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Items: 1 to 20 of 142

1.

Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254).

Turlington M, Noetzel MJ, Chun A, Zhou Y, Gogliotti RD, Nguyen ED, Gregory KJ, Vinson PN, Rook JM, Gogi KK, Xiang Z, Bridges TM, Daniels JS, Jones C, Niswender CM, Meiler J, Conn PJ, Lindsley CW, Stauffer SR.

J Med Chem. 2013 Oct 24;56(20):7976-96. doi: 10.1021/jm401028t. Epub 2013 Oct 9.

2.

Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity.

Rook JM, Noetzel MJ, Pouliot WA, Bridges TM, Vinson PN, Cho HP, Zhou Y, Gogliotti RD, Manka JT, Gregory KJ, Stauffer SR, Dudek FE, Xiang Z, Niswender CM, Daniels JS, Jones CK, Lindsley CW, Conn PJ.

Biol Psychiatry. 2013 Mar 15;73(6):501-9. doi: 10.1016/j.biopsych.2012.09.012. Epub 2012 Nov 7.

3.

Biotransformation of a novel positive allosteric modulator of metabotropic glutamate receptor subtype 5 contributes to seizure-like adverse events in rats involving a receptor agonism-dependent mechanism.

Bridges TM, Rook JM, Noetzel MJ, Morrison RD, Zhou Y, Gogliotti RD, Vinson PN, Xiang Z, Jones CK, Niswender CM, Lindsley CW, Stauffer SR, Conn PJ, Daniels JS.

Drug Metab Dispos. 2013 Sep;41(9):1703-14. doi: 10.1124/dmd.113.052084. Epub 2013 Jul 2.

4.

VU0477573: Partial Negative Allosteric Modulator of the Subtype 5 Metabotropic Glutamate Receptor with In Vivo Efficacy.

Nickols HH, Yuh JP, Gregory KJ, Morrison RD, Bates BS, Stauffer SR, Emmitte KA, Bubser M, Peng W, Nedelcovych MT, Thompson A, Lv X, Xiang Z, Daniels JS, Niswender CM, Lindsley CW, Jones CK, Conn PJ.

J Pharmacol Exp Ther. 2016 Jan;356(1):123-36. doi: 10.1124/jpet.115.226597. Epub 2015 Oct 26.

5.

Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅).

Turlington M, Malosh C, Jacobs J, Manka JT, Noetzel MJ, Vinson PN, Jadhav S, Herman EJ, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Martín-Martín ML, Tong HM, López S, MacDonald GJ, Steckler T, Daniels JS, Weaver CD, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR.

J Med Chem. 2014 Jul 10;57(13):5620-37. doi: 10.1021/jm500259z. Epub 2014 Jun 25.

6.

SAR studies on mGlu5 receptor positive allosteric modulators (2003- 2013).

Hao J, Xiong H.

Curr Top Med Chem. 2014;14(15):1789-841. Review.

PMID:
25176124
7.

A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling.

Noetzel MJ, Gregory KJ, Vinson PN, Manka JT, Stauffer SR, Lindsley CW, Niswender CM, Xiang Z, Conn PJ.

Mol Pharmacol. 2013 Apr;83(4):835-47. doi: 10.1124/mol.112.082891. Epub 2013 Jan 24. Erratum in: Mol Pharmacol. 2013 Oct;84(4):654.

8.

Mechanism based neurotoxicity of mGlu5 positive allosteric modulators--development challenges for a promising novel antipsychotic target.

Parmentier-Batteur S, Hutson PH, Menzel K, Uslaner JM, Mattson BA, O'Brien JA, Magliaro BC, Forest T, Stump CA, Tynebor RM, Anthony NJ, Tucker TJ, Zhang XF, Gomez R, Huszar SL, Lambeng N, Fauré H, Le Poul E, Poli S, Rosahl TW, Rocher JP, Hargreaves R, Williams TM.

Neuropharmacology. 2014 Jul;82:161-73. doi: 10.1016/j.neuropharm.2012.12.003. Epub 2013 Jan 2.

PMID:
23291536
9.

Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships.

Gregory KJ, Noetzel MJ, Rook JM, Vinson PN, Stauffer SR, Rodriguez AL, Emmitte KA, Zhou Y, Chun AC, Felts AS, Chauder BA, Lindsley CW, Niswender CM, Conn PJ.

Mol Pharmacol. 2012 Nov;82(5):860-75. doi: 10.1124/mol.112.080531. Epub 2012 Aug 3.

10.

N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement.

Gregory KJ, Herman EJ, Ramsey AJ, Hammond AS, Byun NE, Stauffer SR, Manka JT, Jadhav S, Bridges TM, Weaver CD, Niswender CM, Steckler T, Drinkenburg WH, Ahnaou A, Lavreysen H, Macdonald GJ, Bartolomé JM, Mackie C, Hrupka BJ, Caron MG, Daigle TL, Lindsley CW, Conn PJ, Jones CK.

