug Effects Metabolism, Antipsychotic Agents Pharmacology, Astrocytes Drug Effects Metabolism, Heterocyclic Pharmacology, Neurons Drug Effects Metabolism, Neuroprotective Agents Pharmacology, Psychotic Disorders Drug Therapy Etiology Metabolism, Pyridines Pharmacology, Metabotropic Glutamate Drug Effects Metabolism Physiology, Sulfonamides Pharmacology, Transforming Growth Factor Beta1 Pharmacology, Xanthenes Pharmacology, 4 Dichlorobenzyl) Pyrrolidin 3 Amine Methanesulfonate Hydrate, 2 Amino 2 (2 Carboxycyclopropyl) 3 (xanthen 9 Yl) Propionic Acid, 4 Amino 2 Oxabicyclo [3 1 0] Hexane 4, Cyano Biphenyl 3 Yl) N (3 Pyridinylmethyl) Ethanesulfonamide,
Affiliations:
*** IBB - CNR ***
Department of Pharmaceutical Sciences, University of Catania, Catania, Italy
Experimental and Clinical Pharmacology, University of Catania, Catania, Italy
Istituto Neurologico Mediterraneo Neuromed, Pozzilli, Italy
Istituto Nazionale Biostrutture e Biosistemi, Rome, Italy
Institute of Biostructure and Bioimaging, National Research Council, Catania, Italy
Department of Physiology and Pharmacology, University of Rome Sapienza, Piazzale Aldo Moro 6, 00185, Rome, Italy
Neuroscience Discovery Research, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN, United States
References:
Arosio, B., Bergamaschini, L., Galimberti, L., La, P.C., Zanetti, M., Calabresi, C., Scarpini, E., Vergani, C., +10 T/C polymorphisms in the gene of transforming growth factor-β1 are associated with neurodegeneration and its clinical evolution (2007) Mechanisms of Ageing and Development, 128 (10), pp. 553-557. , DOI 10.1016/j.mad.2007.07.006, PII S004763740700122
Ashe, K.H., Zahs, K.R., Probing the biology of Alzheimer's disease in mice (2010) Neuron, 66, pp. 631-645
Bruno, V., Battaglia, G., Casabona, G., Copani, A., Caciagli, F., Nicoletti, F., Neuroprotection by glial metabotropic glutamate receptors is mediated by transforming growth factor-β (1998) Journal of Neuroscience, 18 (23), pp. 9594-9600
Bullock, R., Treatment of behavioural and psychiatric symptoms in dementia: Implications of recent safety warnings (2005) Curr Med Res Opin, 21, pp. 1-10
Caraci, F., Battaglia, G., Bruno, V., Bosco, P., Carbonaro, V., Giuffrida, M.L., Drago, F., Copani, A., TGF-β1 pathway as a new target for neuroprotection in Alzheimer's disease (2009) CNS Neurosci Ther, , doi:10.1111/j.1755-5949.2009.00115.x
Carter, K., Dickerson, J., Schoepp, D.D., Reilly, M., Herring, N., Williams, J., Sallee, F.R., Sharp, F.R., The mGlu2/3 receptor agonist LY379268 injected into cortex or thalamus decreases neuronal injury in retrosplenial cortex produced by NMDA receptor antagonist MK-801: Possible implications for psychosis (2004) Neuropharmacology, 47 (8), pp. 1135-1145. , DOI 10.1016/j.neuropharm.2004.08.018, PII S0028390804002461
Cartmell, J., Monn, J.A., Schoepp, D.D., Attenuation of specific PCP-evoked behaviors by the potent mGlu2/3 receptor agonist, LY379268 and comparison with the atypical antipsychotic, clozapine (2000) Psychopharmacology, 148 (4), pp. 423-429
Ciceroni, C., Mosillo, P., Mastrantoni, E., Sale, P., Ricci-Vitiani, L., Biagioni, F., Stocchi, F., Melchiorri, D., MGLU3 metabotropic glutamate receptors modulate the differentiation of SVZ-derived neural stem cells towards the astrocytic lineage (2010) Glia, 58, pp. 813-822
Conn, P.J., Lindsley, C.W., Jones, C.K., Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia (2009) Trends Pharmacol Sci, 30, pp. 25-31
Copani, A., Condorelli, F., Caruso, A., Vancheri, C., Sala, A., Giuffrida Stella, A.M., Canonico, P.L., Sortino, M.A., Mitotic signaling by β-amyloid causes neuronal death (1999) FASEB J, 13, pp. 2225-2234
Copani, A., Koh, J.Y., Cotman, C.W., Beta-amyloid increases neuronal susceptibility to injury by glucose deprivation (1991) Neuroreport, 2, pp. 763-765
