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Items: 33

1.

The Positive Allosteric Modulator of α2/3-Containing GABAA Receptors, KRM-II-81, Is Active in Pharmaco-Resistant Models of Epilepsy and Reduces Hyperexcitability after Traumatic Brain Injury.

Witkin JM, Li G, Golani LK, Xiong W, Smith JL, Ping X, Rashid F, Jahan R, Cerne R, Cook JM, Jin X.

J Pharmacol Exp Ther. 2020 Jan;372(1):83-94. doi: 10.1124/jpet.119.260968. Epub 2019 Nov 6.

PMID:
31694876
2.

The value of human epileptic tissue in the characterization and development of novel antiepileptic drugs: The example of CERC-611 and KRM-II-81.

Witkin JM, Ping X, Cerne R, Mouser C, Jin X, Hobbs J, Tiruveedhula VVNPB, Li G, Jahan R, Rashid F, Kumar Golani L, Cook JM, Smith JL.

Brain Res. 2019 Nov 1;1722:146356. doi: 10.1016/j.brainres.2019.146356. Epub 2019 Jul 29. Review.

PMID:
31369732
3.

The α2,3-selective potentiator of GABAA receptors, KRM-II-81, reduces nociceptive-associated behaviors induced by formalin and spinal nerve ligation in rats.

Witkin JM, Cerne R, Davis PG, Freeman KB, do Carmo JM, Rowlett JK, Methuku KR, Okun A, Gleason SD, Li X, Krambis MJ, Poe M, Li G, Schkeryantz JM, Jahan R, Yang L, Guo W, Golani LK, Anderson WH, Catlow JT, Jones TM, Porreca F, Smith JL, Knopp KL, Cook JM.

Pharmacol Biochem Behav. 2019 May;180:22-31. doi: 10.1016/j.pbb.2019.02.013. Epub 2019 Feb 27.

PMID:
30825491
4.

Catechol estrogens stimulate insulin secretion in pancreatic β-cells via activation of the transient receptor potential A1 (TRPA1) channel.

Ma W, Chen X, Cerne R, Syed SK, Ficorilli JV, Cabrera O, Obukhov AG, Efanov AM.

J Biol Chem. 2019 Feb 22;294(8):2935-2946. doi: 10.1074/jbc.RA118.005504. Epub 2018 Dec 26.

PMID:
30587572
5.

Use of ambiguous detections to improve estimates from species distribution models.

Louvrier J, Molinari-Jobin A, Kéry M, Chambert T, Miller D, Zimmermann F, Marboutin E, Molinari P, Müeller O, Černe R, Gimenez O.

Conserv Biol. 2019 Feb;33(1):185-195. doi: 10.1111/cobi.13191. Epub 2018 Sep 27.

PMID:
30009479
6.

Pharmacological characterization of the neurotrophic sesquiterpene jiadifenolide reveals a non-convulsant signature and potential for progression in neurodegenerative disease studies.

Witkin JM, Shenvi RA, Li X, Gleason SD, Weiss J, Morrow D, Catow JT, Wakulchik M, Ohtawa M, Lu HH, Martinez MD, Schkeryantz JM, Carpenter TS, Lightstone FC, Cerne R.

Biochem Pharmacol. 2018 Sep;155:61-70. doi: 10.1016/j.bcp.2018.06.022. Epub 2018 Jun 22.

7.

Bioisosteres of ethyl 8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo [1,5-a][1,4]diazepine-3-carboxylate (HZ-166) as novel alpha 2,3 selective potentiators of GABAA receptors: Improved bioavailability enhances anticonvulsant efficacy.

Witkin JM, Smith JL, Ping X, Gleason SD, Poe MM, Li G, Jin X, Hobbs J, Schkeryantz JM, McDermott JS, Alatorre AI, Siemian JN, Cramer JW, Airey DC, Methuku KR, Tiruveedhula VVNPB, Jones TM, Crawford J, Krambis MJ, Fisher JL, Cook JM, Cerne R.

