-
1
-
-
50249155962
-
-
W: mGluR5 antagonists: Discovery, characterization and drug development. Curr Opin Drug Discovery Dev (2008) 11(5): 655-665.
-
W: mGluR5 antagonists: Discovery, characterization and drug development. Curr Opin Drug Discovery Dev (2008) 11(5): 655-665.
-
-
-
-
2
-
-
40749139454
-
mGlu5 receptor antagonists and their therapeutic potential
-
Jaeschke G, Wettstein JG, Nordquist RE, Spooren W: mGlu5 receptor antagonists and their therapeutic potential.Expert Opin Ther Patents (2008) 18(2):123-142.
-
(2008)
Expert Opin Ther Patents
, vol.18
, Issue.2
, pp. 123-142
-
-
Jaeschke, G.1
Wettstein, J.G.2
Nordquist, R.E.3
Spooren, W.4
-
3
-
-
35949000501
-
Recent progress in the development of allosteric modulators of mGluR5
-
Rodriguez AL, Williams R: Recent progress in the development of allosteric modulators of mGluR5. Curr Opin Drug Discovery Dev (2007) 10(6):715-722.
-
(2007)
Curr Opin Drug Discovery Dev
, vol.10
, Issue.6
, pp. 715-722
-
-
Rodriguez, A.L.1
Williams, R.2
-
4
-
-
34147127072
-
Metabotropic glutamate receptor 5 modulators and their therapeutic applications
-
Bach P, Isaac M, Slassi A: Metabotropic glutamate receptor 5 modulators and their therapeutic applications. Expert Opin Ther Patents (2007) 17(4):371-384.
-
(2007)
Expert Opin Ther Patents
, vol.17
, Issue.4
, pp. 371-384
-
-
Bach, P.1
Isaac, M.2
Slassi, A.3
-
5
-
-
0032834028
-
Pharmacological agents acting at subtypes of metabotropic glutamate receptors
-
Provides a historical perspective of the evolution of the mGluR field as a therapeutic target, ·
-
Schoepp DD, Jane DE, Monn JA: Pharmacological agents acting at subtypes of metabotropic glutamate receptors.Neuropharmacology (1999) 38(10):1431-1476. · Provides a historical perspective of the evolution of the mGluR field as a therapeutic target.
-
(1999)
Neuropharmacology
, vol.38
, Issue.10
, pp. 1431-1476
-
-
Schoepp, D.D.1
Jane, D.E.2
Monn, J.A.3
-
6
-
-
0030995878
-
Pharmacology and functions of metabotropic glutamate receptors
-
Thoroughly discusses the pharmacology, function and therapeutic potential of the mGluRs, ·
-
Conn PJ, Pin J-P: Pharmacology and functions of metabotropic glutamate receptors. Annu Rev Pharmacol Toxicol (1997) 37:205- 237. · Thoroughly discusses the pharmacology, function and therapeutic potential of the mGluRs.
-
(1997)
Annu Rev Pharmacol Toxicol
, vol.37
, pp. 205-237
-
-
Conn, P.J.1
Pin, J.-P.2
-
7
-
-
26444616159
-
Molecular pharmacology and therapeutic prospects of metabotropic glutamate receptor allosteric modulators
-
Ritzén A, Mathiesen JM, Thomsen C: Molecular pharmacology and therapeutic prospects of metabotropic glutamate receptor allosteric modulators. Basic Clin Pharmacol Toxicol (2005) 97(4):202-213.
-
(2005)
Basic Clin Pharmacol Toxicol
, vol.97
, Issue.4
, pp. 202-213
-
-
Ritzén, A.1
Mathiesen, J.M.2
Thomsen, C.3
-
8
-
-
8844263762
-
Positive and negative allosteric modulation of metabotropic glutamate receptors: Emerging therapeutic potential
-
Kew JN: Positive and negative allosteric modulation of metabotropic glutamate receptors: Emerging therapeutic potential. Pharmacol Ther (2004) 104(3):233-244.
-
(2004)
Pharmacol Ther
, vol.104
, Issue.3
, pp. 233-244
-
-
Kew, J.N.1
-
9
-
-
0032853255
-
2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systematically active mGlu5 receptor antagonist
-
Details the early in vitro and in vivo pharmacological characterization of MPEP, ··
-
Gasparini F, Lingenhöhl K, Stoehr N, Flor PJ, Heinrich M, Vranesic I, Biollaz M, Allgeier H, Heckendorn R, Urwyler S, Varney MA et al: 2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systematically active mGlu5 receptor antagonist. Neuropharmacology (1999) 38(10):1493-1503. ·· Details the early in vitro and in vivo pharmacological characterization of MPEP.
