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Items: 39

1.

Correction to Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective NaV1.7 Inhibitors for the Treatment of Pain.

Luo G, Chen L, Easton A, Newton A, Bourin C, Shields E, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Sivarao DV, Senapati A, Bristow LJ, Meanwell NA, Thompson LA, Dzierba C.

J Med Chem. 2019 Feb 28;62(4):2213. doi: 10.1021/acs.jmedchem.9b00202. Epub 2019 Feb 8. No abstract available.

PMID:
30734560
2.

Discovery of new indole-based acylsulfonamide Nav1.7 inhibitors.

Wu YJ, Venables B, Guernon J, Chen J, Sit SY, Rajamani R, Knox RJ, Matchett M, Pieschl RL, Herrington J, Bristow LJ, Meanwell NA, Thompson LA, Dzierba C.

Bioorg Med Chem Lett. 2019 Feb 15;29(4):659-663. doi: 10.1016/j.bmcl.2018.12.013. Epub 2018 Dec 6.

PMID:
30638874
3.

Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective NaV1.7 Inhibitors for the Treatment of Pain.

Luo G, Chen L, Easton A, Newton A, Bourin C, Shields E, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Sivarao DV, Senapati A, Bristow LJ, Meanwell NA, Thompson LA, Dzierba C.

J Med Chem. 2019 Jan 24;62(2):831-856. doi: 10.1021/acs.jmedchem.8b01550. Epub 2019 Jan 8. Erratum in: J Med Chem. 2019 Feb 28;62(4):2213.

PMID:
30576602
4.

Diminished responses to monoaminergic antidepressants but not ketamine in a mouse model for neuropsychiatric lupus.

Srikumar BN, Naidu PS, Kalidindi N, Paschapur M, Adepu B, Subramani S, Nagar J, Srivastava R, Sreedhara MV, Prasad DS, Das ML, Louis JV, Kuchibhotla VK, Dudhgaonkar S, Pieschl RL, Li YW, Bristow LJ, Ramarao M, Vikramadithyan RK.

J Psychopharmacol. 2019 Jan;33(1):25-36. doi: 10.1177/0269881118812102. Epub 2018 Nov 28.

PMID:
30484737
5.

Discovery of morpholine-based aryl sulfonamides as Nav1.7 inhibitors.

Wu YJ, Guernon J, McClure A, Venables B, Rajamani R, Robbins KJ, Knox RJ, Matchett M, Pieschl RL, Herrington J, Bristow LJ, Meanwell NA, Olson R, Thompson LA, Dzierba C.

Bioorg Med Chem Lett. 2018 Mar 1;28(5):958-962. doi: 10.1016/j.bmcl.2018.01.035. Epub 2018 Feb 1.

PMID:
29439904
6.

Mapping the central effects of (±)-ketamine and traxoprodil using pharmacological magnetic resonance imaging in awake rats.

Tang H, Kukral D, Li YW, Fronheiser M, Malone H, Pena A, Pieschl R, Sidik K, Tobon G, Chow PL, Bristow LJ, Hayes W, Luo F.

J Psychopharmacol. 2018 Feb;32(2):146-155. doi: 10.1177/0269881117746901. Epub 2018 Jan 30.

PMID:
29378483
7.

Preclinical Characterization of (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one (BMS-986169), a Novel, Intravenous, Glutamate N-Methyl-d-Aspartate 2B Receptor Negative Allosteric Modulator with Potential in Major Depressive Disorder.

Bristow LJ, Gulia J, Weed MR, Srikumar BN, Li YW, Graef JD, Naidu PS, Sanmathi C, Aher J, Bastia T, Paschapur M, Kalidindi N, Kumar KV, Molski T, Pieschl R, Fernandes A, Brown JM, Sivarao DV, Newberry K, Bookbinder M, Polino J, Keavy D, Newton A, Shields E, Simmermacher J, Kempson J, Li J, Zhang H, Mathur A, Kallem RR, Sinha M, Ramarao M, Vikramadithyan RK, Thangathirupathy S, Warrier J, Islam I, Bronson JJ, Olson RE, Macor JE, Albright CF, King D, Thompson LA, Marcin LR, Sinz M.

J Pharmacol Exp Ther. 2017 Dec;363(3):377-393. doi: 10.1124/jpet.117.242784. Epub 2017 Sep 27.

PMID:
28954811
8.

Characterization of the adrenocorticotrophic hormone - induced mouse model of resistance to antidepressant drug treatment.

Srikumar BN, Paschapur M, Kalidindi N, Adepu B, Das ML, Sreedhara MV, Kuchibhotla VK, Pieschl RL, Li YW, Ega DSP, Louis JV, Murugesan S, Naidu PS, Ramarao M, Bristow LJ, Vikramadithyan RK.

