OFFICIAL RESULTS

Poster session rev1
1
POSTER SESSION
Tuesday, September 30th
evening session ▪ 9.00 pm
Alcantara Room ▪ Hotel Capotaormina
The poster board will be 100 cm (39,4 inches) wide and
140 cm (56,2 inches) high
Poster session rev1
Tuesday, September 30th evening session 9.00pm
Receptor localization and function
1.
Towards functional and pharmacological characterization of mGlu heterodimers
D.Moreno, P. Scholler, E. Doumazane, P. Rondard and J.P. Pin (France)
2.
Heterodimerization between dopamine D1 and Glutamate mGlu5 receptors controls cellular signaling
E. Goyet, N. Bouquier, V. Homburger, A. Burguière, L. Fagni and J. Perroy (France)
3.
Molecular mechanisms that desensitize Metabotropic Glutamate Receptors: an overview
L. Iacovelli, F. Nicoletti and A. De Blasi (Italy)
4.
Investigating the molecular mechanisms underlying the differential subcellular targeting of the
metabotropic glutamate receptor 1 (mGlu1) in the cerebellar cortex
M. Mansouri, H. Lindner and F. Ferraguti (Austria)
5.
Altered proteomic profile in synaptic endings from brain cortex of Grm1 mice
I. Musante, L. Musante, M. Bruschi, P.I. Rossi,L. Emionite, G. Candiano, R. Ravazzolo, A. Pittaluga and
A. Puliti (Italy)
6.
ExtracellularChlorideModulatesMetabotropic Glutamate ReceptorsActivity
A.Tora, X. Rovira, N. Doyon, H.O. Bertrand, I. Brabet, Y. De Koninck, J.P. Pin, F. Acher and C. Goudet
(France and Canada)
7.
Structural Basis of Chloride Selectivity between Group II Metabotropic Glutamate Receptors
E.J. Miller, J.O. DiRaddo, E. Grajkowska, B. Wroblewska, B.B. Wolfe, J.P. Snyder, J.T. Wroblewski and
D.C. Liotta (USA)
8.
Chloride is an Agonist of mGlu3, mGlu4, mGlu6, and mGlu8 Receptors
J.O. DiRaddo, E.J. Miller, E. Grajkowska, B. Wroblewska, J.P. Snyder, B.B. Wolfe, D.C. Liotta and
J.T. Wroblewski (USA)
9.
A Real-Time Method for Measuring cAMP Production Modulated by Gαi/o-Coupled Metabotropic
Glutamate Receptors
J.O. DiRaddo, E.J. Miller, H.A. Hathaway, E. Grajkowska, B. Wroblewska; B.B. Wolfe; D.C. Liotta and
J.T. Wroblewski (USA)
crv4
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10. The contribution of high glutamate concentration on mGlu 7 receptors functionality in cAMP accumulation
assays
G. Burnat, P. Brański, B. Chruścicka , M. Marciniak and A. Pilc (Poland)
11. The group II metabotropic glutamate receptor mGlu3 poteniates cAMP production and reduces excitatory
transmission in a form of glial-neuronal communication induced during coincident β-adrenergic receptor
activation.
D.J. Sheffler, A.G. Walker, A.S. Lewis, Z. Xiang and P.J. Conn (USA)
12. Tetracycline-based system for controlled inducible expression of metabotropic glutamate receptors.
B. Chruścicka, G. Burnat, P. Brański and A. Pilc (Poland)
13. Modulation of hippocampal synaptic transmission and functional evaluation of the kynurenine pathway
member xanthurenic acid
C.S. Copeland, S.A. Neale and T.E. Salt (UK)
Poster session rev1
14. GLYT1, NMDA and AMPA autoreceptors in hippocampal glutamatergic nerve endings :
an unexpected “ménage a trois”
E. Merega , S. Prisco Silvia, D. Graglia, S. Righetti and A.Pittaluga (Italy)
15.
Presynaptic release regulating mGlu2/3 autoreceptors in mouse cortex and spinal cord.