-
(1999)
Neuropharmacology
, vol.38
, Issue.10
, pp. 1493-1503
-
-
Gasparini, F.1
Lingenhöhl, K.2
Stoehr, N.3
Flor, P.J.4
Heinrich, M.5
Vranesic, I.6
Biollaz, M.7
Allgeier, H.8
Heckendorn, R.9
Urwyler, S.10
Varney, M.A.11
-
10
-
-
0037448394
-
3-[(2-Methyl- 1,3-thiazol-4-yl)ethynyl]-pyridine: A potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity
-
Cosford ND, Tehrani L, Roppe J, Schweiger E, Smith ND, Anderson J, Bristow L, Brodkin J, Jiang X, McDonald I, Rao S et al: 3-[(2-Methyl- 1,3-thiazol-4-yl)ethynyl]-pyridine: A potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. J Med Chem (2003) 46(2):204-206.
-
(2003)
J Med Chem
, vol.46
, Issue.2
, pp. 204-206
-
-
Cosford, N.D.1
Tehrani, L.2
Roppe, J.3
Schweiger, E.4
Smith, N.D.5
Anderson, J.6
Bristow, L.7
Brodkin, J.8
Jiang, X.9
McDonald, I.10
Rao, S.11
-
11
-
-
8844238423
-
Effects of MPEP on locomotion, sensitization and conditioned reward induced by cocaine or morphine
-
Herzig V, Schmidt WJ: Effects of MPEP on locomotion, sensitization and conditioned reward induced by cocaine or morphine. Neuropharmacology (2004) 47(7):973-984.
-
(2004)
Neuropharmacology
, vol.47
, Issue.7
, pp. 973-984
-
-
Herzig, V.1
Schmidt, W.J.2
-
12
-
-
28344451556
-
The mGluR5 antagonist MPEP selectively inhibits the onset and maintenance of ethanol self-administration in C57BL/6J mice
-
Hodge CW, Miles MF, Sharko AC, Stevenson RA, Hillmann JR, Lepoutre V, Besheer J, Schroeder JP: The mGluR5 antagonist MPEP selectively inhibits the onset and maintenance of ethanol self-administration in C57BL/6J mice.Psychopharmacology (2006) 183(4):429-438.
-
(2006)
Psychopharmacology
, vol.183
, Issue.4
, pp. 429-438
-
-
Hodge, C.W.1
Miles, M.F.2
Sharko, A.C.3
Stevenson, R.A.4
Hillmann, J.R.5
Lepoutre, V.6
Besheer, J.7
Schroeder, J.P.8
-
13
-
-
9944223305
-
Assessing the role of metabotropic glutamate receptor 5 in multiple nociceptive modalities
-
Zhu CZ, Wilson SG, Mikusa JP, Wismer CT, Gauvin DM, Lynch JJ 3rd, Wade CL, Decker MW, Honore P: Assessing the role of metabotropic glutamate receptor 5 in multiple nociceptive modalities. Eur J Pharmacol (2004) 506(2):107-118.
-
(2004)
Eur J Pharmacol
, vol.506
, Issue.2
, pp. 107-118
-
-
Zhu, C.Z.1
Wilson, S.G.2
Mikusa, J.P.3
Wismer, C.T.4
Gauvin, D.M.5
Lynch 3rd, J.J.6
Wade, C.L.7
Decker, M.W.8
Honore, P.9
-
14
-
-
18844364756
-
Anxiolytic-like effects of mGlu1 and mGlu5 receptor antagonists in rats
-
Pietraszek M, Sukhanov I, Maciejak P, Szyndler J, Gravius A, Wisłowska A, Płaźnik A, Bespalov AY, Danysz W: Anxiolytic-like effects of mGlu1 and mGlu5 receptor antagonists in rats.Eur J Pharmacol (2005) 514(1):25-34.
