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Items: 1 to 50 of 540

1.

Structure-activity relationships, pharmacokinetics, and pharmacodynamics of the Kir6.2/SUR1-specific channel opener, VU0071063.

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

J Pharmacol Exp Ther. 2019 Jun 14. pii: jpet.119.257204. doi: 10.1124/jpet.119.257204. [Epub ahead of print]

2.

Identification of novel allosteric modulators of mGlu5 acting at site distinct from MPEP binding.

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

ACS Chem Neurosci. 2019 May 27. doi: 10.1021/acschemneuro.8b00227. [Epub ahead of print]

PMID:
31132237
3.

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
4.

NeuroChat with Professor Cody Wenthur.

Lindsley CW.

ACS Chem Neurosci. 2019 May 15;10(5):2085-2086. doi: 10.1021/acschemneuro.9b00178. No abstract available.

PMID:
31088066
5.

NeuroChat with Professor Kathryn Commons.

Lindsley CW.

ACS Chem Neurosci. 2019 May 15;10(5):2084. doi: 10.1021/acschemneuro.9b00170. No abstract available.

PMID:
31088064
6.

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
7.

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
8.

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
9.

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
10.

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
11.

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
12.

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
13.

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
14.

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
15.

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
16.

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
17.

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
18.

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.

19.

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
20.

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.

21.

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
22.

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.

PMID:
30560697
23.

Direct Activation of G-protein-gated Inward Rectifying K+ Channels (GIRK) Promotes Non-Rapid 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. 2018 Dec 11. doi: 10.1093/sleep/zsy244. [Epub ahead of print]

PMID:
30535004
24.

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
25.

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
26.

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.

PMID:
30451500
27.

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.

PMID:
30446311
28.

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.

29.

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
30.

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
31.

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.

PMID:
30326237
32.

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
33.

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.

PMID:
30258541
34.

Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu4).

Bollinger SR, Engers DW, Panarese JD, West M, Engers JL, Loch MT, Rodriguez AL, Blobaum AL, Jones CK, Thompson Gray A, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.

J Med Chem. 2019 Jan 10;62(1):342-358. doi: 10.1021/acs.jmedchem.8b00994. Epub 2018 Oct 10.

PMID:
30247901
35.

DARK Classics in Chemical Neuroscience: Opium, a Historical Perspective.

Presley CC, Lindsley CW.

ACS Chem Neurosci. 2018 Oct 17;9(10):2503-2518. doi: 10.1021/acschemneuro.8b00459. Epub 2018 Oct 8.

PMID:
30247870
36.

What Papers Are People Citing and What Are People Reading?

Lindsley CW.

ACS Chem Neurosci. 2018 Sep 19;9(9):2097-2098. doi: 10.1021/acschemneuro.8b00438. No abstract available.

PMID:
30227714
37.

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
38.

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
39.

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.

PMID:
30076050
40.

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
41.

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
42.

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
43.

DARK Classics in Chemical Neuroscience: Phencyclidine (PCP).

Bertron JL, Seto M, Lindsley CW.

ACS Chem Neurosci. 2018 Oct 17;9(10):2459-2474. doi: 10.1021/acschemneuro.8b00266. Epub 2018 Jul 17.

PMID:
29953199
44.

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
45.

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
46.

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.

47.

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
48.

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.

49.

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.

PMID:
29701957
50.

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

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