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Items: 1 to 50 of 80

1.

The need for new approaches in CNS drug discovery: Why drugs have failed, and what can be done to improve outcomes.

Gribkoff VK, Kaczmarek LK.

Neuropharmacology. 2017 Jul 1;120:11-19. doi: 10.1016/j.neuropharm.2016.03.021. Epub 2016 Mar 12. Review.

2.

The mitochondrial complex V-associated large-conductance inner membrane current is regulated by cyclosporine and dexpramipexole.

Alavian KN, Dworetzky SI, Bonanni L, Zhang P, Sacchetti S, Li H, Signore AP, Smith PJ, Gribkoff VK, Jonas EA.

Mol Pharmacol. 2015 Jan;87(1):1-8. doi: 10.1124/mol.114.095661. Epub 2014 Oct 20.

3.

Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain.

Wu YJ, Conway CM, Sun LQ, Machet F, Chen J, Chen P, He H, Bourin C, Calandra V, Polino JL, Davis CD, Heman K, Gribkoff VK, Boissard CG, Knox RJ, Thompson MW, Fitzpatrick W, Weaver D, Harden DG, Natale J, Dworetzky SI, Starrett JE Jr.

Bioorg Med Chem Lett. 2013 Nov 15;23(22):6188-91. doi: 10.1016/j.bmcl.2013.08.092. Epub 2013 Sep 8.

PMID:
24070783
4.

Effects of dexpramipexole on brain mitochondrial conductances and cellular bioenergetic efficiency.

Alavian KN, Dworetzky SI, Bonanni L, Zhang P, Sacchetti S, Mariggio MA, Onofrj M, Thomas A, Li H, Mangold JE, Signore AP, Demarco U, Demady DR, Nabili P, Lazrove E, Smith PJ, Gribkoff VK, Jonas EA.

Brain Res. 2012 Mar 29;1446:1-11. doi: 10.1016/j.brainres.2012.01.046. Epub 2012 Jan 28.

5.

The effects of dexpramipexole (KNS-760704) in individuals with amyotrophic lateral sclerosis.

Cudkowicz M, Bozik ME, Ingersoll EW, Miller R, Mitsumoto H, Shefner J, Moore DH, Schoenfeld D, Mather JL, Archibald D, Sullivan M, Amburgey C, Moritz J, Gribkoff VK.

Nat Med. 2011 Nov 20;17(12):1652-6. doi: 10.1038/nm.2579.

PMID:
22101764
6.

Safety, tolerability, and pharmacokinetics of KNS-760704 (dexpramipexole) in healthy adult subjects.

Bozik ME, Mather JL, Kramer WG, Gribkoff VK, Ingersoll EW.

J Clin Pharmacol. 2011 Aug;51(8):1177-85. doi: 10.1177/0091270010379412. Epub 2010 Oct 19.

PMID:
20959524
7.

KNS-760704 [(6R)-4,5,6,7-tetrahydro-N6-propyl-2, 6-benzothiazole-diamine dihydrochloride monohydrate] for the treatment of amyotrophic lateral sclerosis.

Gribkoff VK, Bozik ME.

CNS Neurosci Ther. 2008 Fall;14(3):215-26. doi: 10.1111/j.1755-5949.2008.00048.x. Review.

8.

The therapeutic potential of neuronal K V 7 (KCNQ) channel modulators: an update.

Gribkoff VK.

Expert Opin Ther Targets. 2008 May;12(5):565-81. doi: 10.1517/14728222.12.5.565 . Review.

PMID:
18410240
9.

Atropisomeric 3-(beta-hydroxyethyl)-4-arylquinolin-2-ones as Maxi-K potassium channel openers.

Vrudhula VM, Dasgupta B, Qian-Cutrone J, Kozlowski ES, Boissard CG, Dworetzky SI, Wu D, Gao Q, Kimura R, Gribkoff VK, Starrett JE Jr.

J Med Chem. 2007 Mar 8;50(5):1050-7. Epub 2007 Feb 3.

PMID:
17274609
10.

3-[(5-Chloro-2-hydroxyphenyl)methyl]-5-[4-(trifluoromethyl)phenyl ]-1,3,4-oxadiazol-2(3H)-one, BMS-191011: opener of large-conductance Ca(2+)-activated potassium (maxi-K) channels, identification, solubility, and SAR.

Romine JL, Martin SW, Meanwell NA, Gribkoff VK, Boissard CG, Dworetzky SI, Natale J, Moon S, Ortiz A, Yeleswaram S, Pajor L, Gao Q, Starrett JE Jr.

J Med Chem. 2007 Feb 8;50(3):528-42.

PMID:
17266205
11.

The role of voltage-gated calcium channels in pain and nociception.

Gribkoff VK.

Semin Cell Dev Biol. 2006 Oct;17(5):555-64. Epub 2006 Sep 23. Review.

PMID:
17141538
12.