-
(2005)
Eur J Pharmacol
, vol.514
, Issue.1
, pp. 25-34
-
-
Pietraszek, M.1
Sukhanov, I.2
Maciejak, P.3
Szyndler, J.4
Gravius, A.5
Wisłowska, A.6
Płaźnik, A.7
Bespalov, A.Y.8
Danysz, W.9
-
15
-
-
3042685523
-
The behavioral profile of the potent and selective mGlu5 receptor antagonist 3-(2-methyl-1,3-thiazol-4-yl)ethynyl] pyridine (MTEP) in rodent models of anxiety
-
Busse CS, Brodkin J, Tattersall D, Anderson JJ, Warren N, Tehrani L, Bristow LJ, Varney MA, Cosford ND: The behavioral profile of the potent and selective mGlu5 receptor antagonist 3-(2-methyl-1,3-thiazol-4-yl)ethynyl] pyridine (MTEP) in rodent models of anxiety. Neuropsychopharmacology (2004) 29(11):1971-1979.
-
(2004)
Neuropsychopharmacology
, vol.29
, Issue.11
, pp. 1971-1979
-
-
Busse, C.S.1
Brodkin, J.2
Tattersall, D.3
Anderson, J.J.4
Warren, N.5
Tehrani, L.6
Bristow, L.J.7
Varney, M.A.8
Cosford, N.D.9
-
16
-
-
3042683441
-
Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABAA signaling
-
Klodzinska A, TatarczyŃska E, Chojnacka-Wójcik E, Nowak G, Cosford ND, Pilc A: Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABAA signaling. Neuropharmacol (2004) 47(3):342-350.
-
(2004)
Neuropharmacol
, vol.47
, Issue.3
, pp. 342-350
-
-
Klodzinska, A.1
TatarczyŃska, E.2
Chojnacka-Wójcik, E.3
Nowak, G.4
Cosford, N.D.5
Pilc, A.6
-
17
-
-
0033680311
-
Anxiolytic-like effects of the prototypical metabotropic glutamate receptor 5 antagonist 2-methyl-6- (phenylethynyl)pyridine in rodents
-
Spooren WPJM, Vassout A, Neijt HC, Kuhn R, Gasparini F, Roux S, Porsolt RD, Gentsch C: Anxiolytic-like effects of the prototypical metabotropic glutamate receptor 5 antagonist 2-methyl-6- (phenylethynyl)pyridine in rodents. J Pharmacol Exp Ther (2000) 295(3):1267-1275.
-
(2000)
J Pharmacol Exp Ther
, vol.295
, Issue.3
, pp. 1267-1275
-
-
Spooren, W.P.J.M.1
Vassout, A.2
Neijt, H.C.3
Kuhn, R.4
Gasparini, F.5
Roux, S.6
Porsolt, R.D.7
Gentsch, C.8
-
18
-
-
27744549064
-
Transient lower esophageal sphincter relaxations in dogs are inhibited by a metabotropic glutamate receptor 5 antagonist
-
Jensen J, Lehmann A, Uvebrant A, Carlsson A, Jerndal G, Nilsson K, Frisby C, Blackshaw LA, Mattsson JP: Transient lower esophageal sphincter relaxations in dogs are inhibited by a metabotropic glutamate receptor 5 antagonist. Eur J Pharmacol (2005) 519(1-2):154-157.
-
(2005)
Eur J Pharmacol
, vol.519
, Issue.1-2
, pp. 154-157
-
-
Jensen, J.1
Lehmann, A.2
Uvebrant, A.3
Carlsson, A.4
Jerndal, G.5
Nilsson, K.6
Frisby, C.7
Blackshaw, L.A.8
Mattsson, J.P.9
-
19
-
-
24144487047
-
Inhibition of transient lower esophageal sphincter relaxation and gastroesophageal reflux by metabotropic glutamate receptor ligands
-
Frisby CL, Mattsson JP, Jensen JM, Lehmann A, Dent J, Blackshaw LA: Inhibition of transient lower esophageal sphincter relaxation and gastroesophageal reflux by metabotropic glutamate receptor ligands. Gastroenterology(2005) 129(3):995-1004.
-
(2005)
Gastroenterology
, vol.129
, Issue.3
, pp. 995-1004
-
-
Frisby, C.L.1
Mattsson, J.P.2
Jensen, J.M.3
Lehmann, A.4
Dent, J.5
Blackshaw, L.A.6
-
20
-
-
44949125523
-
Rescue of behavioral phenotype and neuronal protrusion morphology in Fmr1 KO mice
-
de Vrij FM, Levenga J, van der Linde HC, Koekkoek SK, De Zeeuw CI, Nelson DL, Oostra BA, Willemsen R: Rescue of behavioral phenotype and neuronal protrusion morphology in Fmr1 KO mice. Neurobiol Dis (2008) 31(1):127-132.
