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Items: 1 to 50 of 557

1.

Discovery of VU6015929: A Selective Discoidin Domain Receptor 1/2 (DDR1/2) Inhibitor to Explore the Role of DDR1 in Antifibrotic Therapy.

Jeffries DE, Borza CM, Blobaum AL, Pozzi A, Lindsley CW.

ACS Med Chem Lett. 2019 Nov 25;11(1):29-33. doi: 10.1021/acsmedchemlett.9b00382. eCollection 2020 Jan 9.

PMID:
31938459
2.

NeuroChat with Professor Kyle Emmitte.

Lindsley CW.

ACS Chem Neurosci. 2020 Jan 15;11(2):99-100. doi: 10.1021/acschemneuro.9b00582. No abstract available.

PMID:
31937105
3.

NeuroChat with Professor P. Jeffrey Conn.

Lindsley CW.

ACS Chem Neurosci. 2020 Jan 2;11(1):1-2. doi: 10.1021/acschemneuro.9b00567. No abstract available.

PMID:
31894694
4.

NeuroChat with Professor Danny Winder.

Lindsley CW.

ACS Chem Neurosci. 2019 Dec 18;10(12):4766-4767. doi: 10.1021/acschemneuro.9b00557. No abstract available.

PMID:
31847522
5.

Biased M1 receptor-positive allosteric modulators reveal role of phospholipase D in M1-dependent rodent cortical plasticity.

Moran SP, Xiang Z, Doyle CA, Maksymetz J, Lv X, Faltin S, Fisher NM, Niswender CM, Rook JM, Lindsley CW, Conn PJ.

Sci Signal. 2019 Dec 3;12(610). pii: eaax2057. doi: 10.1126/scisignal.aax2057.

PMID:
31796631
6.

Discovery of structurally distinct tricyclic M4 positive allosteric modulator (PAM) chemotypes.

Temple KJ, Long MF, Engers JL, Watson KJ, Chang S, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW.

Bioorg Med Chem Lett. 2020 Feb 15;30(4):126811. doi: 10.1016/j.bmcl.2019.126811. Epub 2019 Nov 11.

PMID:
31787491
7.

Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M4 positive allosteric modulator (PAM) chemotype.

Temple KJ, Engers JL, Long MF, Watson KJ, Chang S, Luscombe VB, Jenkins MT, Rodriguez AL, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW.

Bioorg Med Chem Lett. 2020 Feb 1;30(3):126812. doi: 10.1016/j.bmcl.2019.126812. Epub 2019 Nov 13.

PMID:
31784320
8.

Crystal structure of the M5 muscarinic acetylcholine receptor.

Vuckovic Z, Gentry PR, Berizzi AE, Hirata K, Varghese S, Thompson G, van der Westhuizen ET, Burger WAC, Rahmani R, Valant C, Langmead CJ, Lindsley CW, Baell JB, Tobin AB, Sexton PM, Christopoulos A, Thal DM.

Proc Natl Acad Sci U S A. 2019 Dec 17;116(51):26001-26007. doi: 10.1073/pnas.1914446116. Epub 2019 Nov 26.

9.

mGlu2 and mGlu3 Negative Allosteric Modulators Divergently Enhance Thalamocortical Transmission and Exert Rapid Antidepressant-like Effects.

Joffe ME, Santiago CI, Oliver KH, Maksymetz J, Harris NA, Engers JL, Lindsley CW, Winder DG, Conn PJ.

Neuron. 2020 Jan 8;105(1):46-59.e3. doi: 10.1016/j.neuron.2019.09.044. Epub 2019 Nov 14.

PMID:
31735403
10.

RedH and PigC Catalyze the Biosynthesis of Hybrubins via Phosphorylation of 4'-Methoxy-2,2'-Bipyrrole-5'-Carbaldehyde.

Long Q, Jeffries DE, Lin S, Chen X, He W, Wang Y, Deng Z, Lindsley CW, Tao M.

Appl Environ Microbiol. 2020 Jan 7;86(2). pii: e02331-19. doi: 10.1128/AEM.02331-19. Print 2020 Jan 7.

PMID:
31704680
11.

