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Items: 1 to 50 of 596

1.

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
2.

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. 2018 Aug 9. doi: 10.1021/acschemneuro.8b00311. [Epub ahead of print]

PMID:
30086237
3.

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, Jeffrey Conn P, 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.

PMID:
30076050
4.

New 2017 Data and Statistics for Pharmaceutical Products.

Lindsley CW.

ACS Chem Neurosci. 2018 Jul 18;9(7):1518-1519. doi: 10.1021/acschemneuro.8b00320. No abstract available.

PMID:
30016875
5.

2018: A New Impact Factor and an Expanded Cast of Associate Editors.

Lindsley CW.

ACS Chem Neurosci. 2018 Jul 18;9(7):1517. doi: 10.1021/acschemneuro.8b00318. No abstract available.

PMID:
30016874
6.

Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu4 positive allosteric modulators that mitigate CYP1A2 induction liability.

Engers DW, Bollinger SR, Engers JL, Panarese JD, Breiner MM, Gregro A, Blobaum AL, Bronson JJ, Wu YJ, Macor JE, Rodriguez AL, Zamorano R, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.

Bioorg Med Chem Lett. 2018 Aug 15;28(15):2641-2646. doi: 10.1016/j.bmcl.2018.06.034. Epub 2018 Jun 19.

PMID:
29958762
7.

DARK Classics in Chemical Neuroscience: Phencyclidine (PCP).

Bertron JL, Seto M, Lindsley CW.

ACS Chem Neurosci. 2018 Jul 17. doi: 10.1021/acschemneuro.8b00266. [Epub ahead of print]

PMID:
29953199
8.

Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992.

Kharade SV, Kurata H, Bender AM, Blobaum AL, Figueroa EE, Duran A, Kramer M, Days E, Vinson P, Flores D, Satlin LM, Meiler J, Weaver CD, Lindsley CW, Hopkins CR, Denton JS.

Mol Pharmacol. 2018 Aug;94(2):926-937. doi: 10.1124/mol.118.112359. Epub 2018 Jun 12.

PMID:
29895592
9.

Sterol 14α-Demethylase Structure-Based Design of VNI (( R)- N-(1-(2,4-Dichlorophenyl)-2-(1 H-imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives To Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallographic Analysis.

Friggeri L, Hargrove TY, Wawrzak Z, Blobaum AL, Rachakonda G, Lindsley CW, Villalta F, Nes WD, Botta M, Guengerich FP, Lepesheva GI.

J Med Chem. 2018 Jul 12;61(13):5679-5691. doi: 10.1021/acs.jmedchem.8b00641. Epub 2018 Jun 25.

PMID:
29894182
10.

Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor.

Khajehali E, Valant C, Jörg M, Tobin AB, Conn PJ, Lindsley CW, Sexton PM, Scammells PJ, Christopoulos A.

Biochem Pharmacol. 2018 Aug;154:243-254. doi: 10.1016/j.bcp.2018.05.009. Epub 2018 May 17.

11.

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.

PMID:
29754948
12.

Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

Felts AS, Rodriguez AL, Morrison RD, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2018 Jun 1;28(10):1679-1685. doi: 10.1016/j.bmcl.2018.04.053. Epub 2018 Apr 22.

PMID:
29705142
13.

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 May 8. doi: 10.1021/acschemneuro.8b00131. [Epub ahead of print]

PMID:
29701957
14.

Classics in Chemical Neuroscience: Risperidone.

Chopko TC, Lindsley CW.

ACS Chem Neurosci. 2018 Jul 18;9(7):1520-1529. doi: 10.1021/acschemneuro.8b00159. Epub 2018 May 11.

PMID:
29695153
15.

Structure-Activity Relationships of Pan-Gαq/11 Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators.

Berizzi AE, Bender AM, Lindsley CW, Conn PJ, Sexton PM, Langmead CJ, Christopoulos A.