-
(2008)
Neurobiol Dis
, vol.31
, Issue.1
, pp. 127-132
-
-
de Vrij, F.M.1
Levenga, J.2
van der Linde, H.C.3
Koekkoek, S.K.4
De Zeeuw, C.I.5
Nelson, D.L.6
Oostra, B.A.7
Willemsen, R.8
-
21
-
-
24344457816
-
Suppression of two major fragile X Syndrome mouse model phenotypes by the mGluR5 antagonist MPEP
-
Yan QJ, Rammal M, Tranfaglia M, Bauchwitz RP: Suppression of two major fragile X Syndrome mouse model phenotypes by the mGluR5 antagonist MPEP. Neuropharmacol (2005) 49(7): 1053-1066.
-
(2005)
Neuropharmacol
, vol.49
, Issue.7
, pp. 1053-1066
-
-
Yan, Q.J.1
Rammal, M.2
Tranfaglia, M.3
Bauchwitz, R.P.4
-
22
-
-
58149462237
-
Metabotropic glutamate receptors 5 blockade reverses spatial memory deficits in a mouse model of Parkinson's disease
-
Leonibus ED, Managò F, Giordani F, Petrosino F, Lopez S, Oliverio A, Amalric M, Mele A: Metabotropic glutamate receptors 5 blockade reverses spatial memory deficits in a mouse model of Parkinson's disease. Neuropsychopharmacology (2009) 34(3):729-738.
-
(2009)
Neuropsychopharmacology
, vol.34
, Issue.3
, pp. 729-738
-
-
Leonibus, E.D.1
Managò, F.2
Giordani, F.3
Petrosino, F.4
Lopez, S.5
Oliverio, A.6
Amalric, M.7
Mele, A.8
-
23
-
-
53149127661
-
Antagonism of glutamatergic NMDA and mGluR5 receptors decreases consumption of food in baboon model of binge-eating disorder
-
Bisaga A, Danysz W, Foltin RW: Antagonism of glutamatergic NMDA and mGluR5 receptors decreases consumption of food in baboon model of binge-eating disorder.Eur Neuropsychopharmacol (2008) 18(11):794-802.
-
(2008)
Eur Neuropsychopharmacol
, vol.18
, Issue.11
, pp. 794-802
-
-
Bisaga, A.1
Danysz, W.2
Foltin, R.W.3
-
24
-
-
0035197286
-
mGluR5 antagonists 2-methyl-6-(phenylethynyl)- pyridine and (E)-2-methyl-6-(2-phenylethenyl)-pyridine reduce traumatic neuronal injury in vitro and in vivo by antagonizing N-methyl d-aspartate receptors
-
Movsesyan VA, O'Leary DM, Fan L, Bao W, Mullins PG, Knoblach SM, Faden AI: mGluR5 antagonists 2-methyl-6-(phenylethynyl)- pyridine and (E)-2-methyl-6-(2-phenylethenyl)-pyridine reduce traumatic neuronal injury in vitro and in vivo by antagonizing N-methyl d-aspartate receptors. J Pharmacol Exp Ther (2001) 296(1):41-47.
-
(2001)
J Pharmacol Exp Ther
, vol.296
, Issue.1
, pp. 41-47
-
-
Movsesyan, V.A.1
O'Leary, D.M.2
Fan, L.3
Bao, W.4
Mullins, P.G.5
Knoblach, S.M.6
Faden, A.I.7
-
25
-
-
0037363728
-
Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP
-
Mathiesen JM, Svendsen N, Bräuner-Osborne H, Thomsen C, Ramirez MT: Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP. Br J Pharmacol (2003) 138(6):1026-1030.
-
(2003)
Br J Pharmacol
, vol.138
, Issue.6
, pp. 1026-1030
-
-
Mathiesen, J.M.1
Svendsen, N.2
Bräuner-Osborne, H.3
Thomsen, C.4
Ramirez, M.T.5
-
26
-
-
2942525894
-
Inhibition of human hepatic CYP isoforms by mGluR5 antagonists
-
King CD: Inhibition of human hepatic CYP isoforms by mGluR5 antagonists. Life Sci 75(8):947-953.
-
Life Sci
, vol.75
, Issue.8
, pp. 947-953
-
-
King, C.D.1
-
27
-
-
28444457736
-
In vitro metabolic studies on the selective metabotropic glutamate receptor sub-type 5 (mGluR5) antagonist 3-[(2-methyl-1,3-thiazol-4- yl)ethynyl]-pyridine (MTEP)
-
Green MD, Yang X, Cramer M, King CD: In vitro metabolic studies on the selective metabotropic glutamate receptor sub-type 5 (mGluR5) antagonist 3-[(2-methyl-1,3-thiazol-4- yl)ethynyl]-pyridine (MTEP). Neurosci Lett (2006) 391(3):91-95.