Pharmacol Biochem Behav. 2017 Oct;161:53-61. doi: 10.1016/j.pbb.2017.09.003. Epub 2017 Sep 11.

PMID:
28911960
9.

Discovery of non-zwitterionic aryl sulfonamides as Nav1.7 inhibitors with efficacy in preclinical behavioral models and translational measures of nociceptive neuron activation.

Wu YJ, Guernon J, McClure A, Luo G, Rajamani R, Ng A, Easton A, Newton A, Bourin C, Parker D, Mosure K, Barnaby O, Soars MG, Knox RJ, Matchett M, Pieschl R, Herrington J, Chen P, Sivarao DV, Bristow LJ, Meanwell NA, Bronson J, Olson R, Thompson LA, Dzierba C.

Bioorg Med Chem. 2017 Oct 15;25(20):5490-5505. doi: 10.1016/j.bmc.2017.08.012. Epub 2017 Aug 9.

PMID:
28818462
10.

A Functional NaV1.7-NaVAb Chimera with a Reconstituted High-Affinity ProTx-II Binding Site.

Rajamani R, Wu S, Rodrigo I, Gao M, Low S, Megson L, Wensel D, Pieschl RL, Post-Munson DJ, Watson J, Langley DR, Ahlijanian MK, Bristow LJ, Herrington J.

Mol Pharmacol. 2017 Sep;92(3):310-317. doi: 10.1124/mol.117.108712. Epub 2017 Jun 23.

PMID:
28645932
11.

Effects of BMS-902483, an α7 nicotinic acetylcholine receptor partial agonist, on cognition and sensory gating in relation to receptor occupancy in rodents.

Pieschl RL, Miller R, Jones KM, Post-Munson DJ, Chen P, Newberry K, Benitex Y, Molski T, Morgan D, McDonald IM, Macor JE, Olson RE, Asaka Y, Digavalli S, Easton A, Herrington J, Westphal RS, Lodge NJ, Zaczek R, Bristow LJ, Li YW.

Eur J Pharmacol. 2017 Jul 15;807:1-11. doi: 10.1016/j.ejphar.2017.04.024. Epub 2017 Apr 22.

PMID:
28438647
12.

[3H]BMT-046091 a potent and selective radioligand to determine AAK1 distribution and target engagement.

Louis JV, Lu Y, Pieschl R, Tian Y, Hong Y, Dandapani K, Naidu S, Vikramadithyan RK, Dzierba C, Sarvasiddhi SK, Nara SJ, Bronson J, Macor JE, Albright C, Kostich W, Li YW.

Neuropharmacology. 2017 May 15;118:167-174. doi: 10.1016/j.neuropharm.2017.03.015. Epub 2017 Mar 15.

PMID:
28315351
13.

Development of New Benzenesulfonamides As Potent and Selective Nav1.7 Inhibitors for the Treatment of Pain.

Wu YJ, Guernon J, Shi J, Ditta J, Robbins KJ, Rajamani R, Easton A, Newton A, Bourin C, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Bristow LJ, Meanwell NA, Olson R, Thompson LA, Dzierba C.

J Med Chem. 2017 Mar 23;60(6):2513-2525. doi: 10.1021/acs.jmedchem.6b01918. Epub 2017 Mar 10.

PMID:
28234467
14.

B-973, a novel piperazine positive allosteric modulator of the α7 nicotinic acetylcholine receptor.

Post-Munson DJ, Pieschl RL, Molski TF, Graef JD, Hendricson AW, Knox RJ, McDonald IM, Olson RE, Macor JE, Weed MR, Bristow LJ, Kiss L, Ahlijanian MK, Herrington J.

Eur J Pharmacol. 2017 Mar 15;799:16-25. doi: 10.1016/j.ejphar.2017.01.037. Epub 2017 Jan 26.

PMID:
28132910
15.

Discovery of Indazoles as Potent, Orally Active Dual Neurokinin 1 Receptor Antagonists and Serotonin Transporter Inhibitors for the Treatment of Depression.

Degnan AP, Tora GO, Huang H, Conlon DA, Davis CD, Hanumegowda UM, Hou X, Hsiao Y, Hu J, Krause R, Li YW, Newton AE, Pieschl RL, Raybon J, Rosner T, Sun JH, Taber MT, Taylor SJ, Wong MK, Zhang H, Lodge NJ, Bronson JJ, Macor JE, Gillman KW.

ACS Chem Neurosci. 2016 Dec 21;7(12):1635-1640. doi: 10.1021/acschemneuro.6b00337. Epub 2016 Oct 18.

PMID:
27744678
16.

The Novel, Nicotinic Alpha7 Receptor Partial Agonist, BMS-933043, Improves Cognition and Sensory Processing in Preclinical Models of Schizophrenia.

