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Items: 1 to 20 of 79

1.

Pyridine containing M(1) positive allosteric modulators with reduced plasma protein binding.

Kuduk SD, Di Marco CN, Cofre V, Pitts DR, Ray WJ, Ma L, Wittmann M, Seager MA, Koeplinger K, Thompson CD, Hartman GD, Bilodeau MT.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):657-61. doi: 10.1016/j.bmcl.2009.11.059. Epub 2009 Dec 2. Erratum in: Bioorg Med Chem Lett. 2010 Mar 1;20(5):1796. Seager, Matthew [corrected to Seager, Matthew A].

PMID:
19962304
2.

Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.

Yang FV, Shipe WD, Bunda JL, Nolt MB, Wisnoski DD, Zhao Z, Barrow JC, Ray WJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Hartman GD, Lindsley CW.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):531-6. doi: 10.1016/j.bmcl.2009.11.100. Epub 2009 Nov 24.

PMID:
20004574
3.

Fused heterocyclic M1 positive allosteric modulators.

Kuduk SD, Di Marco CN, Cofre V, Ray WJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Thompson CD, Hartman GD, Bilodeau MT.

Bioorg Med Chem Lett. 2011 May 1;21(9):2769-72. doi: 10.1016/j.bmcl.2010.10.028. Epub 2010 Oct 16.

PMID:
21055928
4.

Heterocyclic fused pyridone carboxylic acid M(1) positive allosteric modulators.

Kuduk SD, Di Marco CN, Chang RK, Ray WJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Thompson CD, Hartman GD, Bilodeau MT.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2533-7. doi: 10.1016/j.bmcl.2010.02.096. Epub 2010 Mar 3.

PMID:
20303264
5.

Synthesis and evaluation of xanomeline analogs--probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor.

Kane BE, Grant MK, El-Fakahany EE, Ferguson DM.

Bioorg Med Chem. 2008 Feb 1;16(3):1376-92. Epub 2007 Oct 22.

PMID:
17977730
6.

Hydroxy cycloalkyl fused pyridone carboxylic acid M(1) positive allosteric modulators.

Kuduk SD, DiPardo RM, Beshore DC, Ray WJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Thompson CD, Hartman GD, Bilodeau MT.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2538-41. doi: 10.1016/j.bmcl.2010.02.095. Epub 2010 Mar 10.

PMID:
20346667
7.

Scaffold hopping from pyridones to imidazo[1,2-a]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor.

Tresadern G, Cid JM, Macdonald GJ, Vega JA, de Lucas AI, García A, Matesanz E, Linares ML, Oehlrich D, Lavreysen H, Biesmans I, Trabanco AA.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):175-9. doi: 10.1016/j.bmcl.2009.11.008. Epub 2009 Nov 10.

PMID:
19932615
8.

Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration.

Panarese JD, Cho HP, Adams JJ, Nance KD, Garcia-Barrantes PM, Chang S, Morrison RD, Blobaum AL, Niswender CM, Stauffer SR, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3822-5. doi: 10.1016/j.bmcl.2016.04.083. Epub 2016 Apr 29.

9.

Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor.

Mistry SN, Valant C, Sexton PM, Capuano B, Christopoulos A, Scammells PJ.

J Med Chem. 2013 Jun 27;56(12):5151-72. doi: 10.1021/jm400540b. Epub 2013 Jun 17.

PMID:
23718562
10.

Hybrid molecules from xanomeline and tacrine: enhanced tacrine actions on cholinesterases and muscarinic M1 receptors.

Fang L, Jumpertz S, Zhang Y, Appenroth D, Fleck C, Mohr K, Tränkle C, Decker M.

J Med Chem. 2010 Mar 11;53(5):2094-103. doi: 10.1021/jm901616h.

PMID:
20158205
11.

Discovery of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator.

Ward SE, Harries M, Aldegheri L, Andreotti D, Ballantine S, Bax BD, Harris AJ, Harker AJ, Lund J, Melarange R, Mingardi A, Mookherjee C, Mosley J, Neve M, Oliosi B, Profeta R, Smith KJ, Smith PW, Spada S, Thewlis KM, Yusaf SP.