Discovery of a novel 3,4-dimethylcinnoline carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping.

Temple KJ, Engers JL, Long MF, Gregro AR, Watson KJ, Chang S, Jenkins MT, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW.

Bioorg Med Chem Lett. 2019 Nov 1;29(21):126678. doi: 10.1016/j.bmcl.2019.126678. Epub 2019 Sep 10.

PMID:
31537424
12.

Evaluation of Synthetic Cytochrome P450-Mimetic Metalloporphyrins To Facilitate "Biomimetic" Biotransformation of a Series of mGlu5 Allosteric Ligands.

Presley CC, Perry CK, Childress ES, Mulder MJ, Luscombe VB, Rodriguez AL, Niswender CM, Conn PJ, Lindsley CW.

ACS Omega. 2019 Jul 26;4(7):12782-12789. doi: 10.1021/acsomega.9b02017. eCollection 2019 Jul 31.

13.

Formal Total Synthesis of Pericoannosin A.

Fulton MG, Bertron JL, Reed CW, Lindsley CW.

J Org Chem. 2019 Sep 20;84(18):12187-12191. doi: 10.1021/acs.joc.9b01846. Epub 2019 Sep 4.

PMID:
31436090
14.

Further exploration of an N-aryl phenoxyethoxy pyridinone-based series of mGlu3 NAMs: Challenging SAR, enantiospecific activity and in vivo efficacy.

Yamada Y, Yohn SE, Gilliland K, Loch MT, Schulte ML, Rodriguez AL, Blobaum AL, Niswender CM, Jeffrey Conn P, Lindsley CW.

Bioorg Med Chem Lett. 2019 Sep 15;29(18):2670-2674. doi: 10.1016/j.bmcl.2019.07.030. Epub 2019 Jul 19.

PMID:
31358468
15.

DARK Classics in Chemical Neuroscience: Gamma-Hydroxybutyrate (GHB).

Trombley TA, Capstick RA, Lindsley CW.

ACS Chem Neurosci. 2019 Jul 23. doi: 10.1021/acschemneuro.9b00336. [Epub ahead of print]

PMID:
31287661
16.

The effect of the EP3 antagonist DG-041 on male mice with diet-induced obesity.

Ceddia RP, Downey JD, Morrison RD, Kraemer MP, Davis SE, Wu J, Lindsley CW, Yin H, Daniels JS, Breyer RM.

Prostaglandins Other Lipid Mediat. 2019 Oct;144:106353. doi: 10.1016/j.prostaglandins.2019.106353. Epub 2019 Jul 2.

PMID:
31276827
17.

Acute Negative Allosteric Modulation of M5 Muscarinic Acetylcholine Receptors Inhibits Oxycodone Self-Administration and Cue-Induced Reactivity with No Effect on Antinociception.

Gould RW, Gunter BW, Bubser M, Matthews RT, Teal LB, Ragland MG, Bridges TM, Garrison AT, Winder DG, Lindsley CW, Jones CK.

ACS Chem Neurosci. 2019 Aug 21;10(8):3740-3750. doi: 10.1021/acschemneuro.9b00274. Epub 2019 Jul 24.

PMID:
31268669
18.

mGlu5 Positive Allosteric Modulators Facilitate Long-Term Potentiation via Disinhibition Mediated by mGlu5-Endocannabinoid Signaling.

Xiang Z, Lv X, Maksymetz J, Stansley BJ, Ghoshal A, Gogliotti RG, Niswender CM, Lindsley CW, Conn PJ.

ACS Pharmacol Transl Sci. 2019 Jun 14;2(3):198-209. doi: 10.1021/acsptsci.9b00017. Epub 2019 May 15.

19.

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
20.

Structure-Activity Relationships, Pharmacokinetics, and Pharmacodynamics of the Kir6.2/SUR1-Specific Channel Opener VU0071063.

Kharade SV, Sanchez-Andres JV, Fulton MG, Shelton EL, Blobaum AL, Engers DW, Hofmann CS, Dadi PK, Lantier L, Jacobson DA, Lindsley CW, Denton JS.

J Pharmacol Exp Ther. 2019 Sep;370(3):350-359. doi: 10.1124/jpet.119.257204. Epub 2019 Jun 14.