ACS Chem Neurosci. 2018 Jul 18;9(7):1818-1828. doi: 10.1021/acschemneuro.8b00136. Epub 2018 Apr 30.

PMID:
29683647
16.

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 Apr 25. doi: 10.1021/acschemneuro.8b00106. [Epub ahead of print]

PMID:
29683646
17.

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.

PMID:
29678111
18.

Genetic and Rare Disease of the CNS. Part II: Holoprosencephaly (HPE).

Lindsley CW.

ACS Chem Neurosci. 2018 Apr 18;9(4):626-627. doi: 10.1021/acschemneuro.8b00135. No abstract available.

PMID:
29665691
19.

mGlu1 and mGlu5 modulate distinct excitatory inputs to the nucleus accumbens shell.

Turner BD, Rook JM, Lindsley CW, Conn PJ, Grueter BA.

Neuropsychopharmacology. 2018 Sep;43(10):2075-2082. doi: 10.1038/s41386-018-0049-1. Epub 2018 Mar 27.

PMID:
29654259
20.

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.

PMID:
29581537
21.

Call for Papers: Allosteric Modulators of Drug Targets-Special Issue for 2019.

Lindsley CW.

ACS Chem Neurosci. 2018 Mar 21;9(3):391. doi: 10.1021/acschemneuro.8b00077. No abstract available.

PMID:
29558807
22.

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.

PMID:
29545267
23.

Total RNA Sequencing of Rett Syndrome Autopsy Samples Identifies the M4 Muscarinic Receptor as a Novel Therapeutic Target.

Gogliotti RG, Fisher NM, Stansley BJ, Jones CK, Lindsley CW, Conn PJ, Niswender CM.

J Pharmacol Exp Ther. 2018 May;365(2):291-300. doi: 10.1124/jpet.117.246991. Epub 2018 Mar 9.

PMID:
29523700
24.

Muscarinic M5 receptors modulate ethanol seeking in rats.

Berizzi AE, Perry CJ, Shackleford DM, Lindsley CW, Jones CK, Chen NA, Sexton PM, Christopoulos A, Langmead CJ, Lawrence AJ.

Neuropsychopharmacology. 2018 Jun;43(7):1510-1517. doi: 10.1038/s41386-017-0007-3. Epub 2018 Feb 5.

25.

Pharmacokinetics, Tissue Localization, Toxicity, and Treatment Efficacy in the First Small Animal (Rabbit) Model of Intra-Arterial Chemotherapy for Retinoblastoma.

Daniels AB, Froehler MT, Pierce JM, Nunnally AH, Calcutt MW, Bridges TM, LaNeve DC, Williams PE, Boyd KL, Reyzer ML, Lindsley CW, Friedman DL, Richmond A.

Invest Ophthalmol Vis Sci. 2018 Jan 1;59(1):446-454. doi: 10.1167/iovs.17-22302.

26.

Editors' Favorites of 2017.

Lindsley CW, Cunningham KA, Hooker JM, Andrews AM.

ACS Chem Neurosci. 2018 Jan 17;9(1):1-4. doi: 10.1021/acschemneuro.8b00001. No abstract available.

PMID:
29338186
27.

Metabotropic glutamate receptor subtype 3 gates acute stress-induced dysregulation of amygdalo-cortical function.

Joffe ME, Santiago CI, Engers JL, Lindsley CW, Conn PJ.

Mol Psychiatry. 2017 Dec 21. doi: 10.1038/s41380-017-0015-z. [Epub ahead of print]

28.

Cholinergic Projections to the Substantia Nigra Pars Reticulata Inhibit Dopamine Modulation of Basal Ganglia through the M4 Muscarinic Receptor.

Moehle MS, Pancani T, Byun N, Yohn SE, Wilson GH 3rd, Dickerson JW, Remke DH, Xiang Z, Niswender CM, Wess J, Jones CK, Lindsley CW, Rook JM, Conn PJ.