Corti, C., Battaglia, G., Molinaro, G., Riozzi, B., Pittaluga, A., Corsi, M., Mugnaini, M., Bruno, V., The use of knock-out mice unravels distinct roles for mGlu2 and mGlu3 metabotropic glutamate receptors in mechanisms of neurodegeneration/ neuroprotection (2007) Journal of Neuroscience, 27 (31), pp. 8297-8308. , http://www.jneurosci.org/cgi/reprint/27/31/8297, DOI 10.1523/JNEUROSCI.1889-07.2007
D'Onofrio, M., Cuomo, L., Battaglia, G., Ngomba, R.T., Storto, M., Kingston, A.E., Orzi, F., Bruno, V., Neuroprotection mediated by glial group-II metabotropic glutamate receptors requires the activation of the MAP kinase and the phosphatidylinositol-3-kinase pathways (2001) Journal of Neurochemistry, 78 (3), pp. 435-445. , DOI 10.1046/j.1471-4159.2001.00435.x
Fell, M.J., Svensson, K.A., Johnson, B.G., Schoepp, D.D., Evidence for the role of metabotropic glutamate (mGlu)2 not mGlu3 receptors in the preclinical antipsychotic pharmacology of the mGlu2/3 receptor agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]hexane-4,6- dicarboxylic acid (LY404039) (2008) Journal of Pharmacology and Experimental Therapeutics, 326 (1), pp. 209-217. , http://jpet.aspetjournals.org/cgi/reprint/326/1/209, DOI 10.1124/jpet.108.136861
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Gill, S.S., Rochon, P.A., Herrmann, N., Lee, P.E., Sykora, K., Gunraj, N., Normand, S.L., Wodchis, W.P., Atypical antipsychotic drugs and risk of ischaemic stroke: Population based retrospective cohort study (2005) BMJ, 330, p. 445
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Kim, S.H., Fraser, P.E., Westaway, D., St George-Hyslop, P.H., Ehrlich, M.E., Gandy, S., Group II metabotropic glutamate receptor stimulation triggers production and release of Alzheimer's amyloid(β)42 from isolated intact nerve terminals (2010) J Neurosci, 30, pp. 3870-3875
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Lee, H.G., Zhu, X., Casadesus, G., Pallàs, M., Camins, A., O'Neill, M.J., Nakanishi, S., Smith, M.A., The effect of mGluR2 activation on signal transduction pathways and neuronal cell survival (2009) Brain Res, 1249, pp. 244-250
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Patil, S.T., Zhang, L., Martenyi, F., Lowe, S.L., Jackson, K.A., Andreev, B.V., Avedisova, A.S., Schoepp, D.D., Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: A randomized Phase 2 clinical trial (2007) Nature Medicine, 13 (9), pp. 1102-1107. , DOI 10.1038/nm1632, PII NM1632
Pérez-Neri, I., Ramírez-Bermúdez, J., Montes, S., Ríos, C., Possible mechanisms of neurodegeneration in schizophrenia (2006) Neurochem Res, 31, pp. 1279-1294
Querfurth, H.W., LaFerla, F.M., Alzheimer's disease (2010) N Engl J Med, 362, pp. 329-344
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Rorick-Kehn, L.M., Hart, J.C., McKinzie, D.L., Pharmacological characterization of stress-induced hyperthermia in DBA/2 mice using metabotropic and ionotropic glutamate receptor ligands (2005) Psychopharmacology, 183 (2), pp. 226-240. , DOI 10.1007/s00213-005-0169-2
Rund, B.R., Is schizophrenia a neurodegenerative disorder? (2009) Nord J Psychiatry, 63, pp. 196-201
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Swanson, C.J., Schoepp, D.D., A Role for Noradrenergic Transmission in the Actions of Phencyclidine and the Antipsychotic and Antistress Effects of mGlu2/3 Receptor Agonists (2003) Annals of the New York Academy of Sciences, 1003, pp. 309-317. , DOI 10.1196/annals.1300.019
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Fell, M. J., Svensson, K. A., Johnson, B. G., Schoepp, D. D., Evidence for the role of metabotropic glutamate (mGlu) 2 not mGlu3 receptors in the preclinical antipsychotic pharmacology of the mGlu2/3 receptor agonist (-) - (1R, 4S, 5S, 6S) -4-amino-2-sulfonylbicyclo [3. 1. 0] hexane-4, 6- dicarboxylic acid (LY404039) (2008) Journal of Pharmacology and Experimental Therapeutics, 326 (1), pp. 209-217. , http: //jpet. aspetjournals. org/cgi/reprint/326/1/209, DOI 10. 1124/jpet. 108. 136861