Donepezil primarily attenuates scopolamine-induced deficits in psychomotor function, with moderate effects on simple conditioning and attention, and small effects on working memory and spatial mapping.

Lindner MD, Hogan JB, Hodges DB Jr, Orie AF, Chen P, Corsa JA, Leet JE, Gillman KW, Rose GM, Jones KM, Gribkoff VK.

Psychopharmacology (Berl). 2006 Nov;188(4):629-40. Epub 2006 Sep 27.

PMID:
17004085
13.

Pharmacological activation and inhibition of Slack (Slo2.2) channels.

Yang B, Gribkoff VK, Pan J, Damagnez V, Dworetzky SI, Boissard CG, Bhattacharjee A, Yan Y, Sigworth FJ, Kaczmarek LK.

Neuropharmacology. 2006 Sep;51(4):896-906. Epub 2006 Jul 28.

PMID:
16876206
14.

Soluble Abeta and cognitive function in aged F-344 rats and Tg2576 mice.

Lindner MD, Hogan JB, Krause RG, Machet F, Bourin C, Hodges DB Jr, Corsa JA, Barten DM, Toyn JH, Stock DA, Rose GM, Gribkoff VK.

Behav Brain Res. 2006 Oct 2;173(1):62-75. Epub 2006 Jul 7.

PMID:
16828889
15.

Analogs of a potent maxi-K potassium channel opener with an improved inhibitory profile toward cytochrome P450 isozymes.

Vrudhula VM, Dasgupta B, Boissard CG, Gribkoff VK, Santone KS, Dalterio RA, Lodge NJ, Starrett JE Jr.

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4286-90.

PMID:
16061379
16.

Use-dependent blockade of Cav2.2 voltage-gated calcium channels for neuropathic pain.

Winquist RJ, Pan JQ, Gribkoff VK.

Biochem Pharmacol. 2005 Aug 15;70(4):489-99. Review.

PMID:
15950195
17.

Voltage-gated cation channel modulators for the treatment of stroke.

Gribkoff VK, Winquist RJ.

Expert Opin Investig Drugs. 2005 May;14(5):579-92. Review.

PMID:
15926865
18.

3-Thio-quinolinone maxi-K openers for the treatment of erectile dysfunction.

Boy KM, Guernon JM, Sit SY, Xie K, Hewawasam P, Boissard CG, Dworetzky SI, Natale J, Gribkoff VK, Lodge N, Starrett JE Jr.

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5089-93.

PMID:
15380205
19.

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
20.

4-Aryl-3-(mercapto)quinolin-2-ones: novel maxi-K channel opening relaxants of corporal smooth muscle.

Hewawasam P, Fan W, Cook DA, Newberry KS, Boissard CG, Gribkoff VK, Starrett J, Lodge NJ.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4479-82.

PMID:
15357975
21.

Synthesis and structure-activity relationship of acrylamides as KCNQ2 potassium channel openers.

Wu YJ, He H, Sun LQ, L'Heureux A, Chen J, Dextraze P, Starrett JE Jr, Boissard CG, Gribkoff VK, Natale J, Dworetzky SI.

J Med Chem. 2004 May 20;47(11):2887-96.

PMID:
15139767
22.

(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
23.

The synthesis and structure-activity relationships of 3-amino-4-benzylquinolin-2-ones; discovery of novel KCNQ2 channel openers.

Hewawasam P, Chen N, Ding M, Natale JT, Boissard CG, Yeola S, Gribkoff VK, Starrett J, Dworetzky SI.

Bioorg Med Chem Lett. 2004 Apr 5;14(7):1615-8.

PMID:
15026035
24.

Long-lasting functional disabilities in middle-aged rats with small cerebral infarcts.

Lindner MD, Gribkoff VK, Donlan NA, Jones TA.

J Neurosci. 2003 Nov 26;23(34):10913-22.

25.

The therapeutic potential of neuronal KCNQ channel modulators.

Gribkoff VK.

Expert Opin Ther Targets. 2003 Dec;7(6):737-48. Review.

PMID:
14640909
26.

An assessment of the effects of serotonin 6 (5-HT6) receptor antagonists in rodent models of learning.

Lindner MD, Hodges DB Jr, Hogan JB, Orie AF, Corsa JA, Barten DM, Polson C, Robertson BJ, Guss VL, Gillman KW, Starrett JE Jr, Gribkoff VK.

J Pharmacol Exp Ther. 2003 Nov;307(2):682-91. Epub 2003 Sep 15.

PMID:
12975483
27.

(S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine.

Wu YJ, Boissard CG, Greco C, Gribkoff VK, Harden DG, He H, L'Heureux A, Kang SH, Kinney GG, Knox RJ, Natale J, Newton AE, Lehtinen-Oboma S, Sinz MW, Sivarao DV, Starrett JE Jr, Sun LQ, Tertyshnikova S, Thompson MW, Weaver D, Wong HS, Zhang L, Dworetzky SI.