Neuron. 2017 Dec 20;96(6):1358-1372.e4. doi: 10.1016/j.neuron.2017.12.008.

PMID:
29268098
29.

VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides.

Reed CW, McGowan KM, Spearing PK, Stansley BJ, Roenfanz HF, Engers DW, Rodriguez AL, Engelberg EM, Luscombe VB, Loch MT, Remke DH, Rook JM, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW.

ACS Med Chem Lett. 2017 Nov 8;8(12):1326-1330. doi: 10.1021/acsmedchemlett.7b00429. eCollection 2017 Dec 14.

PMID:
29259756
30.

A Possible Repeal of the Orphan Drug Tax Credit?

Lindsley CW.

ACS Chem Neurosci. 2017 Dec 20;8(12):2569. doi: 10.1021/acschemneuro.7b00453. No abstract available.

PMID:
29258314
31.

Genetic and Rare Disease of the CNS. Part I: Fatal Familial Insomnia (FFI).

Lindsley CW.

ACS Chem Neurosci. 2017 Dec 20;8(12):2570-2572. doi: 10.1021/acschemneuro.7b00463. No abstract available.

PMID:
29258312
32.

cFLIP critically modulates apoptotic resistance in epithelial-to-mesenchymal transition.

Padmanabhan C, Rellinger EJ, Zhu J, An H, Woodbury LG, Chung DH, Waterson AG, Lindsley CW, Means AL, Beauchamp RD.

Oncotarget. 2017 Jul 25;8(60):101072-101086. doi: 10.18632/oncotarget.19557. eCollection 2017 Nov 24.

33.

Effects of muscarinic M1 and M4 acetylcholine receptor stimulation on extinction and reinstatement of cocaine seeking in male mice, independent of extinction learning.

Stoll K, Hart R, Lindsley CW, Thomsen M.

Psychopharmacology (Berl). 2018 Mar;235(3):815-827. doi: 10.1007/s00213-017-4797-0. Epub 2017 Dec 18.

PMID:
29250738
34.

Isoxazole compound ML327 blocks MYC expression and tumor formation in neuroblastoma.

Rellinger EJ, Padmanabhan C, Qiao J, Craig BT, An H, Zhu J, Correa H, Waterson AG, Lindsley CW, Beauchamp RD, Chung DH.

Oncotarget. 2017 Jul 20;8(53):91040-91051. doi: 10.18632/oncotarget.19406. eCollection 2017 Oct 31.

35.

Embarking on a 5 Year Journey to Highlight Genetic and Rare Diseases of the Central Nervous System.

Lindsley CW.

ACS Chem Neurosci. 2017 Nov 15;8(11):2349. doi: 10.1021/acschemneuro.7b00401. No abstract available.

PMID:
29137461
36.

Feeling Rejected? ACS Chemical Neuroscience Can Help Get Your Science to the Neuroscience Community As Quickly As Possible.

Lindsley CW.

ACS Chem Neurosci. 2017 Nov 15;8(11):2348. doi: 10.1021/acschemneuro.7b00380. No abstract available.

PMID:
29137460
37.

Contextual Fear Extinction Induces Hippocampal Metaplasticity Mediated by Metabotropic Glutamate Receptor 5.

Stansley BJ, Fisher NM, Gogliotti RG, Lindsley CW, Conn PJ, Niswender CM.

Cereb Cortex. 2017 Nov 9:1-14. doi: 10.1093/cercor/bhx282. [Epub ahead of print]

PMID:
29136107
38.

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.

PMID:
29089231
39.

Functional partnership between mGlu3 and mGlu5 metabotropic glutamate receptors in the central nervous system.

Di Menna L, Joffe ME, Iacovelli L, Orlando R, Lindsley CW, Mairesse J, Gressèns P, Cannella M, Caraci F, Copani A, Bruno V, Battaglia G, Conn PJ, Nicoletti F.