-
(2006)
Neurosci Lett
, vol.391
, Issue.3
, pp. 91-95
-
-
Green, M.D.1
Yang, X.2
Cramer, M.3
King, C.D.4
-
28
-
-
34447515618
-
-
Carroll FI, Kotturi SV, Navarro HA, Mascarella SW, Gilmour BP, Smith FL, Gabra BH, Dewey WL: Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl) pyridine. J Med Chem(2007) 50(14):3388-3391.
-
Carroll FI, Kotturi SV, Navarro HA, Mascarella SW, Gilmour BP, Smith FL, Gabra BH, Dewey WL: Synthesis and pharmacological evaluation of phenylethynyl[1,2,4]methyltriazines as analogues of 3-methyl-6-(phenylethynyl) pyridine. J Med Chem(2007) 50(14):3388-3391.
-
-
-
-
29
-
-
32344445040
-
Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl] pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications
-
Iso Y, Grajkowska E, Wroblewski JT, Davis J, Goeders NE, Johnson KM, Sanker S, Roth BL, Tueckmantel W, Kozikowski AP: Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl] pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.J Med Chem (2006) 49(3):1080-1110.
-
(2006)
J Med Chem
, vol.49
, Issue.3
, pp. 1080-1110
-
-
Iso, Y.1
Grajkowska, E.2
Wroblewski, J.T.3
Davis, J.4
Goeders, N.E.5
Johnson, K.M.6
Sanker, S.7
Roth, B.L.8
Tueckmantel, W.9
Kozikowski, A.P.10
-
30
-
-
40849123742
-
Phenylethynylpyrrolo[ 1,2-a]pyrazine: A new potent and selective tool in the mGluR5 antagonist arena
-
Micheli F, Bertani B, Bozzoli A, Crippa L, Cavanni P, Di Fabio R, Donati D, Marzorati P, Merlo G, Paio A, Perugini L et al: Phenylethynylpyrrolo[ 1,2-a]pyrazine: A new potent and selective tool in the mGluR5 antagonist arena. Bioorg Med Chem Lett (2008) 18(6):1804-1809.
-
(2008)
Bioorg Med Chem Lett
, vol.18
, Issue.6
, pp. 1804-1809
-
-
Micheli, F.1
Bertani, B.2
Bozzoli, A.3
Crippa, L.4
Cavanni, P.5
Di Fabio, R.6
Donati, D.7
Marzorati, P.8
Merlo, G.9
Paio, A.10
Perugini, L.11
-
31
-
-
47149106805
-
Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: Unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold
-
Describes a 'molecular switch' that affords both negative and positive allosteric modulators of mGluR5 within the same chemical series, ··
-
Sharma S, Rodriguez AL, Conn PJ, Lindsley CW: Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: Unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.Bioorg Med Chem Lett (2008) 18(14):4098-4101. ·· Describes a 'molecular switch' that affords both negative and positive allosteric modulators of mGluR5 within the same chemical series.
-
(2008)
Bioorg Med Chem Lett
, vol.18
, Issue.14
, pp. 4098-4101
-
-
Sharma, S.1
Rodriguez, A.L.2
Conn, P.J.3
Lindsley, C.W.4
-
32
-
-
27844482134
-
A close structural analog of 2-methyl-6- (phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators
-
Describes the pharmacology of a neutral allosteric ligand of mGluR5 and two partial antagonists that bind at the same allosteric site, ·
-
Rodriguez AL, Nong Y, Sekaran NK, Alagille D, Tamagnan GD, Conn PJ: A close structural analog of 2-methyl-6- (phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators.Mol Pharmacol (2005) 68(6):1793-1802. · Describes the pharmacology of a neutral allosteric ligand of mGluR5 and two partial antagonists that bind at the same allosteric site.
-
(2005)
Mol Pharmacol
, vol.68
, Issue.6
, pp. 1793-1802
-
-
Rodriguez, A.L.1
Nong, Y.2
Sekaran, N.K.3
Alagille, D.4
Tamagnan, G.D.5
Conn, P.J.6
-
33
-
-
33646923402
-
Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists
-
Kulkarni SS, Nightingale B, Dersch CM, Rothman RB, Newman AH: Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett(2006) 16(13):3371-3375.