J Pharmacol Exp Ther. 2013 Nov;347(2):438-57. doi: 10.1124/jpet.113.206623. Epub 2013 Aug 21.

11.

Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition.

Ellard JM, Madin A, Philps O, Hopkin M, Henderson S, Birch L, O'Connor D, Arai T, Takase K, Morgan L, Reynolds D, Talma S, Howley E, Powney B, Payne AH, Hall A, Gartlon JE, Dawson LA, Castro L, Atkinson PJ.

Bioorg Med Chem Lett. 2015 Dec 15;25(24):5792-6. doi: 10.1016/j.bmcl.2015.10.050. Epub 2015 Oct 17.

PMID:
26531152
12.

Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency.

Turlington M, Noetzel MJ, Bridges TM, Vinson PN, Steckler T, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Tong HM, Macdonald GJ, Daniels JS, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3641-6. doi: 10.1016/j.bmcl.2014.04.087. Epub 2014 May 2.

13.

Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).

Martín-Martín ML, Bartolomé-Nebreda JM, Conde-Ceide S, Alonso de Diego SA, López S, Martínez-Viturro CM, Tong HM, Lavreysen H, Macdonald GJ, Steckler T, Mackie C, Bridges TM, Daniels JS, Niswender CM, Noetzel MJ, Jones CK, Conn PJ, Lindsley CW, Stauffer SR.

Bioorg Med Chem Lett. 2015 Mar 15;25(6):1310-7. doi: 10.1016/j.bmcl.2015.01.038. Epub 2015 Jan 28.

14.

Biased mGlu5-Positive Allosteric Modulators Provide In Vivo Efficacy without Potentiating mGlu5 Modulation of NMDAR Currents.

Rook JM, Xiang Z, Lv X, Ghoshal A, Dickerson JW, Bridges TM, Johnson KA, Foster DJ, Gregory KJ, Vinson PN, Thompson AD, Byun N, Collier RL, Bubser M, Nedelcovych MT, Gould RW, Stauffer SR, Daniels JS, Niswender CM, Lavreysen H, Mackie C, Conde-Ceide S, Alcazar J, Bartolomé-Nebreda JM, Macdonald GJ, Talpos JC, Steckler T, Jones CK, Lindsley CW, Conn PJ.

Neuron. 2015 May 20;86(4):1029-40. doi: 10.1016/j.neuron.2015.03.063. Epub 2015 Apr 30.

15.

Probing the metabotropic glutamate receptor 5 (mGlu₅) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a "molecular switch" in PAM pharmacology.

Gregory KJ, Nguyen ED, Reiff SD, Squire EF, Stauffer SR, Lindsley CW, Meiler J, Conn PJ.

Mol Pharmacol. 2013 May;83(5):991-1006. doi: 10.1124/mol.112.083949. Epub 2013 Feb 26.

16.

Identification of glutathione conjugates of acetylene-containing positive allosteric modulators of metabotropic glutamate receptor subtype 5.

Zhuo X, Huang XS, Degnan AP, Snyder LB, Yang F, Huang H, Shu YZ, Johnson BM.

Drug Metab Dispos. 2015 Apr;43(4):578-89. doi: 10.1124/dmd.114.061879. Epub 2015 Jan 29.

17.

Fused thiazolyl alkynes as potent mGlu5 receptor positive allosteric modulators.

Packiarajan M, Grenon M, Zorn S, Hopper AT, White AD, Chandrasena G, Pu X, Brodbeck RM, Robichaud AJ.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4037-43. doi: 10.1016/j.bmcl.2013.05.070. Epub 2013 May 30.

PMID:
23770058
18.

Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles.

Rook JM, Tantawy MN, Ansari MS, Felts AS, Stauffer SR, Emmitte KA, Kessler RM, Niswender CM, Daniels JS, Jones CK, Lindsley CW, Conn PJ.

Neuropsychopharmacology. 2015 Feb;40(3):755-65. doi: 10.1038/npp.2014.245. Epub 2014 Sep 22.

19.

Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators.

Chae E, Shin YJ, Ryu EJ, Ji MK, Ryune Cho N, Lee KH, Jeong HJ, Kim SJ, Choi Y, Seok Oh K, Park CE, Soo Yoon Y.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2134-9. doi: 10.1016/j.bmcl.2013.01.116. Epub 2013 Feb 4.

PMID:
23434029
20.

Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery.

Sengmany K, Singh J, Stewart GD, Conn PJ, Christopoulos A, Gregory KJ.

Neuropharmacology. 2016 Jul 5. pii: S0028-3908(16)30287-8. doi: 10.1016/j.neuropharm.2016.07.001. [Epub ahead of print]

PMID:
27392634

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