Neuropharmacology. 2018 Jan;128:301-313. doi: 10.1016/j.neuropharm.2017.10.026. Epub 2017 Oct 25.

PMID:
29079293
40.

Discovery of VU6005649, a CNS Penetrant mGlu7/8 Receptor PAM Derived from a Series of Pyrazolo[1,5-a]pyrimidines.

Abe M, Seto M, Gogliotti RG, Loch MT, Bollinger KA, Chang S, Engelberg EM, Luscombe VB, Harp JM, Bubser M, Engers DW, Jones CK, Rodriguez AL, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW.

ACS Med Chem Lett. 2017 Sep 1;8(10):1110-1115. doi: 10.1021/acsmedchemlett.7b00317. eCollection 2017 Oct 12.

PMID:
29057060
41.

Selective inhibition of M5 muscarinic acetylcholine receptors attenuates cocaine self-administration in rats.

Gunter BW, Gould RW, Bubser M, McGowan KM, Lindsley CW, Jones CK.

Addict Biol. 2017 Oct 18. doi: 10.1111/adb.12567. [Epub ahead of print]

PMID:
29044937
42.

ACS Chemical Neuroscience: Most Cited Papers from 2016.

Lindsley CW.

ACS Chem Neurosci. 2017 Oct 18;8(10):2097-2098. doi: 10.1021/acschemneuro.7b00354. No abstract available.

PMID:
29041780
43.

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.

PMID:
29037946
44.

Preparation of Unsymmetrical 1,2,4,5-Tetrazines via a Mild Suzuki Cross-Coupling Reaction.

Bender AM, Chopko TC, Bridges TM, Lindsley CW.

Org Lett. 2017 Oct 20;19(20):5693-5696. doi: 10.1021/acs.orglett.7b02868. Epub 2017 Oct 4.

PMID:
28976768
45.

Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

Felts AS, Rodriguez AL, Morrison RD, Bollinger KA, Venable DF, Blobaum AL, Byers FW, Thompson Gray A, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2017 Nov 1;27(21):4858-4866. doi: 10.1016/j.bmcl.2017.09.042. Epub 2017 Sep 20.

PMID:
28958625
46.

Design and Synthesis of N-Aryl Phenoxyethoxy Pyridinones as Highly Selective and CNS Penetrant mGlu3 NAMs.

Engers JL, Bollinger KA, Weiner RL, Rodriguez AL, Long MF, Breiner MM, Chang S, Bollinger SR, Bubser M, Jones CK, Morrison RD, Bridges TM, Blobaum AL, Niswender CM, Conn PJ, Emmitte KA, Lindsley CW.

ACS Med Chem Lett. 2017 Aug 15;8(9):925-930. doi: 10.1021/acsmedchemlett.7b00249. eCollection 2017 Sep 14.

PMID:
28947938
47.

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.

PMID:
28947937
48.

Species-Specific Involvement of Aldehyde Oxidase and Xanthine Oxidase in the Metabolism of the Pyrimidine-Containing mGlu5-Negative Allosteric Modulator VU0424238 (Auglurant).

Crouch RD, Blobaum AL, Felts AS, Conn PJ, Lindsley CW.

Drug Metab Dispos. 2017 Dec;45(12):1245-1259. doi: 10.1124/dmd.117.077552. Epub 2017 Sep 22.

PMID:
28939686
49.

Emerging Data Strengthens the Argument That the Microbiome Is the Fifth Horseman of the Drug Discovery Apocalypse.

Lindsley CW.

ACS Chem Neurosci. 2017 Sep 20;8(9):1813. doi: 10.1021/acschemneuro.7b00295. No abstract available.

PMID:
28927279
50.

Call for Papers: DARK Classics in Chemical Neuroscience.

Lindsley CW.

ACS Chem Neurosci. 2017 Sep 20;8(9):1812. doi: 10.1021/acschemneuro.7b00306. No abstract available.

PMID:
28927278

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