PMID:
31201216
21.

Identification of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Acting at Site Distinct from 2-Methyl-6-(phenylethynyl)-pyridine Binding.

Butkiewicz M, Rodriguez AL, Rainey SE, Wieting J, Luscombe VB, Stauffer SR, Lindsley CW, Conn PJ, Meiler J.

ACS Chem Neurosci. 2019 Aug 21;10(8):3427-3436. doi: 10.1021/acschemneuro.8b00227. Epub 2019 Jun 17.

PMID:
31132237
22.

VU6005806/AZN-00016130, an advanced M4 positive allosteric modulator (PAM) profiled as a potential preclinical development candidate.

Engers DW, Melancon BJ, Gregro AR, Bertron JL, Bollinger SR, Felts AS, Konkol LC, Wood MR, Bollinger KA, Luscombe VB, Rodriguez AL, Jones CK, Bubser M, Yohn SE, Wood MW, Brandon NJ, Dugan ME, Niswender CM, Jeffrey Conn P, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2019 Jul 15;29(14):1714-1718. doi: 10.1016/j.bmcl.2019.05.026. Epub 2019 May 16.

PMID:
31113706
23.

Towards a TREK-1/2 (TWIK-Related K+ Channel 1 and 2) dual activator tool compound: Multi-dimensional optimization of BL-1249.

Iwaki Y, Yashiro K, Kokubo M, Mori T, Wieting JM, McGowan KM, Bridges TM, Engers DW, Denton JS, Kurata H, Lindsley CW.

Bioorg Med Chem Lett. 2019 Jul 1;29(13):1601-1604. doi: 10.1016/j.bmcl.2019.04.048. Epub 2019 Apr 29.

PMID:
31072652
24.

Total Synthesis of Hinduchelins A-D, Stereochemical Revision of Hinduchelin A, and Biological Evaluation of Natural and Unnatural Analogues.

Childress ES, Garrison AT, Sheldon JR, Skaar EP, Lindsley CW.

J Org Chem. 2019 May 17;84(10):6459-6464. doi: 10.1021/acs.joc.9b00391. Epub 2019 May 8.

PMID:
31039303
25.

M1 Muscarinic Receptors Modulate Fear-Related Inputs to the Prefrontal Cortex: Implications for Novel Treatments of Posttraumatic Stress Disorder.

Maksymetz J, Joffe ME, Moran SP, Stansley BJ, Li B, Temple K, Engers DW, Lawrence JJ, Lindsley CW, Conn PJ.

Biol Psychiatry. 2019 Jun 15;85(12):989-1000. doi: 10.1016/j.biopsych.2019.02.020. Epub 2019 Mar 7.

PMID:
31003787
26.

Asymmetric Synthesis of Natural and Unnatural Dibenzylbutane Lignans from a Common Intermediate.

Jeffries DE, Lindsley CW.

J Org Chem. 2019 May 3;84(9):5974-5979. doi: 10.1021/acs.joc.9b00633. Epub 2019 Apr 24.

PMID:
31002498
27.

NeuroChat with Professor Steven Townsend.

Lindsley CW.

ACS Chem Neurosci. 2019 Apr 17;10(4):2082-2083. doi: 10.1021/acschemneuro.9b00169. No abstract available.

PMID:
30991808
28.

Editors' Favorites: Best of 2018.

Lindsley CW, Abbott C, Andrews AM, Hooker JM, Zhou J.

ACS Chem Neurosci. 2019 Jan 16;10(1):1-4. doi: 10.1021/acschemneuro.8b00717. No abstract available.

PMID:
30990663
29.

Correction to Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models.

Abney KK, Bubser M, Du Y, Kozek KA, Bridges TM, Lindsley CW, Daniels JS, Morrison RD, Wickman K, Hopkins CR, Jones CK, Weaver CD.

ACS Chem Neurosci. 2019 May 15;10(5):2621. doi: 10.1021/acschemneuro.9b00165. Epub 2019 Mar 26. No abstract available.

PMID:
30912639
30.

Surveying heterocycles as amide bioisosteres within a series of mGlu7 NAMs: Discovery of VU6019278.