Fraley, M. E., Positive allosteric modulators of the metabotropic glutamate receptor 2 for the treatment of schizophrenia (2009) Expert Opin Ther Pat, 19, pp. 1259-1275
Gill, S. S., Rochon, P. A., Herrmann, N., Lee, P. E., Sykora, K., Gunraj, N., Normand, S. L., Wodchis, W. P., Atypical antipsychotic drugs and risk of ischaemic stroke: Population based retrospective cohort study (2005) BMJ, 330, p. 445
Giuffrida, M. L., Caraci, F., Pignataro, B., Cataldo, S., De Bona, P., Bruno, V., Molinaro, G., Palmigiano, A., Beta-amyloid monomers are neuroprotective (2009) J Neurosci, 29, pp. 10582-10587
Giuffrida, M. L., Grasso, G., Ruvo, M., Pedone, C., Saporito, A., Marasco, D., Pignataro, B., Rizzarelli, E., A (25-35) and its C- And/or N-blocked derivatives: Copper driven structural features and neurotoxicity (2007) J Neurosci Res, 85, pp. 623-633
Johnson, M. P., Barda, D., Britton, T. C., Emkey, R., Hornback, W. J., Jagdmann, G. E., McKinzie, D. L., Schoepp, D. D., Metabotropic glutamate 2 receptor potentiators: Receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and psychosis model (s) (2005) Psychopharmacology, 179 (1), pp. 271-283. , DOI 10. 1007/s00213-004-2099-9
Kim, S. H., Fraser, P. E., Westaway, D., St George-Hyslop, P. H., Ehrlich, M. E., Gandy, S., Group II metabotropic glutamate receptor stimulation triggers production and release of Alzheimer's amyloid () 42 from isolated intact nerve terminals (2010) J Neurosci, 30, pp. 3870-3875
Koh, J. -Y., Yang, L. L., Cotman, C. W., Beta-Amyloid protein increases the vulnerability of cultured cortical neurons to excitotoxic damage (1990) Brain Research, 533 (2), pp. 315-320. , DOI 10. 1016/0006-8993 (90) 91355-K
Lambert, M. P., Barlow, A. K., Chromy, B. A., Edwards, C., Freed, R., Liosatos, M., Morgan, T. E., Viola, K. L., Diffusible, nonfibrillar ligands derived from A 1-42 are potent central nervous system neurotoxins (1998) Proc Natl Acad Sci USA, 95, pp. 6448-6453
Lee, H. -G., Ogawa, O., Zhu, X., O'Neil, M. J., Petersen, R. B., Castellani, R. J., Ghanbari, H., Smith, M. A., Aberrant expression of metabotropic glutamate receptor 2 in the vulnerable neurons of Alzheimer's disease (2004) Acta Neuropathologica, 107 (4), pp. 365-371. , DOI 10. 1007/s00401-004-0820-8
Lee, H. G., Zhu, X., Casadesus, G., Pall s, M., Camins, A., O'Neill, M. J., Nakanishi, S., Smith, M. A., The effect of mGluR2 activation on signal transduction pathways and neuronal cell survival (2009) Brain Res, 1249, pp. 244-250
Lieberman, J. A., Is schizophrenia a neurodegenerative disorder? A clinical and neurobiological perspective (1999) Biol Psychiatry, 46, pp. 729-739
Lieberman, J. A., Neuroprotection: A new strategy in the treatment of schizophrenia. Neurobiological basis of neurodegeneration and neuroprotection (2007) CNS Spectr, 12 (SUPPL. 18), pp. 4-6
Niswender, C. M., Conn, P. J., Metabotropic glutamate receptors: Physiology, pharmacology, and disease (2010) Annu Rev Pharmacol Toxicol, 50, pp. 295-322
Patil, S. T., Zhang, L., Martenyi, F., Lowe, S. L., Jackson, K. A., Andreev, B. V., Avedisova, A. S., Schoepp, D. D., Activation of mGlu2/3 receptors as a new approach to treat schizophrenia: A randomized Phase 2 clinical trial (2007) Nature Medicine, 13 (9), pp. 1102-1107. , DOI 10. 1038/nm1632, PII NM1632
P rez-Neri, I., Ram rez-Berm dez, J., Montes, S., R os, C., Possible mechanisms of neurodegeneration in schizophrenia (2006) Neurochem Res, 31, pp. 1279-1294
Querfurth, H. W., LaFerla, F. M., Alzheimer's disease (2010) N Engl J Med, 362, pp. 329-344