Bristow LJ, Easton AE, Li YW, Sivarao DV, Lidge R, Jones KM, Post-Munson D, Daly C, Lodge NJ, Gallagher L, Molski T, Pieschl R, Chen P, Hendricson A, Westphal R, Cook J, Iwuagwu C, Morgan D, Benitex Y, King D, Macor JE, Zaczek R, Olson R.

PLoS One. 2016 Jul 28;11(7):e0159996. doi: 10.1371/journal.pone.0159996. eCollection 2016.

17.

Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.

Kostich W, Hamman BD, Li YW, Naidu S, Dandapani K, Feng J, Easton A, Bourin C, Baker K, Allen J, Savelieva K, Louis JV, Dokania M, Elavazhagan S, Vattikundala P, Sharma V, Das ML, Shankar G, Kumar A, Holenarsipur VK, Gulianello M, Molski T, Brown JM, Lewis M, Huang Y, Lu Y, Pieschl R, O'Malley K, Lippy J, Nouraldeen A, Lanthorn TH, Ye G, Wilson A, Balakrishnan A, Denton R, Grace JE, Lentz KA, Santone KS, Bi Y, Main A, Swaffield J, Carson K, Mandlekar S, Vikramadithyan RK, Nara SJ, Dzierba C, Bronson J, Macor JE, Zaczek R, Westphal R, Kiss L, Bristow L, Conway CM, Zambrowicz B, Albright CF.

J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. doi: 10.1124/jpet.116.235333. Epub 2016 Jul 13.

18.

Inhibition of in vivo [(3)H]MK-801 binding by NMDA receptor open channel blockers and GluN2B antagonists in rats and mice.

Fernandes A, Wojcik T, Baireddy P, Pieschl R, Newton A, Tian Y, Hong Y, Bristow L, Li YW.

Eur J Pharmacol. 2015 Nov 5;766:1-8. doi: 10.1016/j.ejphar.2015.08.044. Epub 2015 Aug 29.

PMID:
26325093
19.

Effect of acute NR2B antagonist treatment on long-term potentiation in the rat hippocampus.

Graef JD, Newberry K, Newton A, Pieschl R, Shields E, Luan FN, Simmermacher J, Luchetti D, Schaeffer E, Li YW, Kiss L, Bristow LJ.

Brain Res. 2015 Jun 3;1609:31-9. doi: 10.1016/j.brainres.2015.03.019. Epub 2015 Mar 19.

PMID:
25796435
20.

NR2B Antagonist CP-101,606 Abolishes Pitch-Mediated Deviance Detection in Awake Rats.

Sivarao DV, Chen P, Yang Y, Li YW, Pieschl R, Ahlijanian MK.

Front Psychiatry. 2014 Aug 5;5:96. doi: 10.3389/fpsyt.2014.00096. eCollection 2014.

21.

Monoamine reuptake site occupancy of sibutramine: Relationship to antidepressant-like and thermogenic effects in rats.

Li YW, Langdon S, Pieschl R, Strong T, Wright RN, Rohrbach K, Lelas S, Lodge NJ.

Eur J Pharmacol. 2014 Aug 15;737:47-56. doi: 10.1016/j.ejphar.2014.03.024. Epub 2014 May 10.

PMID:
24821570
22.

Synthesis and evaluation of candidate PET radioligands for corticotropin-releasing factor type-1 receptors.

Lodge NJ, Li YW, Chin FT, Dischino DD, Zoghbi SS, Deskus JA, Mattson RJ, Imaizumi M, Pieschl R, Molski TF, Fujita M, Dulac H, Zaczek R, Bronson JJ, Macor JE, Innis RB, Pike VW.

Nucl Med Biol. 2014 Jul;41(6):524-35. doi: 10.1016/j.nucmedbio.2014.03.005. Epub 2014 Mar 29.

23.

NK1 receptor antagonism lowers occupancy requirement for antidepressant-like effects of SSRIs in the gerbil forced swim test.

Lelas S, Li YW, Wallace-Boone TL, Taber MT, Newton AE, Pieschl RL, Davis CD, Molski TF, Newberry KS, Parker MF, Gillman KW, Bronson JJ, Macor JE, Lodge NJ.

Neuropharmacology. 2013 Oct;73:232-40. doi: 10.1016/j.neuropharm.2013.05.038. Epub 2013 Jun 12.

PMID:
23770339
24.

Design, optimization, and in vivo evaluation of a series of pyridine derivatives with dual NK1 antagonism and SERT inhibition for the treatment of depression.

Gillman KW, Parker MF, Silva M, Degnan AP, Tora GO, Lodge NJ, Li YW, Lelas S, Taber M, Krause RG, Bertekap RL, Newton AE, Pieschl RL, Lengyel KD, Johnson KA, Taylor SJ, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2013 Jan 15;23(2):407-11. doi: 10.1016/j.bmcl.2012.11.094. Epub 2012 Nov 30.