S. Di Prisco , E. Merega , D. Graglia , S. Righetti and A. Pittaluga (Italy)
Drug development
16. Metabotropic Glutamate Receptors: A Challenging System for Computational Modeling
I. Lans, J. Dalton, X. Rovira, D. Roche, C. Christov and J. Giraldo (Spain)
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17. Characterization of the mGlu2 PAM radioligand[ H]JNJ-46281222and its application for ex vivo receptor
occupancy in rat brain.
P. te Riele, I. Biesmans, L. Peeters, H. Lavreysen and X. Langlois (Belgium)
18. Development of novel mGlu1 PAMs as tools to improve functionality of mutant receptor isoforms found in
a schizophrenic population.
P. M. Garcia-Barrantes, H. P. Cho, J. T. Brogan, C.R. Hopkins, C. M. Niswender, R. D. Morrison, J. S. Daniels,
P. J. Conn and C. W. Lindsley (USA)
19. Synthesis and characterization of pyrazolo[1,5-a]quinazolin-5-one derivatives: potent non-competitive
mGluR2 NAMs. From hit toin vivo procognitionProof of Concept.
S. Mayer, C. Amalric, L. Cardona, T. Catelain, F. Courivaud, G. Hommet, N. Lotz, B. Manteau, S. Mikidadi, E.
Steinberg, L. Deshons, L. Baron, S. Scheffler, C Franchet, M. Frauli and S. Schann. (France)
20. Structural aspects of agonist and antagonist binding to human mGlu2 and mGlu3 receptors amino terminal
domains
J. Hao, S. Ashok, S. Atwell, K. Bain, M. Bures, J. H. Carter, D. Clawson, B. Condon, K. Conners, M. Dickey,
T. Gheyi, C. Groshong, B. Heinz, F. Lu, M. Kearins, R. Madsen, D. Manglicmot, L. Rodgers, M. Rutter,
M. Vargas, J. Wang, X. Wang, A. Zhang and J. A. Monn (USA)
21. LY2969822: Pharmacological characterization of an orally bioavailable prodrug for a potent, selective
mGlu2/3 receptor agonist
D. McKinzie, B. Johnson, K. Knitowski, D. Shaw, L. Rorick-Kehn, J. Katner, K. Perry, S. Swanson, J. Catlow,
M. Johnson, L. Prieto, C. Beadle and J. Monn (USA and Spain)
22. Synthesis and characterization of thioheteroaryl-substituted bicyclic amino acids. Identification of potent,
functionally selective mGlu2-receptor agonists
J. A. Monn, L. Prieto, L. Taboada, J. Hao, M.R. Reinhard, S. S. Henry, C. Beadle, L. Walton, T. Man, H. Rudyk,
B. Clark, D. Tupper, S. R. Baker, C. Lamas, C. Montero, A. Marcos, J. Blanco, M. Bures, D.K. Clawson,
S. Atwell, F. Lu, M. Russell, B. Heinz, X. Wang, J. Carter, B. Getman, J. Catlow, S. Swanson, B. G. Johnson, D.
Shaw and D. L. McKinzie (USA)
23. In vitro attributes of LY3020371, a potent and selective mGlu2/3 receptor antagonist
J. A. Monn, J. M. Witkin, P. L. Ornstein, C. H. Mitch, R. Li, S. C. Smith, X. Wang, C. Xiang, J. H. Carter,
J. Wang, S. Atwell, F. Pasqui, S. Fitzjohn and B. A. Heinz (USA and UK)
24. LY3020371: In vivo characterization of a novel mGlu2/3 receptor antagonist
J.M. Witkin, C. Overshiner, X. Li, G. Gilmour, J. Li, L. Rorick-Kehn, K. Rasmussen, B. Johnson, SN Mitchell,
K.G. Phillips, K.A. Wafford, D.L. McKinzie, A. Nikolayev, V.V. Tolstikov, M-S Kuo, P.L.Ornstein, C.H.Mitch,
R. Li, S.C. Smith, X-S Wang, B.A. Heinz, D. Allen, S. Swanson and J.A. Monn (USA and UK)
25. Safety, Tolerability, and Pharmacokinetic Evaluation of Single- and Multiple- Doses of LY2979165, a Prodrug of an Orthosteric metabotropic Glutamate 2 (mGlu2) Receptor Agonist in Healthy Subjects
