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Items: 1 to 50 of 66

1.

SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M4 PAMs.

Chopko TC, Han C, Gregro AR, Engers DW, Felts AS, Poslusney MS, Bollinger KA, Morrison RD, Bubser M, Lamsal A, Luscombe VB, Cho HP, Schnetz-Boutaud NC, Rodriguez AL, Chang S, Daniels JS, Stec DF, Niswender CM, Jones CK, Wood MR, Wood MW, Duggan ME, Brandon NJ, Conn PJ, Bridges TM, Lindsley CW, Melancon BJ.

Bioorg Med Chem Lett. 2019 Aug 15;29(16):2224-2228. doi: 10.1016/j.bmcl.2019.06.032. Epub 2019 Jun 20.

PMID:
31248774
2.

Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5- a]pyrimidine-5-carboxamide and Thieno[3,2- b]pyridine-5-carboxamide Cores.

Childress ES, Wieting JM, Felts AS, Breiner MM, Long MF, Luscombe VB, Rodriguez AL, Cho HP, Blobaum AL, Niswender CM, Emmitte KA, Conn PJ, Lindsley CW.

J Med Chem. 2019 Jan 10;62(1):378-384. doi: 10.1021/acs.jmedchem.8b01266. Epub 2018 Oct 31.

PMID:
30350962
3.

VU6007477, a Novel M1 PAM Based on a Pyrrolo[2,3-b]pyridine Carboxamide Core Devoid of Cholinergic Adverse Events.

Engers JL, Childress ES, Long MF, Capstick RA, Luscombe VB, Cho HP, Dickerson JW, Rook JM, Blobaum AL, Niswender CM, Engers DW, Conn PJ, Lindsley CW.

ACS Med Chem Lett. 2018 Sep 4;9(9):917-922. doi: 10.1021/acsmedchemlett.8b00261. eCollection 2018 Sep 13.

4.

Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators.

Yohn SE, Foster DJ, Covey DP, Moehle MS, Galbraith J, Garcia-Barrantes PM, Cho HP, Bubser M, Blobaum AL, Joffe ME, Cheer JF, Jones CK, Lindsley CW, Conn PJ.

Mol Psychiatry. 2018 Aug 16. doi: 10.1038/s41380-018-0206-2. [Epub ahead of print]

PMID:
30116027
5.

Discovery of Tricyclic Triazolo- and Imidazopyridine Lactams as M1 Positive Allosteric Modulators.

Engers JL, Bender AM, Kalbfleisch JJ, Cho HP, Lingenfelter KS, Luscombe VB, Han C, Melancon BJ, Blobaum AL, Dickerson JW, Rook JM, Niswender CM, Emmitte KA, Conn PJ, Lindsley CW.

ACS Chem Neurosci. 2019 Mar 20;10(3):1035-1042. doi: 10.1021/acschemneuro.8b00311. Epub 2018 Aug 9.

PMID:
30086237
6.

Corrigendum to "Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides" [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179-5184].

Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2018 Sep 15;28(17):3014. doi: 10.1016/j.bmcl.2018.07.022. Epub 2018 Jul 31. No abstract available.

7.

The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core.

Bertron JL, Cho HP, Garcia-Barrantes PM, Panarese JD, Salovich JM, Nance KD, Engers DW, Rook JM, Blobaum AL, Niswender CM, Stauffer SR, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2018 Jul 1;28(12):2175-2179. doi: 10.1016/j.bmcl.2018.05.009. Epub 2018 May 5.

8.

A Novel M1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity.

Rook JM, Bertron JL, Cho HP, Garcia-Barrantes PM, Moran SP, Maksymetz JT, Nance KD, Dickerson JW, Remke DH, Chang S, Harp JM, Blobaum AL, Niswender CM, Jones CK, Stauffer SR, Conn PJ, Lindsley CW.

ACS Chem Neurosci. 2018 Sep 19;9(9):2274-2285. doi: 10.1021/acschemneuro.8b00131. Epub 2018 May 8.

9.

PF-06827443 Displays Robust Allosteric Agonist and Positive Allosteric Modulator Activity in High Receptor Reserve and Native Systems.

Moran SP, Cho HP, Maksymetz J, Remke DH, Hanson RM, Niswender CM, Lindsley CW, Rook JM, Conn PJ.

ACS Chem Neurosci. 2018 Sep 19;9(9):2218-2224. doi: 10.1021/acschemneuro.8b00106. Epub 2018 Apr 25.

10.

Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold.

Bender AM, Cho HP, Nance KD, Lingenfelter KS, Luscombe VB, Gentry PR, Voigtritter K, Berizzi AE, Sexton PM, Langmead CJ, Christopoulos A, Locuson CW, Bridges TM, Chang S, O'Neill JC, Zhan X, Niswender CM, Jones CK, Conn PJ, Lindsley CW.