Neuropharmacology. 2018 Jul 15;137:332-343. doi: 10.1016/j.neuropharm.2018.05.006. Epub 2018 May 3.

PMID:
29778948
8.

An antidepressant-related pharmacological signature for positive allosteric modulators of α2/3-containing GABAA receptors.

Methuku KR, Li X, Cerne R, Gleason SD, Schkeryantz JM, Tiruveedhula VVNPB, Golani LK, Li G, Poe MM, Rahman MT, Cook JM, Fisher JL, Witkin JM.

Pharmacol Biochem Behav. 2018 Jul;170:9-13. doi: 10.1016/j.pbb.2018.04.009. Epub 2018 Apr 30.

PMID:
29715490
9.

Negative allosteric modulation of alpha 5-containing GABAA receptors engenders antidepressant-like effects and selectively prevents age-associated hyperactivity in tau-depositing mice.

Xu NZ, Ernst M, Treven M, Cerne R, Wakulchik M, Li X, Jones TM, Gleason SD, Morrow D, Schkeryantz JM, Rahman MT, Li G, Poe MM, Cook JM, Witkin JM.

Psychopharmacology (Berl). 2018 Apr;235(4):1151-1161. doi: 10.1007/s00213-018-4832-9. Epub 2018 Jan 26.

PMID:
29374303
10.

Synthesis of (-)-11-O-Debenzoyltashironin: Neurotrophic Sesquiterpenes Cause Hyperexcitation.

Ohtawa M, Krambis MJ, Cerne R, Schkeryantz JM, Witkin JM, Shenvi RA.

J Am Chem Soc. 2017 Jul 19;139(28):9637-9644. doi: 10.1021/jacs.7b04206. Epub 2017 Jul 6.

PMID:
28644021
11.

Further evaluation of the potential anxiolytic activity of imidazo[1,5-a][1,4]diazepin agents selective for α2/3-containing GABAA receptors.

Witkin JM, Cerne R, Wakulchik M, S J, Gleason SD, Jones TM, Li G, Arnold LA, Li JX, Schkeryantz JM, Methuku KR, Cook JM, Poe MM.

Pharmacol Biochem Behav. 2017 Jun;157:35-40. doi: 10.1016/j.pbb.2017.04.009. Epub 2017 Apr 22.

12.

Automated Electrophysiology Assays.

Priest BT, Cerne R, Krambis MJ, Schmalhofer WA, Wakulchik M, Wilenkin B, Burris KD.

In: Sittampalam GS, Grossman A, Brimacombe K, Arkin M, Auld D, Austin CP, Baell J, Bejcek B, Caaveiro JMM, Chung TDY, Coussens NP, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Haas JV, Hoare SRJ, Inglese J, Iversen PW, Kahl SD, Kales SC, Kirshner S, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Saradjian P, Trask OJ Jr., Weidner JR, Wildey MJ, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.
2017 Mar 9.

13.

Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABAA) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy.

Poe MM, Methuku KR, Li G, Verma AR, Teske KA, Stafford DC, Arnold LA, Cramer JW, Jones TM, Cerne R, Krambis MJ, Witkin JM, Jambrina E, Rehman S, Ernst M, Cook JM, Schkeryantz JM.

J Med Chem. 2016 Dec 8;59(23):10800-10806. Epub 2016 Nov 28.

14.

IonWorks Barracuda Assay for Assessment of State-Dependent Sodium Channel Modulators.

Cerne R, Wakulchik M, Krambis MJ, Burris KD, Priest BT.

Assay Drug Dev Technol. 2016 Mar;14(2):84-92. doi: 10.1089/adt.2015.677. Epub 2016 Feb 4.

PMID:
26844665
15.

An Integrated Approach for Screening and Identification of Positive Allosteric Modulators of N-Methyl-D-Aspartate Receptors.