Recupero, P. R., Rainey, S. E., Managing risk when considering the use of atypical antipsychotics for elderly patients with dementia-related psychosis (2007) Journal of Psychiatric Practice, 13 (3), pp. 143-152. , DOI 10. 1097/01. pra. 0000271655. 02093. 49, PII 0013174620070500000002
Rorick-Kehn, L. M., Hart, J. C., McKinzie, D. L., Pharmacological characterization of stress-induced hyperthermia in DBA/2 mice using metabotropic and ionotropic glutamate receptor ligands (2005) Psychopharmacology, 183 (2), pp. 226-240. , DOI 10. 1007/s00213-005-0169-2
Rund, B. R., Is schizophrenia a neurodegenerative disorder? (2009) Nord J Psychiatry, 63, pp. 196-201
Schoepp, D. D., Jane, D. E., Monn, J. A., Pharmacological agents acting at subtypes of metabotropic glutamate receptors (1999) Neuropharmacology, 38 (10), pp. 1431-1476. , DOI 10. 1016/S0028-3908 (99) 00092-1, PII S0028390899000921
Swanson, C. J., Schoepp, D. D., A Role for Noradrenergic Transmission in the Actions of Phencyclidine and the Antipsychotic and Antistress Effects of mGlu2/3 Receptor Agonists (2003) Annals of the New York Academy of Sciences, 1003, pp. 309-317. , DOI 10. 1196/annals. 1300. 019
Trifir, G., Spina, E., Gambassi, G., Use of antipsychotics in elderly patients with dementia: Do atypical and conventional agents have a similar safety profile? (2009) Pharmacol Res, 59, pp. 1-12
Targeting group II Metabotropic Glutamate (mGlu) receptors for the treatment of psychosis associated with alzheimer's disease: Selective activation of mGlu2 receptors amplifies β-amyloid toxicity in cultured neurons, whereas dual activation of mGlu2 and mGlu3 receptors is neuroprotective
Dual orthosteric agonists of metabotropic glutamate 2 (mGlu2) and mGlu3 receptors are being developed as novel antipsychotic agents devoid of the adverse effects of conventional antipsychotics. Therefore, these drugs could be helpful for the treatment of psychotic symptoms associated with Alzheimer's disease (AD). In experimental animals, the antipsychotic activity of mGlu2/3 receptor agonists is largely mediated by the activation of mGlu2 receptors and is mimicked by selective positive allosteric modulators (PAMs) of mGlu2 receptors. We investigated the distinct influence of mGlu2 and mGlu3 receptors in mixed and pure neuronal cultures exposed to synthetic β-amyloid protein (Aβ) to model neurodegeneration occurring in AD. The mGlu2 receptor PAM, N-4′-cyano-biphenyl-3-yl)-N-(3-pyridinylmethyl)-ethanesulfonamide hydrochloride (LY566332), devoid of toxicity per se, amplified Aβ-induced neurodegeneration, and this effect was prevented by the mGlu2/3 receptor antagonist (2S,1′S,2′S)-2-(9-xanthylmethyl)-2-(2′- carboxycyclopropyl)glycine (LY341495). LY566332 potentiated Aβ toxicity regardless of the presence of glial mGlu3 receptors, but it was inactive when neurons lacked mGlu2 receptors. The dual mGlu2/3 receptor agonist, (-)-2-oxa-4-aminobicyclo[3.1.0]exhane-4,6-dicarboxylic acid (LY379268), was neuroprotective in mixed cultures via a paracrine mechanism mediated by transforming growth factor-β1. LY379268 lost its protective activity in neurons grown with astrocytes lacking mGlu3 receptors, indicating that protection against Aβ neurotoxicity was mediated entirely by glial mGlu3 receptors. The selective noncompetitive mGlu3 receptor antagonist, (3S)-1-(5-bromopyrimidin-2-yl)-N-(2,4-dichlorobenzyl)pyrrolidin-3-amine methanesulfonate hydrate (LY2389575), amplified Aβ toxicity on its own, and, interestingly, unmasked a neurotoxic activity of LY379268, which probably was mediated by the activation of mGlu2 receptors. These data indicate that selective potentiation of mGlu2 receptors enhances neuronal vulnerability to Aβ, whereas dual activation of mGlu2 and mGlu3 receptors is protective against Aβ-induced toxicity. Copyright © 2011 The American Society for Pharmacology and Experimental Therapeutics.