-
(2006)
Bioorg Med Chem Lett
, vol.16
, Issue.13
, pp. 3371-3375
-
-
Kulkarni, S.S.1
Nightingale, B.2
Dersch, C.M.3
Rothman, R.B.4
Newman, A.H.5
-
34
-
-
33947166901
-
Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists
-
Kulkarni SS, Newman AH: Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett (2007) 17(7):2074- 2079.
-
(2007)
Bioorg Med Chem Lett
, vol.17
, Issue.7
, pp. 2074-2079
-
-
Kulkarni, S.S.1
Newman, A.H.2
-
35
-
-
16244380185
-
Dipyridyl amides: Potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists
-
Bonnefous C, Vernier J-M, Hutchinson JH, Chung J, Reyes-Manalo G, Kamenecka T: Dipyridyl amides: Potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.Bioorg Med Chem Lett (2005) 15(4):1197-1200.
-
(2005)
Bioorg Med Chem Lett
, vol.15
, Issue.4
, pp. 1197-1200
-
-
Bonnefous, C.1
Vernier, J.-M.2
Hutchinson, J.H.3
Chung, J.4
Reyes-Manalo, G.5
Kamenecka, T.6
-
36
-
-
23944483488
-
Dipyridyl amines: Potent metabotropic glutamate subtype 5 receptor antagonists
-
Kamenecka TM, Bonnefous C, Govek S, Vernier J-M, Hutchinson J, Chung J, Reyes-Manalo G, Anderson JJ: Dipyridyl amines: Potent metabotropic glutamate subtype 5 receptor antagonists. Bioorg Med Chem Lett (2005) 15(19):4350-4353.
-
(2005)
Bioorg Med Chem Lett
, vol.15
, Issue.19
, pp. 4350-4353
-
-
Kamenecka, T.M.1
Bonnefous, C.2
Govek, S.3
Vernier, J.-M.4
Hutchinson, J.5
Chung, J.6
Reyes-Manalo, G.7
Anderson, J.J.8
-
37
-
-
34248176184
-
Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists
-
Kulkarni SS, Newman AH: Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett (2007) 17(11):2987-2991.
-
(2007)
Bioorg Med Chem Lett
, vol.17
, Issue.11
, pp. 2987-2991
-
-
Kulkarni, S.S.1
Newman, A.H.2
-
38
-
-
34447340637
-
-
Milbank JB, Knauer CS, Augelli-Szafran CE, Sakkab-Tan AT, Lin KK, Yamagata K, Hoffman JK, Zhuang N, Thomas J, Galatsis P, Wendt JA et al: Rational design of 7-arylquinolines as noncompetitive metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett (2007) 17(16):4415-4418. ·· Describes the discovery of an mGluR5 NAM from a chemotype other than MPEP with activity in a rodent anxiety model when administered orally.
-
Milbank JB, Knauer CS, Augelli-Szafran CE, Sakkab-Tan AT, Lin KK, Yamagata K, Hoffman JK, Zhuang N, Thomas J, Galatsis P, Wendt JA et al: Rational design of 7-arylquinolines as noncompetitive metabotropic glutamate receptor subtype 5 antagonists. Bioorg Med Chem Lett (2007) 17(16):4415-4418. ·· Describes the discovery of an mGluR5 NAM from a chemotype other than MPEP with activity in a rodent anxiety model when administered orally.
-
-
-
-
39
-
-
0015004136
-
A simple and reliable conflict procedure for testing anti-anxiety
-
Vogel JR, Beer B, Clody DE: A simple and reliable conflict procedure for testing anti-anxiety. Psychopharmacologia (1971) 21(1):1-7.
-
(1971)
Psychopharmacologia
, vol.21
, Issue.1
, pp. 1-7
-
-
Vogel, J.R.1
Beer, B.2
Clody, D.E.3
-
40
-
-
34548563730
-
-
Wendt JA, Deeter SD, Bove SE, Knauer CS, Brooker RM, Augelli-Szafran CE, Schwarz RD, Kinsora JJ, Kilgore KS: Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists. Bioorg Med Chem Lett (2007) 17(19): 5396-5399. ·· Describes the discovery of an mGluR5 NAM from a chemotype other than MPEP with activity in a rodent model of OA pain when administered orally.
-
Wendt JA, Deeter SD, Bove SE, Knauer CS, Brooker RM, Augelli-Szafran CE, Schwarz RD, Kinsora JJ, Kilgore KS: Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists. Bioorg Med Chem Lett (2007) 17(19): 5396-5399. ·· Describes the discovery of an mGluR5 NAM from a chemotype other than MPEP with activity in a rodent model of OA pain when administered orally.