J. McColm, S. Swanson, S. Tauscher-Wisniewski, J. Foster, S. Suriyapperuma and K. Jackson (USA)
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Poster session rev1
26. The selective mGlu4 receptor agonist LSP1-2111 is not transformed into L-AP4 under alkaline pH
conditions
H. Pedersen, X. Huang, F. Acher and D.Doller (Denmark, USA and France)
27. Positive allosteric modulation of mGlu4 receptors: challenges and opportunities
E. Dale, H. Hong, X. Huang, N. J. Boyle, M. Collins, J.A.Tamm, R.M. Brodbeck, H. Zhong, F. Acher and
D. Doller (USA and France)
28. Overlapping binding sites drive allosteric agonism and positive cooperativity in type 4 metabotropic
glutamate receptors
X. Rovira, F. Malhaire, P. Scholler, J. Rodrigo de Losada, P. Gonzalez-Bulnes, A. Llebaria, J.P. Pin, J. Giraldo
and C. Goudet (France and Spain)
29. Clickable photoaffinity labels for metabotropic glutamate receptor 5 based on allosteric modulator
scaffolds
K. J. Gregory, R. Velagaleti, D.M. Thal, A. Christopoulos, P. J. Conn and D.J. Lapinsky (Australia and USA)
30. Licencing opportunity for RGH-618 an orally active mGluR5 negative allosteric modulator
K. Gál, M. Darida, M. Kapás, Gy. Selényi and S. Farkas (Hungary)
31. Preclinical pharmacological profile of basimglurant (RO4917523, RG7090), a unique mGlu5 negative
allosteric modulator in clinical development for both Fragile X syndrome and depression
L. Lindemann, G. Jaeschke, R. Porter , S. Scharf, B. Kuennecke, M. von Kienlin, A. Harrison, A. Paehler,
C. Funk, A. Gloge, M. Schneider, N.J. Parrott, L. Polonchuk, U. Niederhauser, S.R. Morairty, T.S. Kilduff,
E. Vieira, B. Buettelmann, T. Hartung, S. Kolczewski, M. Honer, E. Borroni, J.L. Moreau , E. Prinssen,
W. Spooren and J. G. Wettstein (Switzerland and USA)
32. IP27039 a novel nonselective mGluR8 agonist?
P. Brański, A. Hogendorf, G. Burnat, A. Bojarski, B. Chruścicka, R.Bugno and A. Pilc (Poland)
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33. (±)-AZ12216052 is not an optimal mGlu8 receptor positive allosteric modulator tool compound
X. Huang, C.Bundgaard and D. Doller (USA and Denmark)
Sleep/Epilepsy
34. Metabotropic glutamate receptor type (mGlu7) action at GABAergic and glutamatergic synapses of the
mouse thalamocortical loop
V. Tassin, D. Rigault, M. Kalinichev, A. Chotte, B. Girard, F. Acher, L. Fagni and F. Bertaso (France)
35. Effects of selective Group I Metabotropic Glutamate Receptor enhancers locally infused in the corticothalamo-cortical circuit in the Wag/Rij rat model of absence epilepsy
V. D’Amore, C. von Randow, T. van Rijn, I. Santolini, R. Celli, M. Guiducci, F. Nicoletti, R. T. Ngomba and
G. van Luijtelaar (The Netherland and Italy)
36. A role for group-I metabotropic glutamate receptors (mGluR1/5) in sleep-wake regulation
A. Sousek, P. Franken, H-P. Landolt and M. Tafti (Switzerland)
37. FMR1 and mGluR5 as prospective molecular markers of sleep need in humans
S.C. Holst, K. Hefti, A. Baumer, A. Buck, S.M. Ametamey, M. Scheidegger, R. Dürr, E. Seifritz and H.-P. Landolt
(Switzerland)