Dual orthosteric agonists of metabotropic glutamate 2 (mGlu2) and mGlu3 receptors are being developed as novel antipsychotic agents devoid of the adverse effects of conventional antipsychotics. Therefore, these drugs could be helpful for the treatment of psychotic symptoms associated with Alzheimer's disease (AD). In experimental animals, the antipsychotic activity of mGlu2/3 receptor agonists is largely mediated by the activation of mGlu2 receptors and is mimicked by selective positive allosteric modulators (PAMs) of mGlu2 receptors. We investigated the distinct influence of mGlu2 and mGlu3 receptors in mixed and pure neuronal cultures exposed to synthetic β-amyloid protein (Aβ) to model neurodegeneration occurring in AD. The mGlu2 receptor PAM, N-4′-cyano-biphenyl-3-yl)-N-(3-pyridinylmethyl)-ethanesulfonamide hydrochloride (LY566332), devoid of toxicity per se, amplified Aβ-induced neurodegeneration, and this effect was prevented by the mGlu2/3 receptor antagonist (2S,1′S,2′S)-2-(9-xanthylmethyl)-2-(2′- carboxycyclopropyl)glycine (LY341495). LY566332 potentiated Aβ toxicity regardless of the presence of glial mGlu3 receptors, but it was inactive when neurons lacked mGlu2 receptors. The dual mGlu2/3 receptor agonist, (-)-2-oxa-4-aminobicyclo[3.1.0]exhane-4,6-dicarboxylic acid (LY379268), was neuroprotective in mixed cultures via a paracrine mechanism mediated by transforming growth factor-β1. LY379268 lost its protective activity in neurons grown with astrocytes lacking mGlu3 receptors, indicating that protection against Aβ neurotoxicity was mediated entirely by glial mGlu3 receptors. The selective noncompetitive mGlu3 receptor antagonist, (3S)-1-(5-bromopyrimidin-2-yl)-N-(2,4-dichlorobenzyl)pyrrolidin-3-amine methanesulfonate hydrate (LY2389575), amplified Aβ toxicity on its own, and, interestingly, unmasked a neurotoxic activity of LY379268, which probably was mediated by the activation of mGlu2 receptors. These data indicate that selective potentiation of mGlu2 receptors enhances neuronal vulnerability to Aβ, whereas dual activation of mGlu2 and mGlu3 receptors is protective against Aβ-induced toxicity. Copyright © 2011 The American Society for Pharmacology and Experimental Therapeutics.
Targeting group II Metabotropic Glutamate (mGlu) receptors for the treatment of psychosis associated with alzheimer's disease: Selective activation of mGlu2 receptors amplifies β-amyloid toxicity in cultured neurons, whereas dual activation of mGlu2 and mGlu3 receptors is neuroprotective
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Targeting group II Metabotropic Glutamate (mGlu) receptors for the treatment of psychosis associated with alzheimer's disease: Selective activation of mGlu2 receptors amplifies β-amyloid toxicity in cultured neurons, whereas dual activation of mGlu2 and mGlu3 receptors is neuroprotective
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Di Menna L, Joffe ME, Iacovelli L, Orlando R, Lindsley CW, Mairesse J, Gressèns P, Cannella M, Caraci F, Copani A, Bruno V, Battaglia G, Conn PJ, Nicoletti F
* Functional partnership between mGlu3 and mGlu5 metabotropic glutamate receptors in the central nervous system (394 views)
Neuropharm (ISSN: 0028-3908linking, 1873-7064electronic), 2018 Jan; 128: 301-313.