-
-
-
-
41
-
-
0242606943
-
Weight bearing as a measure of disease progression and efficacy of anti-inflammatory compounds in a model of monosodium iodoacetate-induced osteoarthritis
-
Bove SE, Calcaterra SL, Brooker RM, Huber CM, Guzman RE, Juneau PL, Schrier DJ, Kilgore KS: Weight bearing as a measure of disease progression and efficacy of anti-inflammatory compounds in a model of monosodium iodoacetate-induced osteoarthritis. Osteoarthritis Cartilage (2003) 11(11):821-830.
-
(2003)
Osteoarthritis Cartilage
, vol.11
, Issue.11
, pp. 821-830
-
-
Bove, S.E.1
Calcaterra, S.L.2
Brooker, R.M.3
Huber, C.M.4
Guzman, R.E.5
Juneau, P.L.6
Schrier, D.J.7
Kilgore, K.S.8
-
42
-
-
35648935910
-
Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists
-
Galatsis P, Yamagata K, Wendt JA, Connolly CJ, Mickelson JW, Milbank JB, Bove SE, Knauer CS, Brooker RM, Augelli-Szafran CE, Schwarz RD et al: Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists. Bioorg Med Chem Lett (2007) 17(23):6525-6528.
-
(2007)
Bioorg Med Chem Lett
, vol.17
, Issue.23
, pp. 6525-6528
-
-
Galatsis, P.1
Yamagata, K.2
Wendt, J.A.3
Connolly, C.J.4
Mickelson, J.W.5
Milbank, J.B.6
Bove, S.E.7
Knauer, C.S.8
Brooker, R.M.9
Augelli-Szafran, C.E.10
Schwarz, R.D.11
-
43
-
-
65749112588
-
Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype
-
Describes the first example in a chemical series not based on MPEP of a 'molecular switch' capable of producing both positive and negative allosteric modulators of mGluR5, ··
-
Rodriguez AL, Williams R, Zhou Y, Lindsley SR, Le U, Grier MD, Weaver D, Conn PJ, Lindsley CW: Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype. Bioorg Med Chem Lett (2009) 19(12):3209-3213. ·· Describes the first example in a chemical series not based on MPEP of a 'molecular switch' capable of producing both positive and negative allosteric modulators of mGluR5.
-
(2009)
Bioorg Med Chem Lett
, vol.19
, Issue.12
, pp. 3209-3213
-
-
Rodriguez, A.L.1
Williams, R.2
Zhou, Y.3
Lindsley, S.R.4
Le, U.5
Grier, M.D.6
Weaver, D.7
Conn, P.J.8
Lindsley, C.W.9
-
44
-
-
46749144280
-
-
Addex Pharmaceuticals Inc: Addex announces ADX10059 phase IIa acute anxiety data, January 03
-
Addex Pharmaceuticals Inc: Addex announces ADX10059 phase IIa acute anxiety data. Press Release (2008) January 03.
-
(2008)
Press Release
-
-
-
45
-
-
67649914862
-
-
Addex Pharmaceuticals Inc: Addex: Better tolerated formulation of ADX10059 reduces acid reflux. Press Release (2008) September 10. · Describes clinical data providing further validation of mGluR5 NAMs as a potential treatment for GERD in humans.
-
Addex Pharmaceuticals Inc: Addex: Better tolerated formulation of ADX10059 reduces acid reflux. Press Release (2008) September 10. · Describes clinical data providing further validation of mGluR5 NAMs as a potential treatment for GERD in humans.
-
-
-
-
46
-
-
67649920345
-
Addex starts phase IIb ADX10059, proton pump inhibitor combination study in GERD patients
-
Addex Pharmaceuticals Inc:, December 02
-
Addex Pharmaceuticals Inc: Addex starts phase IIb ADX10059, proton pump inhibitor combination study in GERD patients.Press Release (2008) December 02.
-
(2008)
Press Release
-
-
-
48
-
-
46749144280
-
-
Addex Pharmaceuticals Inc: Addex starts a phase IIb trial of ADX10059 for migraine prevention, December 17
-
Addex Pharmaceuticals Inc: Addex starts a phase IIb trial of ADX10059 for migraine prevention. Press Release (2008) December 17.
-
(2008)
Press Release
-
-
-
49
-
-
67649893112
-
-
FRAXA Research Foundation: Press Release () July 22
-
FRAXA Research Foundation: First fenobam trial results are positive. Press Release (2008) July 22.