38. Ficus platyphylla ameliorates seizure severity and neuronal loss in pentylenetetrazole-kindled mice – role
of GABA-ergic and glutamatergic systems
H. Schröder , B. A. Chindo and A. Becker ( Germany and Nigeria)
Poster session rev1
Synaptic plasticity/ cognitive functions
39. The MK2/3 cascade regulates AMPAR trafficking and cognitive flexibility
K. L. Eales, O.Palygin, T. O’Loughlin, S. Rasooli-Nejad, M. Gaestel, J. Müller, D. R. Collins, Y. Pankratov and
S. A.L. Corrêa (UK and Germany)
40. Group I mGluR-dependent plasticity in hippocampal CA2
M. Samadi, S.M. Dudek and Z.I. Bashir (UK and USA)
41. Effects of mGluR2 Blockade on operant delayed non-matching to position in rats
T. Steckler, N. Aerts, L. Ver Donck and J. Talpos (Belgium)
42. Procognitive effects of an mGlu2 negative allosteric modulatorin rats.
S. Embrechts, H. Van Craenendonck, D.J. Pemberton and L Ver Donck (Belgium)
43. Allosteric modulators of metabotropic glutamate receptors as promising therapeutic strategies for
Alzheimer’s disease
J. M. Rook, J.W. Dickerson, A.Ghoshal, A.G. Walker, G.N. Roop, Q. Huan, S.R. Stauffer, C. M. Niswender, J. S.
Daniels, C. K. Jones, C.W. Lindsley and P..J. Conn (USA)
44. Corticostriatal metaplasticity of group I metabotropic glutamate receptors contributes to habit learning.
B. Greco, A. Cavaccini, A. Rocchi, M. Trusel, V. Paget-Blanc, M. Maria and R .Tonini (Italy)
Peripheral organs
45. Possible functional expression of group III metabotropic glutamate receptors in the male mouse
reproductive system based on mGlu7 receptor example
M. Marciniak, B. Chruścicka, G.Burnat and A.Pilc (Poland)
crv4
46. Phenotypic characterization of Grm1
mice reveals a functional role for the type 1 metabotropic
glutamate receptor in the skeleton
I. Musante, L. Otescu, G. Cangemi C. Gatti, D. Mattinzoli, R. Ravazzo, M.P. Rastaldi, D. Riccardi and
A. Puliti (Italy and UK)
47. Negative Allosteric Modulation of the mGlu7Receptor Reduces Visceral Hypersensitivity in a StressSensitive Rat Strain
R. D. Moloney, R. M O’Connor, M. Kalinichev, T. G. Dinan and J. F. Cryan (Ireland and Switzerland
Pain
48. LY2491503, A Novel mGluR1 Antagonist for Persistent Pain: From Clone to Clinic
E.S.Nisenbaum, S. Iyengar, K.L. Knopp, R.M. Simmons, D. Li, M.J. Fisher, S. Kuklish, V.N. Barth, M.G. Chambers,
B.A. Heinz,S.A. Monk, P. Zanotti-Fregonara, J-S Liow, R. Xu, V.W. Pike, R.B. Innis and L.A. Arendt-Nielsen
(Denmark and USA)
49. The mGluR7 negative modulation alleviates pain and affective/cognitive deficit in neuropathic mice.
E. Palazzo, R. Romano, S. Boccella, L. Luongo, F. Rossi and S. Maione (Italy)
50. Positive allosteric modulators (PAMS) of Metabotropic Glutamate Receptor 2 (mGluR2) are effective nerve
injury induces facial allodynia in rats
Cs. Horváth, K. Galgóczy, K. Sz. Kordás, Á. Kis-Varga, Gy. Túrós, Gy. Szabó and K. Gál (Hungary)
51. N-Acetyl-Cysteine, a drug that facilitates the endogenous activation mGlu2/3 receptors, inhibits
nociceptive transmission in humansa
A.Truini, S. Piroso, E. Pasquale, S. Notartomaso, G. Di Stefano, R.Lattanzi, F. Nicoletti, G. Battaglia and
G. Cruccu (Italy)
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Poster session rev1
Autism
52. Acute biochemical and behavioural effects of indirect activation of presynaptic inhibitory mGluR2/3 by Nacetylcysteine in the mouse.