Impact Factor: 3.383
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Caraci F, Nicoletti F, Copani A
* Metabotropic glutamate receptors: the potential for therapeutic applications in Alzheimer's disease (535 views)
Curr Opin Pharmacol (ISSN: 1471-4892), 2017 Dec 23; 38: 1-7.
Impact Factor: 6.313
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Caraci F, Battaglia G, Sortino MA, Spampinato S, Molinaro G, Copani A, Nicoletti F, Bruno V
* Metabotropic glutamate receptors in neurodegeneration/neuroprotection: Still a hot topic? (625 views)
Neurochem Int (ISSN: 0197-0186), 2012 Sep; 61(4): 559-565.
Impact Factor: 2.659
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Caraci F, Spampinato S, Sortino MA, Bosco P, Battaglia G, Bruno V, Drago F, Nicoletti F, Copani A
* Dysfunction of TGF-β1 signaling in Alzheimer's disease: Perspectives for neuroprotection (876 views)
Cell Tissue Res (ISSN: 0302-766x), 2012 Jan; 347(1): 291-301.
Impact Factor: 3.677
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Chiechio S, Zammataro M, Morales ME, Busceti CL, Drago F, Th Gereau RW, Copani A, Nicoletti F
* Epigenetic modulation of mGlu2 receptors by histone deacetylase inhibitors in the treatment of inflammatory pain (433 views)
Mol Pharmacol (ISSN: 0026-895x), 2009; 75(5): 1014-1020.
Impact Factor: 4.531
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* Functional partnership between mGlu3 and mGlu5 metabotropic glutamate receptors in the central nervous system (394 views)
Neuropharm (ISSN: 0028-3908linking, 1873-7064electronic), 2018 Jan; 128: 301-313.
Impact Factor: 3.383
View Export to BibTeX Export to EndNote
Caraci F, Nicoletti F, Copani A
* Metabotropic glutamate receptors: the potential for therapeutic applications in Alzheimer's disease (535 views)
Curr Opin Pharmacol (ISSN: 1471-4892), 2017 Dec 23; 38: 1-7.
Impact Factor: 6.313
View Export to BibTeX Export to EndNote
Caraci F, Battaglia G, Sortino MA, Spampinato S, Molinaro G, Copani A, Nicoletti F, Bruno V
* Metabotropic glutamate receptors in neurodegeneration/neuroprotection: Still a hot topic? (625 views)
Neurochem Int (ISSN: 0197-0186), 2012 Sep; 61(4): 559-565.
Impact Factor: 2.659
View Export to BibTeX Export to EndNote
Caraci F, Spampinato S, Sortino MA, Bosco P, Battaglia G, Bruno V, Drago F, Nicoletti F, Copani A
* Dysfunction of TGF-β1 signaling in Alzheimer's disease: Perspectives for neuroprotection (876 views)
Cell Tissue Res (ISSN: 0302-766x), 2012 Jan; 347(1): 291-301.
Impact Factor: 3.677
View Export to BibTeX Export to EndNote
Chiechio S, Zammataro M, Morales ME, Busceti CL, Drago F, Th Gereau RW, Copani A, Nicoletti F
* Epigenetic modulation of mGlu2 receptors by histone deacetylase inhibitors in the treatment of inflammatory pain (433 views)
Mol Pharmacol (ISSN: 0026-895x), 2009; 75(5): 1014-1020.
Impact Factor: 4.531
View Export to BibTeX Export to EndNote
5 Records (5 excluding Abstracts).
Total impact factor: 20.563 (20.563 excluding Abstracts).
Total 5 year impact factor: 19.727 (19.727 excluding Abstracts).
Total impact factor: 20.563 (20.563 excluding Abstracts).
Total 5 year impact factor: 19.727 (19.727 excluding Abstracts).
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