Reed CW, Washecheck JP, Quitlag MC, Jenkins MT, Rodriguez AL, Engers DW, Blobaum AL, Jeffrey Conn P, Niswender CM, Lindsley CW.

Bioorg Med Chem Lett. 2019 May 15;29(10):1211-1214. doi: 10.1016/j.bmcl.2019.03.016. Epub 2019 Mar 15.

PMID:
30910459
31.

Discovery of VU2957 (Valiglurax): An mGlu4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease.

Panarese JD, Engers DW, Wu YJ, Bronson JJ, Macor JE, Chun A, Rodriguez AL, Felts AS, Engers JL, Loch MT, Emmitte KA, Castelhano AL, Kates MJ, Nader MA, Jones CK, Blobaum AL, Conn PJ, Niswender CM, Hopkins CR, Lindsley CW.

ACS Med Chem Lett. 2018 Oct 16;10(3):255-260. doi: 10.1021/acsmedchemlett.8b00426. eCollection 2019 Mar 14.

PMID:
30891122
32.

Call for Papers: Strategies and Tactics in CNS Drug Synthesis.

Lindsley CW.

ACS Chem Neurosci. 2019 Mar 20;10(3):1116. doi: 10.1021/acschemneuro.9b00114. No abstract available.

PMID:
30889958
33.

Predictions and Statistics for the Best-Selling Drugs Globally and in the United States in 2018 and a Look Forward to 2024 Projections.

Lindsley CW.

ACS Chem Neurosci. 2019 Mar 20;10(3):1115. doi: 10.1021/acschemneuro.9b00112. No abstract available.

PMID:
30889957
34.

Preparation of 1,5-Dihydropyrazolo[3',4':5,6]pyrano[3,4- b]pyridines via a Microwave-Assisted, Palladium-Catalyzed Regioselective C-H Heteroarylation of Electron-Rich Pyrazoles.

Garrison AT, Childress ES, Davis DC, Lindsley CW.

J Org Chem. 2019 May 3;84(9):5855-5862. doi: 10.1021/acs.joc.9b00144. Epub 2019 Mar 7.

PMID:
30807155
35.

Use of chemical probes to explore the toxicological potential of the K+/Cl- cotransporter (KCC) as a novel insecticide target to control the primary vector of dengue and Zika virus, Aedes aegypti.

Prael FJ 3rd, Chen R, Li Z, Reed CW, Lindsley CW, Weaver CD, Swale DR.

Pestic Biochem Physiol. 2018 Oct;151:10-17. doi: 10.1016/j.pestbp.2018.03.019. Epub 2018 Apr 6.

36.

Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962).

Reed CW, Yohn SE, Washecheck JP, Roenfanz HF, Quitalig MC, Luscombe VB, Jenkins MT, Rodriguez AL, Engers DW, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW.

J Med Chem. 2019 Feb 14;62(3):1690-1695. doi: 10.1021/acs.jmedchem.8b01810. Epub 2019 Jan 17.

PMID:
30608678
37.

Corrigendum: Metabotropic Glutamate Receptor 7: A New Therapeutic Target in Neurodevelopmental Disorders.

Fisher NM, Seto M, Lindsley CW, Niswender CM.

Front Mol Neurosci. 2018 Dec 14;11:444. doi: 10.3389/fnmol.2018.00444. eCollection 2018.

38.

Novel M4 positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in β-amino carboxamide-harboring ligands.

Poslusney MS, Salovich JM, Wood MR, Melancon BJ, Bollinger KA, Luscombe VB, Rodriguez AL, Engers DW, Bridges TM, Niswender CM, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2019 Feb 1;29(3):362-366. doi: 10.1016/j.bmcl.2018.12.039. Epub 2018 Dec 18.

PMID:
30580918
39.

Protease-activated receptor 4 activity promotes platelet granule release and platelet-leukocyte interactions.

Rigg RA, Healy LD, Chu TT, Ngo ATP, Mitrugno A, Zilberman-Rudenko J, Aslan JE, Hinds MT, Vecchiarelli LD, Morgan TK, Gruber A, Temple KJ, Lindsley CW, Duvernay MT, Hamm HE, McCarty OJT.