A.Durieux,C. Fernandes, D.Murphy, M. Labouesse,S.Giovanoli, J. Horder, U. Meyer,
P. So and G. McAlonan (UK and Switzerland)
53. mGlu7 is Critical for Hippocampal Plasticity and is a Potential Therapeutic Target for the
Treatment of Rett Syndrome
R. Klar, R.G. Gogliotti, A.G. Walker, R. Zamorano, J.M. Rook, Z. Xiang, P.J. Conn and C.M. Niswender (USA)
54. The development of mGlu5 positive allosteric modulators as Rettsyndrome therapeutics
R. Gogliotti, R.Klar, A.Ghoshal, R.Zamorano, J.Rook,S. Stauffer, C. Lindsley, P.J.Conn and
C.M. Niswender (USA)
55. Altered mGlu5 receptor surface dynamics are linked to abnormal NMDA receptor function and plasticity in
Fragile X Syndrome
E. Aloisi, J.P. Dupuis, L. Costa, M.G. Haberl, M. Ginger, L. Ladépêche, F. Drago, P.V. Piazza, L. Ciranna,
L. Groc , M.V. Catania and A. Frick (Italy and France)
56. Metabotropic glutamate subtype 5 (mGlu5) receptor-mediated modulation of the interaction between
Fragile X Mental Retardation Protein (FMRP) and the Fragile X related (FXR) proteins FXR1P and FXR2P.
C. M. Bonaccorso, S. D’Antoni, M. Spatuzza, B. Di Marco, G. Barrancotto, S.A. Musumeci, L. Davidovic,
B. Bardoni, M. V. Catania (Italy and France)
57. Selective disruption of mGluR5-homer interactions mimics multiple phenotypes of fragile X syndrome in
mice G.Molinaro,, K.A. Collins, W. Guo, C. M. Reyes, R. Paylor, K.K. Szumlinski, P.F. Worley and K. M. Huber
(USA)
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58. Abnormalities in Subcortical Glutamate/Glutamine, But Not GABA, In Adults With An ASD – A [1H]MRS
Study
J. Horder, M. Mendez, N. Gillan, S. Coghlan and D. Murphy (UK)
59. A Visual Perceptual Task Provides Evidence for an Excitatory:Inhibitory Imbalance in Adults with Autism
M. Mendez, J. Horder, D. Spain, J.Faulkner, J.D. De La Harpe Golden and D. Murphy (UK)
Psychiatric disorders
60. Synthesis and Optimization of Small Molecule Negative Allosteric Modulators (NAMs) of Group II
Metabotropic Glutamate Receptors (mGlus) for the Treatment of Mental Disorders
R.P. Dhanya, D.J. Sheffler, A. Herath, M. Davis, P.S. Lee, L. Yang, H.H. Nickols, H.P. Cho, P.J. Conn,
A. Der-Avakian, A. Markou and N.D.P. Cosford (USA)
61. The effect of mGlu4 selective agonist, LSP-42022 on the immobility time in the TST and in the FST in mice.
A.Pałucha-Poniewiera , M.Marciniak , K.Podkowa, F. Acher and A.Pilc (Poland)
62. Blocking Metabotropic Glutamate Receptor Subtype 7 (mGlu7) via the Venus Flytrap Domain (VFTD)
Inhibits Amygdala Plasticity, Stress, and Anxiety-related Behavior
D. Peterlik, C. E. Gee, C. Neuhäuser, R. Bouhelal, K. Kaupmann, G. Laue, N. Uschold-Schmidt, D. Feuerbach,
K. Zimmermann, S. Ofner, J. F. Cryan, H. van der Putten, M. Fendt, I. Vranesic, R. Glatthar and P. J. Flor
(Germany, Switzerland and Ireland)
Poster session rev1
63. Modulation of mGlu7 Receptor Function Relieves Behavioral and Physiological Consequences Induced by
Chronic Psychosocial Stress
D. Peterlik, A. Bludau,T. Killian, D. Grabski, S. O. Reber, P. J. Flor and N. Uschold-Schmidt (Germany)
64. Ketamine reduces evoked [3H]-D-aspartate release in the prefrontal cortex of Flinders Sensitive Line rats
H.K. Müller, G. Treccani, K.G. du Jardin, G. Wegener and B. Elfving (Denmark)
65. Metabolomics Study of LY3020371, a potent and selective mGlu2/3 receptor antagonist, and Ketamine in
Rats
M. Kuo, V. Tolstikov, A. Nikolayev, H. Wu, J.M. Witkin and J.A. Monn (USA)
66. The pharmacological studies of mGlu5-GABAB interplay in animal models of psychosis.
JM. Wierońska, M. Woźniak, N. Kłeczek and A. Pilc (Poland)
67. Modulation of the rab GDP dissociation inhibitor (GDI) discloses a pharmacodynamic difference between
the mGlu2/3 receptor agonists, LY379268 and LY354740.