-
(2008)
First fenobam trial results are positive
-
-
-
50
-
-
0019957859
-
Treatment of anxiety using fenobam (a nonbenzodiazepine) in a double-blind standard (diazepam) placebo-controlled study
-
Pecknold JC, McClure DJ, Appeltauer L, Wrzesinski L, Allan T: Treatment of anxiety using fenobam (a nonbenzodiazepine) in a double-blind standard (diazepam) placebo-controlled study.J Clin Psychopharmacol (1982) 2(2):129-132.
-
(1982)
J Clin Psychopharmacol
, vol.2
, Issue.2
, pp. 129-132
-
-
Pecknold, J.C.1
McClure, D.J.2
Appeltauer, L.3
Wrzesinski, L.4
Allan, T.5
-
51
-
-
27144537834
-
Fenobam: A clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity
-
Porter RH, Jaeschke G, Spooren W, Ballard TM, Büttelmann B, Kolczewski S, Peters JU, Prinssen E, Wichmann J, Vieira E, Mühlemann A et al: Fenobam: A clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J Pharmacol Exp Ther (2005) 315(2):711-721.
-
(2005)
J Pharmacol Exp Ther
, vol.315
, Issue.2
, pp. 711-721
-
-
Porter, R.H.1
Jaeschke, G.2
Spooren, W.3
Ballard, T.M.4
Büttelmann, B.5
Kolczewski, S.6
Peters, J.U.7
Prinssen, E.8
Wichmann, J.9
Vieira, E.10
Mühlemann, A.11
-
52
-
-
65949096495
-
A pilot open label, single dose trial of fenobam in adults with fragile X syndrome
-
Details the first clinical study of the safety and pharmacokinetics of an mGluR5 antagonist in humans with fragile X syndrome, ··
-
Berry-Kravis E, Hessl D, Coffey S, Hervey C, Schneider A, Yuhas J, Hutchison J, Snape M, Tranfaglia M, Nguyen DV, Hagerman R: A pilot open label, single dose trial of fenobam in adults with fragile X syndrome. J Med Genet (2009) 46(4):266-271. ·· Details the first clinical study of the safety and pharmacokinetics of an mGluR5 antagonist in humans with fragile X syndrome.
-
(2009)
J Med Genet
, vol.46
, Issue.4
, pp. 266-271
-
-
Berry-Kravis, E.1
Hessl, D.2
Coffey, S.3
Hervey, C.4
Schneider, A.5
Yuhas, J.6
Hutchison, J.7
Snape, M.8
Tranfaglia, M.9
Nguyen, D.V.10
Hagerman, R.11
-
53
-
-
67649918017
-
Edison investment research review
-
Neuropharm Group plc:, March 18
-
Neuropharm Group plc: Edison investment research review.Research Notes (2009): March 18.
-
(2009)
Research Notes
-
-
-
54
-
-
67649955305
-
-
Novartis AG (Glatthar R, Carcache D, Spanka C, Vranesic I-T, Troxler TJ, Novel bi-aryl amines. WO-2007113276 2007
-
Novartis AG (Glatthar R, Carcache D, Spanka C, Vranesic I-T, Troxler TJ): Novel bi-aryl amines. WO-2007113276 (2007).
-
-
-
-
55
-
-
67649928920
-
-
Novartis AG (Glatthar R, Orain D, Spanka C, Nicotinic acid derivatives as modulators of metabotropic glutamate receptors. WO-2007071358 2007
-
Novartis AG (Glatthar R, Orain D, Spanka C): Nicotinic acid derivatives as modulators of metabotropic glutamate receptors. WO-2007071358 (2007).
-
-
-
-
56
-
-
67649943653
-
-
Merz Pharma GMBH & Co (Danysz W, Dekundy A, Hechenberger M, Henrich M, Jatzke C, Nagel J, Parsons CGR, Weil T, Fotins J, Gutcaits A, Kalvinsh I et al, Pyrazolopyrimidines, a process for their preparation and the use as a medicine. WO-2008015271 2008
-
Merz Pharma GMBH & Co (Danysz W, Dekundy A, Hechenberger M, Henrich M, Jatzke C, Nagel J, Parsons CGR, Weil T, Fotins J, Gutcaits A, Kalvinsh I et al): Pyrazolopyrimidines, a process for their preparation and the use as a medicine. WO-2008015271 (2008).
-
-
-
|