PMID:
23253443
25.

Ex vivo assessment of binding site occupancy of monoamine reuptake inhibitors: methodology and biological significance.

Lengyel K, Pieschl R, Strong T, Molski T, Mattson G, Lodge NJ, Li YW.

Neuropharmacology. 2008 Jul;55(1):63-70. doi: 10.1016/j.neuropharm.2008.04.014. Epub 2008 Apr 25.

PMID:
18538356
26.

Synthesis and KCNQ2 opener activity of N-(1-benzo[1,3]dioxol-5-yl-ethyl, N-[1-(2,3-dihydro-benzofuran-5-yl)-ethyl, and N-[1-(2,3-dihydro-1H-indol-5-yl)-ethyl acrylamides.

Wu YJ, Sun LQ, He H, Chen J, Starrett JE Jr, Dextraze P, Daris JP, Boissard CG, Pieschl RL, Gribkoff VK, Natale J, Knox RJ, Harden DG, Thompson MW, Fitzpatrick W, Weaver D, Wu D, Gao Q, Dworetzky SI.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4533-7.

PMID:
15357987
27.

(S)-N-[1-(4-cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons.

Wu YJ, Boissard CG, Chen J, Fitzpatrick W, Gao Q, Gribkoff VK, Harden DG, He H, Knox RJ, Natale J, Pieschl RL, Starrett JE Jr, Sun LQ, Thompson M, Weaver D, Wu D, Dworetzky SI.

Bioorg Med Chem Lett. 2004 Apr 19;14(8):1991-5.

PMID:
15050644
28.

GABA receptor-mediated inhibition of neuronal activity in rat SCN in vitro: pharmacology and influence of circadian phase.

Gribkoff VK, Pieschl RL, Dudek FE.

J Neurophysiol. 2003 Sep;90(3):1438-48. Epub 2003 May 15.

29.

Targeted disruption of the mouse Mel(1b) melatonin receptor.

Jin X, von Gall C, Pieschl RL, Gribkoff VK, Stehle JH, Reppert SM, Weaver DR.

Mol Cell Biol. 2003 Feb;23(3):1054-60.

30.

Targeting acute ischemic stroke with a calcium-sensitive opener of maxi-K potassium channels.

Gribkoff VK, Starrett JE Jr, Dworetzky SI, Hewawasam P, Boissard CG, Cook DA, Frantz SW, Heman K, Hibbard JR, Huston K, Johnson G, Krishnan BS, Kinney GG, Lombardo LA, Meanwell NA, Molinoff PB, Myers RA, Moon SL, Ortiz A, Pajor L, Pieschl RL, Post-Munson DJ, Signor LJ, Srinivas N, Taber MT, Thalody G, Trojnacki JT, Wiener H, Yeleswaram K, Yeola SW.

Nat Med. 2001 Apr;7(4):471-7.

PMID:
11283675
31.
32.

A reexamination of the role of GABA in the mammalian suprachiasmatic nucleus.

Gribkoff VK, Pieschl RL, Wisialowski TA, Park WK, Strecker GJ, de Jeu MT, Pennartz CM, Dudek FE.

J Biol Rhythms. 1999 Apr;14(2):126-30.

PMID:
10194649
33.
34.

Molecular dissection of two distinct actions of melatonin on the suprachiasmatic circadian clock.

Liu C, Weaver DR, Jin X, Shearman LP, Pieschl RL, Gribkoff VK, Reppert SM.

Neuron. 1997 Jul;19(1):91-102.

35.

Extreme derangements of acid-base balance in exercise: advantages and limitations of the Stewart analysis.

Fedde MR, Pieschl RL Jr.

Can J Appl Physiol. 1995 Sep;20(3):369-79. Review.

PMID:
8541799
36.

Fluid, electrolyte, and packed cell volume shifts in racing greyhounds.

Toll PW, Gaehtgens P, Neuhaus D, Pieschl RL, Fedde MR.

Am J Vet Res. 1995 Feb;56(2):227-32.

PMID:
7717591
37.

Acid-base changes in the running greyhound: contributing variables.

Pieschl RL, Toll PW, Leith DE, Peterson LJ, Fedde MR.

J Appl Physiol (1985). 1992 Dec;73(6):2297-304.

PMID:
1490936
38.

Mechanism of exercise-induced hypoxemia in horses.

Wagner PD, Gillespie JR, Landgren GL, Fedde MR, Jones BW, DeBowes RM, Pieschl RL, Erickson HH.

J Appl Physiol (1985). 1989 Mar;66(3):1227-33.

PMID:
2496088
39.

O2 transport in the horse during rest and exercise.

Landgren GL, Gillespie JR, Fedde MR, Jones BW, Pieschl RL, Wagner PD.

Adv Exp Med Biol. 1988;227:333-6.

PMID:
3381705

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