Jambrina E, Cerne R, Smith E, Scampavia L, Cuadrado M, Findlay J, Krambis MJ, Wakulchik M, Chase P, Brunavs M, Burris KD, Gallagher P, Spicer TP, Ursu D.

J Biomol Screen. 2016 Jun;21(5):468-79. doi: 10.1177/1087057116628437. Epub 2016 Feb 2.

PMID:
26838761
16.

Optimization of a High-Throughput Assay for Calcium Channel Modulators on IonWorks Barracuda.

Cerne R, Wakulchik M, Li B, Burris KD, Priest BT.

Assay Drug Dev Technol. 2016 Mar;14(2):75-83. doi: 10.1089/adt.2015.678. Epub 2015 Dec 30.

PMID:
26716356
17.

Triphenylphosphine oxide is a potent and selective inhibitor of the transient receptor potential melastatin-5 ion channel.

Palmer RK, Atwal K, Bakaj I, Carlucci-Derbyshire S, Buber MT, Cerne R, Cortés RY, Devantier HR, Jorgensen V, Pawlyk A, Lee SP, Sprous DG, Zhang Z, Bryant R.

Assay Drug Dev Technol. 2010 Dec;8(6):703-13. doi: 10.1089/adt.2010.0334.

PMID:
21158685
18.

Overexpression of human transient receptor potential M5 upregulates endogenous human transient receptor potential A1 in a stable HEK cell line.

Buber MT, Cerne R, Cortés RY, Bryant RW, Lee SP.

Assay Drug Dev Technol. 2010 Dec;8(6):695-702. doi: 10.1089/adt.2010.0316. Epub 2010 Dec 6.

PMID:
21133676
19.

Thymol and related alkyl phenols activate the hTRPA1 channel.

Lee SP, Buber MT, Yang Q, Cerne R, Cortés RY, Sprous DG, Bryant RW.

Br J Pharmacol. 2008 Apr;153(8):1739-49. doi: 10.1038/bjp.2008.85. Epub 2008 Mar 10.

20.

Pharmacological characterization of recombinant N-type calcium channel (Cav2.2) mediated calcium mobilization using FLIPR.

Benjamin ER, Pruthi F, Olanrewaju S, Shan S, Hanway D, Liu X, Cerne R, Lavery D, Valenzano KJ, Woodward RM, Ilyin VI.

Biochem Pharmacol. 2006 Sep 14;72(6):770-82. Epub 2006 Jul 17.

PMID:
16844100
21.

Electrophysiological correlates to the intrinsic optical signal in the rat neocortical slice.

Cerne R, Haglund MM.

Neurosci Lett. 2002 Jan 14;317(3):147-50.

PMID:
11755261
22.

Evidence of altered inhibition in layer V pyramidal neurons from neocortex of Kcna1-null mice.

van Brederode JF, Rho JM, Cerne R, Tempel BL, Spain WJ.

Neuroscience. 2001;103(4):921-9.

PMID:
11301201
23.

GABAA mediated afterdepolarization in pyramidal neurons from rat neocortex.

Cerne R, Spain WJ.

J Neurophysiol. 1997 Feb;77(2):1039-45.

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25.

Interaction of neuropeptides and excitatory amino acids in the rat superficial spinal dorsal horn.

Randić M, Kolaj M, Kojić L, Cerne R, Cheng G, Wang RA.

Prog Brain Res. 1995;104:225-53. Review. No abstract available.

PMID:
8552771
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29.

Interactions between excitatory amino acids and tachykinins and long-term changes of synaptic responses in the rat spinal dorsal horn.

Randic M, Jiang MC, Rusin KI, Cerne R, Kolaj M.

Regul Pept. 1993 Jul 2;46(1-2):418-20. No abstract available.

PMID:
7692554
30.

Interactions between excitatory amino acids and tachykinins in the rat spinal dorsal horn.

Rusin KI, Jiang MC, Cerne R, Randic M.

Brain Res Bull. 1993;30(3-4):329-38.

PMID:
7681351
31.
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