ACS Chem Neurosci. 2018 Jul 18;9(7):1572-1581. doi: 10.1021/acschemneuro.8b00126. Epub 2018 Apr 26.

11.

The robustness of T2 value as a trabecular structural index at multiple spatial resolutions of 7 Tesla MRI.

Lee DK, Song YK, Park BW, Cho HP, Yeom JS, Cho G, Cho H.

Magn Reson Med. 2018 Nov;80(5):1949-1961. doi: 10.1002/mrm.27202. Epub 2018 Apr 15.

PMID:
29656389
12.

M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition.

Moran SP, Dickerson JW, Cho HP, Xiang Z, Maksymetz J, Remke DH, Lv X, Doyle CA, Rajan DH, Niswender CM, Engers DW, Lindsley CW, Rook JM, Conn PJ.

Neuropsychopharmacology. 2018 Jul;43(8):1763-1771. doi: 10.1038/s41386-018-0033-9. Epub 2018 Mar 14.

13.

Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators.

O'Brien DE, Shaw DM, Cho HP, Cross AJ, Wesolowski SS, Felts AS, Bergare J, Elmore CS, Lindsley CW, Niswender CM, Conn PJ.

Mol Pharmacol. 2018 May;93(5):526-540. doi: 10.1124/mol.117.110114. Epub 2018 Mar 15.

14.

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides.

Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2017 Dec 1;27(23):5179-5184. doi: 10.1016/j.bmcl.2017.10.053. Epub 2017 Oct 24. Erratum in: Bioorg Med Chem Lett. 2018 Sep 15;28(17):3014.

15.

Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping.

Long MF, Engers JL, Chang S, Zhan X, Weiner RL, Luscombe VB, Rodriguez AL, Cho HP, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW.

Bioorg Med Chem Lett. 2017 Nov 15;27(22):4999-5001. doi: 10.1016/j.bmcl.2017.10.016. Epub 2017 Oct 9.

16.

Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core.

Bollinger KA, Felts AS, Brassard CJ, Engers JL, Rodriguez AL, Weiner RL, Cho HP, Chang S, Bubser M, Jones CK, Blobaum AL, Niswender CM, Conn PJ, Emmitte KA, Lindsley CW.

ACS Med Chem Lett. 2017 Aug 3;8(9):919-924. doi: 10.1021/acsmedchemlett.7b00279. eCollection 2017 Sep 14.

17.

Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core.

Bewley BR, Spearing PK, Weiner RL, Luscombe VB, Zhan X, Chang S, Cho HP, Rodriguez AL, Niswender CM, Conn PJ, Bridges TM, Engers DW, Lindsley CW.

Bioorg Med Chem Lett. 2017 Sep 15;27(18):4274-4279. doi: 10.1016/j.bmcl.2017.08.043. Epub 2017 Aug 20.

18.

Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists.

Bender AM, Weiner RL, Luscombe VB, Ajmera S, Cho HP, Chang S, Zhan X, Rodriguez AL, Niswender CM, Engers DW, Bridges TM, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2017 Aug 1;27(15):3576-3581. doi: 10.1016/j.bmcl.2017.05.042. Epub 2017 May 15.

19.

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides.

Tarr JC, Wood MR, Noetzel MJ, Bertron JL, Weiner RL, Rodriguez AL, Lamsal A, Byers FW, Chang S, Cho HP, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2017 Jul 1;27(13):2990-2995. doi: 10.1016/j.bmcl.2017.05.014. Epub 2017 May 6.

20.

Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology.

Melancon BJ, Wood MR, Noetzel MJ, Nance KD, Engelberg EM, Han C, Lamsal A, Chang S, Cho HP, Byers FW, Bubser M, Jones CK, Niswender CM, Wood MW, Engers DW, Wu D, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2017 Jun 1;27(11):2296-2301. doi: 10.1016/j.bmcl.2017.04.043. Epub 2017 Apr 13.

21.

Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype.

Bender AM, Weiner RL, Luscombe VB, Cho HP, Niswender CM, Engers DW, Bridges TM, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2017 Jun 1;27(11):2479-2483. doi: 10.1016/j.bmcl.2017.04.009. Epub 2017 Apr 4.

22.

Continued optimization of the M5 NAM ML375: Discovery of VU6008667, an M5 NAM with high CNS penetration and a desired short half-life in rat for addiction studies.

McGowan KM, Nance KD, Cho HP, Bridges TM, Conn PJ, Jones CK, Lindsley CW.

Bioorg Med Chem Lett. 2017 Mar 15;27(6):1356-1359. doi: 10.1016/j.bmcl.2017.02.020. Epub 2017 Feb 13.