Platelets. 2019;30(1):126-135. doi: 10.1080/09537104.2017.1406076. Epub 2018 Dec 18.

40.

Direct activation of G-protein-gated inward rectifying K+ channels promotes nonrapid eye movement sleep.

Zou B, Cao WS, Guan Z, Xiao K, Pascual C, Xie J, Zhang J, Xie J, Kayser F, Lindsley CW, Weaver CD, Fang J, Xie XS.

Sleep. 2019 Mar 1;42(3). pii: zsy244. doi: 10.1093/sleep/zsy244.

41.

Isoform selective PLD inhibition by novel, chiral 2,8-diazaspiro[4.5]decan-1-one derivatives.

Waterson AG, Scott SA, Kett NR, Blobaum AL, Alex Brown H, Lindsley CW.

Bioorg Med Chem Lett. 2018 Dec 15;28(23-24):3670-3673. doi: 10.1016/j.bmcl.2018.10.033. Epub 2018 Oct 22.

PMID:
30528979
42.

The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate.

Panarese JD, Engers DW, Wu YJ, Guernon JM, Chun A, Gregro AR, Bender AM, Capstick RA, Wieting JM, Bronson JJ, Macor JE, Westphal R, Soars M, Engers JE, Felts AS, Rodriguez AL, Emmitte KA, Jones CK, Blobaum AL, Conn PJ, Niswender CM, Hopkins CR, Lindsley CW.

Bioorg Med Chem Lett. 2019 Jan 15;29(2):342-346. doi: 10.1016/j.bmcl.2018.10.050. Epub 2018 Nov 1.

PMID:
30503632
43.

Sterol 14α-Demethylase Structure-Based Optimization of Drug Candidates for Human Infections with the Protozoan Trypanosomatidae.

Friggeri L, Hargrove TY, Rachakonda G, Blobaum AL, Fisher P, de Oliveira GM, da Silva CF, Soeiro MNC, Nes WD, Lindsley CW, Villalta F, Guengerich FP, Lepesheva GI.

J Med Chem. 2018 Dec 13;61(23):10910-10921. doi: 10.1021/acs.jmedchem.8b01671. Epub 2018 Nov 30.

44.

Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

Felts AS, Bollinger KA, Brassard CJ, Rodriguez AL, Morrison RD, Scott Daniels J, Blobaum AL, Niswender CM, Jones CK, Conn PJ, Emmitte KA, Lindsley CW.

Bioorg Med Chem Lett. 2019 Jan 1;29(1):47-50. doi: 10.1016/j.bmcl.2018.11.017. Epub 2018 Nov 10.

45.

Metabotropic Glutamate Receptor 7: A New Therapeutic Target in Neurodevelopmental Disorders.

Fisher NM, Seto M, Lindsley CW, Niswender CM.

Front Mol Neurosci. 2018 Oct 23;11:387. doi: 10.3389/fnmol.2018.00387. eCollection 2018. Review. Erratum in: Front Mol Neurosci. 2018 Dec 14;11:444.

46.

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
47.

Welcome to the DARK Side: DARK Classics in Chemical Neuroscience.

Lindsley CW.

ACS Chem Neurosci. 2018 Oct 17;9(10):2286. doi: 10.1021/acschemneuro.8b00528. No abstract available.

PMID:
30346702
48.

Mechanisms underlying prelimbic prefrontal cortex mGlu3/mGlu5-dependent plasticity and reversal learning deficits following acute stress.

Joffe ME, Santiago CI, Stansley BJ, Maksymetz J, Gogliotti RG, Engers JL, Nicoletti F, Lindsley CW, Conn PJ.

Neuropharmacology. 2019 Jan;144:19-28. doi: 10.1016/j.neuropharm.2018.10.013. Epub 2018 Oct 13.

49.

The Muscarinic Acetylcholine Receptor M5: Therapeutic Implications and Allosteric Modulation.

Bender AM, Garrison AT, Lindsley CW.

ACS Chem Neurosci. 2019 Mar 20;10(3):1025-1034. doi: 10.1021/acschemneuro.8b00481. Epub 2018 Oct 17.

PMID:
30280567
50.

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.

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