R. Orlando, M. Borro, M. Motolese, G. Molinaro, S. Scaccianoce, A. Caruso, L. di Nuzzo, F. Caraci,
C. De Lucia, F. Matrisciano, A. Pittaluga, J. Mairesse, M. Simmaco, R. Nisticò, J. A. Monn and F. Nicoletti
(Italy and USA)
Addiction
68. Ethanol dependence and withdrawal in immature and mature rat organotypic hippocampal slice cultures:
different mechanisms mediated by ionotropic and metabotropic glutamate receptors.
E. Gerace, E. Landucci, A. Totti, I. Orsini, V. Mazzucco, F. Moroni, G. Mannaioni and
D.E. Pellegrini-Giampietro(Italy)
69. Activation of Metabotropic Glutamate Receptor 7 attenuates nicotine taking and nicotine seeking in rats
X .Li, A. Stoker and A. Markou (USA)
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Neurodegenerative and neuroinflammatory disorders
70. Activation of group-I metabotropic glutamate receptors impairs stress granules formation and enhances
cellular damage under stress condition.
B. Di Marco, P. Dell'Albani, M. Spatuzza, C. M. Bonaccorso, S. D'Antoni, B. Bardoni, F. Drago, M.V. Catania
(Italy and France)
71. Profiling Hippocampal Neuronsafter Early Preconditioning with Certain Excitatory Amino Acids
RevealsmGluR3 and mGluR7Contribute to Neuronal Survival
L.K. Friedman and A.M. Slomko (USA)
72. Epigenetic down-regulation of type-2 metabotropic glutamate receptors is linked to selective neuronal
vulnerability following global transient brain ischemia
M. Motolese, M. Cannella, F. Mastroiacovo, A. Gaglione, B. Riozzi, L. Di Menna, R. Gradini, G. Battaglia,
V. Bruno and F. Nicoletti (Italy and France)
73. mGlu4 receptor positive allosteric modulators exert different action at corticostriatal vs. striatopallidal
synapses: implications for Parkinson's disease treatment
P. Gubellini, E. Dale, C. Melon, L. Kerkerian-Le Goff and D. Doller (France and USA)
74. Novel Metabotropic Glutamate Receptor 4 (mGlu4) Positive Allosteric Modulators For Multiple Sclerosis: in
vitro and in vivo Pharmacological Characterization
S. Célanire, C. Mordant, M. Heroux, I. Royer-Urios, C. Orabona, C. Volpi, G. Mondanelli, M. T. Pallotta,
F. Fallarino,L. Galibert, S. Poli and U. Grohmann (Switzerland and Italy)
Poster session rev1
75. Effects of group III mGluRs modulation in the globuspallidus of Parkinsonian rats
T. Deltheil, N. Turle-Lorenzo and M. Amalric (France)
76. Adaptive changes in the expression of Grm4 and Grm5 genes in the mouse striatum of acute models of
drug-induced parkinsonism
M. Cannella, M. Motolese, D. Bucci, G. Molinaro, A. Traficante, J. Marrocco, V. Bruno, F. Nicoletti and
G. Battaglia (Italy)
77. Imaging the antiparkinsonian effects of the novel Metabotropic Glutamate Receptor subtype 4 positive
allosteric modulator ADX88178
N. Byun, A. Huang, R. A. Baheza, R. L. Barry, C.W. Lindsley, C. Hopkins, C. Niswender, C. K. Jones, J. C. Gore
and P. J. Conn (USA)
78. The metabotropic glutamate receptor subtype 5 positive allosteric modulator VU0360172modulates
dopaminergiccircuits
N. Byun, A. Ghoshal, R.L. Barry, R.A. Baheza, W. Pham, J.C. Gore and P.J. Conn (USA)
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