J Med Chem. 2010 Aug 12;53(15):5801-12. doi: 10.1021/jm1005429.

PMID:
20614889
12.

N-heterocyclic derived M1 positive allosteric modulators.

Kuduk SD, Di Marco CN, Cofre V, Pitts DR, Ray WJ, Ma L, Wittmann M, Veng L, Seager MA, Koeplinger K, Thompson CD, Hartman GD, Bilodeau MT.

Bioorg Med Chem Lett. 2010 Feb 15;20(4):1334-7. doi: 10.1016/j.bmcl.2010.01.013. Epub 2010 Jan 11.

PMID:
20097564
13.

Identification of a methoxynaphthalene scaffold as a core replacement in quinolizidinone amide M(1) positive allosteric modulators.

Kuduk SD, Di Marco CN, Saffold JR, Ray WJ, Ma L, Wittmann M, Koeplinger KA, Thompson CD, Hartman GD, Bilodeau MT, Beshore DC.

Bioorg Med Chem Lett. 2014 Mar 1;24(5):1417-20. doi: 10.1016/j.bmcl.2014.01.012. Epub 2014 Jan 13.

PMID:
24485781
14.

Discovery of a selective allosteric M1 receptor modulator with suitable development properties based on a quinolizidinone carboxylic acid scaffold.

Kuduk SD, Chang RK, Di Marco CN, Pitts DR, Greshock TJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Thompson CD, Hartman GD, Bilodeau MT, Ray WJ.

J Med Chem. 2011 Jul 14;54(13):4773-80. doi: 10.1021/jm200400m. Epub 2011 Jun 17.

PMID:
21682298
15.

Long-term changes in the muscarinic M1 receptor induced by instantaneous formation of wash-resistant xanomeline-receptor complex.

De Lorme KC, Grant MK, Noetzel MJ, Polson SB, El-Fakahany EE.

J Pharmacol Exp Ther. 2007 Dec;323(3):868-76. Epub 2007 Sep 12.

16.

Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 2: 4-thiopyridyl acetophenones as non-tetrazole containing mGlu2 receptor potentiators.

Pinkerton AB, Cube RV, Hutchinson JH, James JK, Gardner MF, Schaffhauser H, Rowe BA, Daggett LP, Vernier JM.

Bioorg Med Chem Lett. 2004 Dec 6;14(23):5867-72.

PMID:
15501058
17.

New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2): identification and synthesis of N-propyl-8-chloro-6-substituted isoquinolones.

Trabanco AA, Duvey G, Cid JM, Macdonald GJ, Cluzeau P, Nhem V, Furnari R, Behaj N, Poulain G, Finn T, Lavreysen H, Poli S, Raux A, Thollon Y, Poirier N, D'Addona D, Andrés JI, Lutjens R, Le Poul E, Imogai H, Rocher JP.

Bioorg Med Chem Lett. 2011 Feb 1;21(3):971-6. doi: 10.1016/j.bmcl.2010.12.048. Epub 2010 Dec 21.

PMID:
21232953
18.

Pharmacological assessment of m1 muscarinic acetylcholine receptor-gq/11 protein coupling in membranes prepared from postmortem human brain tissue.

Salah-Uddin H, Thomas DR, Davies CH, Hagan JJ, Wood MD, Watson JM, Challiss RA.

J Pharmacol Exp Ther. 2008 Jun;325(3):869-74. doi: 10.1124/jpet.108.137968. Epub 2008 Mar 5.

20.

8-Fluoroimidazo[1,2-a]pyridine: synthesis, physicochemical properties and evaluation as a bioisosteric replacement for imidazo[1,2-a]pyrimidine in an allosteric modulator ligand of the GABA A receptor.

Humphries AC, Gancia E, Gilligan MT, Goodacre S, Hallett D, Merchant KJ, Thomas SR.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1518-22. Epub 2006 Jan 4.

PMID:
16386901

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