23.

Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Core.

Nance KD, Days EL, Weaver CD, Coldren A, Farmer TD, Cho HP, Niswender CM, Blobaum AL, Niswender KD, Lindsley CW.

J Med Chem. 2017 Feb 23;60(4):1611-1616. doi: 10.1021/acs.jmedchem.6b01706. Epub 2017 Feb 3.

PMID:
28103022
24.

Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs.

Rook JM, Abe M, Cho HP, Nance KD, Luscombe VB, Adams JJ, Dickerson JW, Remke DH, Garcia-Barrantes PM, Engers DW, Engers JL, Chang S, Foster JJ, Blobaum AL, Niswender CM, Jones CK, Conn PJ, Lindsley CW.

ACS Chem Neurosci. 2017 Apr 19;8(4):866-883. doi: 10.1021/acschemneuro.6b00429. Epub 2017 Jan 10.

25.

Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs.

Wood MR, Noetzel MJ, Poslusney MS, Melancon BJ, Tarr JC, Lamsal A, Chang S, Luscombe VB, Weiner RL, Cho HP, Bubser M, Jones CK, Niswender CM, Wood MW, Engers DW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2017 Jan 15;27(2):171-175. doi: 10.1016/j.bmcl.2016.11.086. Epub 2016 Nov 30.

26.

Prefrontal Cortex-Mediated Impairments in a Genetic Model of NMDA Receptor Hypofunction Are Reversed by the Novel M1 PAM VU6004256.

Grannan MD, Mielnik CA, Moran SP, Gould RW, Ball J, Lu Z, Bubser M, Ramsey AJ, Abe M, Cho HP, Nance KD, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW, Jones CK.

ACS Chem Neurosci. 2016 Dec 21;7(12):1706-1716. doi: 10.1021/acschemneuro.6b00230. Epub 2016 Oct 5.

27.

Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypes.

Geanes AR, Cho HP, Nance KD, McGowan KM, Conn PJ, Jones CK, Meiler J, Lindsley CW.

Bioorg Med Chem Lett. 2016 Sep 15;26(18):4487-4491. doi: 10.1016/j.bmcl.2016.07.071. Epub 2016 Jul 30.

28.

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.

29.

Re-exploration of the mGlu₁ PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR.

Garcia-Barrantes PM, Cho HP, Starr TM, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2016 May 1;26(9):2289-92. doi: 10.1016/j.bmcl.2016.03.044. Epub 2016 Mar 14.

30.

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs.

Garcia-Barrantes PM, Cho HP, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):1869-72. doi: 10.1016/j.bmcl.2016.03.031. Epub 2016 Mar 10.

31.

Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool.

Garcia-Barrantes PM, Cho HP, Metts AM, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2016 Feb 1;26(3):751-756. doi: 10.1016/j.bmcl.2015.12.104. Epub 2016 Jan 2.

32.

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core.

Garcia-Barrantes PM, Cho HP, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5107-10. doi: 10.1016/j.bmcl.2015.10.013. Epub 2015 Oct 9.

33.

Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics.

Garcia-Barrantes PM, Cho HP, Niswender CM, Byers FW, Locuson CW, Blobaum AL, Xiang Z, Rook JM, Conn PJ, Lindsley CW.

J Med Chem. 2015 Oct 22;58(20):7959-71. doi: 10.1021/acs.jmedchem.5b00727. Epub 2015 Oct 8.

34.

Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges.

Kurata H, Gentry PR, Kokubo M, Cho HP, Bridges TM, Niswender CM, Byers FW, Wood MR, Daniels JS, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2015 Feb 1;25(3):690-4. doi: 10.1016/j.bmcl.2014.11.082. Epub 2014 Dec 13.

35.

Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380).

Gentry PR, Kokubo M, Bridges TM, Noetzel MJ, Cho HP, Lamsal A, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR.

J Med Chem. 2014 Sep 25;57(18):7804-10. doi: 10.1021/jm500995y. Epub 2014 Sep 3.

36.

Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics.

Cho HP, Garcia-Barrantes PM, Brogan JT, Hopkins CR, Niswender CM, Rodriguez AL, Venable DF, Morrison RD, Bubser M, Daniels JS, Jones CK, Conn PJ, Lindsley CW.

ACS Chem Biol. 2014 Oct 17;9(10):2334-46. doi: 10.1021/cb500560h. Epub 2014 Aug 28.

37.

A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors.

Cho HP, Engers DW, Venable DF, Niswender CM, Lindsley CW, Conn PJ, Emmitte KA, Rodriguez AL.

ACS Chem Neurosci. 2014 Jul 16;5(7):597-610. doi: 10.1021/cn5000343. Epub 2014 May 15.

38.

Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence.

Dhanya RP, Sheffler DJ, Dahl R, Davis M, Lee PS, Yang L, Nickols HH, Cho HP, Smith LH, D'Souza MS, Conn PJ, Der-Avakian A, Markou A, Cosford ND.

J Med Chem. 2014 May 22;57(10):4154-72. doi: 10.1021/jm5000563. Epub 2014 May 9.

39.

Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe.

Gentry PR, Kokubo M, Bridges TM, Cho HP, Smith E, Chase P, Hodder PS, Utley TJ, Rajapakse A, Byers F, Niswender CM, Morrison RD, Daniels JS, Wood MR, Conn PJ, Lindsley CW.

ChemMedChem. 2014 Aug;9(8):1677-82. doi: 10.1002/cmdc.201402051. Epub 2014 Apr 1.

40.

Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator.

Wu H, Wang C, Gregory KJ, Han GW, Cho HP, Xia Y, Niswender CM, Katritch V, Meiler J, Cherezov V, Conn PJ, Stevens RC.

Science. 2014 Apr 4;344(6179):58-64. doi: 10.1126/science.1249489. Epub 2014 Mar 6.

41.

Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375).

Gentry PR, Kokubo M, Bridges TM, Kett NR, Harp JM, Cho HP, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Wood MR, Lindsley CW.

J Med Chem. 2013 Nov 27;56(22):9351-5. doi: 10.1021/jm4013246. Epub 2013 Nov 13.

42.

Octahydropyrrolo[3,4-c]pyrrole negative allosteric modulators of mGlu1.

Manka JT, Rodriguez AL, Morrison RD, Venable DF, Cho HP, Blobaum AL, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2013 Sep 15;23(18):5091-6. doi: 10.1016/j.bmcl.2013.07.029. Epub 2013 Jul 23.

43.

N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats.

Lovell KM, Felts AS, Rodriguez AL, Venable DF, Cho HP, Morrison RD, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3713-8. doi: 10.1016/j.bmcl.2013.05.020. Epub 2013 May 17.

44.

Regulation of phospholipase D activity and phosphatidic acid production after purinergic (P2Y6) receptor stimulation.

Scott SA, Xiang Y, Mathews TP, Cho HP, Myers DS, Armstrong MD, Tallman KA, O'Reilly MC, Lindsley CW, Brown HA.

J Biol Chem. 2013 Jul 12;288(28):20477-87. doi: 10.1074/jbc.M113.451708. Epub 2013 May 30.

45.

Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.

Sheffler DJ, Sevel C, Le U, Lovell KM, Tarr JC, Carrington SJ, Cho HP, Digby GJ, Niswender CM, Conn PJ, Hopkins CR, Wood MR, Lindsley CW.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):223-7. doi: 10.1016/j.bmcl.2012.10.132. Epub 2012 Nov 9.

46.

Targeting selective activation of M(1) for the treatment of Alzheimer's disease: further chemical optimization and pharmacological characterization of the M(1) positive allosteric modulator ML169.

Tarr JC, Turlington ML, Reid PR, Utley TJ, Sheffler DJ, Cho HP, Klar R, Pancani T, Klein MT, Bridges TM, Morrison RD, Blobaum AL, Xiang Z, Daniels JS, Niswender CM, Conn PJ, Wood MR, Lindsley CW.

ACS Chem Neurosci. 2012 Nov 21;3(11):884-95. doi: 10.1021/cn300068s. Epub 2012 Jul 18.

47.

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.

48.

Synthesis and Biological Evaluation of Cremastrine and an Unnatural Analogue.

Hahn KN, Fadeyi OO, Cho HP, Lindsley CW.

Tetrahedron Lett. 2012 Jul 11;53(28):3577-3580. Epub 2012 May 10.

49.

Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models.

Digby GJ, Noetzel MJ, Bubser M, Utley TJ, Walker AG, Byun NE, Lebois EP, Xiang Z, Sheffler DJ, Cho HP, Davis AA, Nemirovsky NE, Mennenga SE, Camp BW, Bimonte-Nelson HA, Bode J, Italiano K, Morrison R, Daniels JS, Niswender CM, Olive MF, Lindsley CW, Jones CK, Conn PJ.

J Neurosci. 2012 Jun 20;32(25):8532-44. doi: 10.1523/JNEUROSCI.0337-12.2012.

50.

Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.

Melancon BJ, Gogliotti RD, Tarr JC, Saleh SA, Chauder BA, Lebois EP, Cho HP, Utley TJ, Sheffler DJ, Bridges TM, Morrison RD, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Wood MR.

Bioorg Med Chem Lett. 2012 May 15;22(10):3467-72. doi: 10.1016/j.bmcl.2012.03.088. Epub 2012 Mar 29.

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