J Med Chem. 2003 Jul 17;46(15):3197-200.

PMID:
12852750
28.

4-Aryl-3-(hydroxyalkyl)quinolin-2-ones: novel maxi-K channel opening relaxants of corporal smooth muscle targeted for erectile dysfunction.

Hewawasam P, Fan W, Ding M, Flint K, Cook D, Goggins GD, Myers RA, Gribkoff VK, Boissard CG, Dworetzky SI, Starrett JE Jr, Lodge NJ.

J Med Chem. 2003 Jul 3;46(14):2819-22.

PMID:
12825925
29.

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.

30.

Synthesis of water-soluble prodrugs of BMS-191011: a maxi-K channel opener targeted for post-stroke neuroprotection.

Hewawasam P, Ding M, Chen N, King D, Knipe J, Pajor L, Ortiz A, Gribkoff VK, Starrett J.

Bioorg Med Chem Lett. 2003 May 19;13(10):1695-8.

PMID:
12729644
31.

Novel openers of Ca2+-dependent large-conductance potassium channels: symmetrical pharmacophore and electrophysiological evaluation of bisphenols.

Li Y, Johnson G, Romine JL, Meanwell NA, Martin SW, Dworetzky SI, Boissard CG, Gribkoff VK, Starrett JE Jr.

Bioorg Med Chem Lett. 2003 Apr 17;13(8):1437-9.

PMID:
12668007
32.

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.

33.

4,5-diphenyltriazol-3-ones: openers of large-conductance Ca(2+)-activated potassium (maxi-K) channels.

Romine JL, Martin SW, Gribkoff VK, Boissard CG, Dworetzky SI, Natale J, Li Y, Gao Q, Meanwell NA, Starrett JE Jr.

J Med Chem. 2002 Jul 4;45(14):2942-52.

PMID:
12086481
34.
35.

The synthesis and structure-activity relationships of 1,3-diaryl 1,2,4-(4H)-triazol-5-ones: a new class of calcium-dependent, large conductance, potassium (maxi-K) channel opener targeted for urge urinary incontinence.

Hewawasam P, Erway M, Thalody G, Weiner H, Boissard CG, Gribkoff VK, Meanwell NA, Lodge N, Starrett JE Jr.

Bioorg Med Chem Lett. 2002 Apr 8;12(7):1117-20.

PMID:
11909730
36.

The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.

Hewawasam P, Gribkoff VK, Pendri Y, Dworetzky SI, Meanwell NA, Martinez E, Boissard CG, Post-Munson DJ, Trojnacki JT, Yeleswaram K, Pajor LM, Knipe J, Gao Q, Perrone R, Starrett JE Jr.

Bioorg Med Chem Lett. 2002 Apr 8;12(7):1023-6.

PMID:
11909708
37.

Synthesis and structure-activity relationships of 3-aryloxindoles: a new class of calcium-dependent, large conductance potassium (maxi-K) channel openers with neuroprotective properties.

Hewawasam P, Erway M, Moon SL, Knipe J, Weiner H, Boissard CG, Post-Munson DJ, Gao Q, Huang S, Gribkoff VK, Meanwell NA.

J Med Chem. 2002 Mar 28;45(7):1487-99.

PMID:
11906290
38.

Radiochemical synthesis and biodistribution of a novel maxi-K potassium channel opener.

Kiesewetter DO, Jagoda EM, Starrett JE Jr, Gribkoff VK, Hewawasam P, Srinivas N, Salazar D, Eckelman WC.

Nucl Med Biol. 2002 Jan;29(1):55-9.

PMID:
11786276
39.

Maxi-K potassium channels: form, function, and modulation of a class of endogenous regulators of intracellular calcium.

Gribkoff VK, Starrett JE Jr, Dworetzky SI.

Neuroscientist. 2001 Apr;7(2):166-77. Review.

PMID:
11496927
41.

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
42.

An assessment of the present and future roles of non-ligand gated ion channel modulators as CNS therapeutics.

Gribkoff VK, Starrett JE.

Expert Opin Pharmacother. 1999 Nov;1(1):61-70. Review.

PMID:
11249565
43.
44.

Cognition-enhancing drugs increase stimulated hippocampal theta rhythm amplitude in the urethane-anesthetized rat.

Kinney GG, Patino P, Mermet-Bouvier Y, Starrett JE Jr, Gribkoff VK.

J Pharmacol Exp Ther. 1999 Oct;291(1):99-106.

PMID:
10490892
45.

Formation of intermediate-conductance calcium-activated potassium channels by interaction of Slack and Slo subunits.

Joiner WJ, Tang MD, Wang LY, Dworetzky SI, Boissard CG, Gan L, Gribkoff VK, Kaczmarek LK.

Nat Neurosci. 1998 Oct;1(6):462-9.

PMID:
10196543
46.

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
47.
48.

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.

49.

The pharmacology and molecular biology of large-conductance calcium-activated (BK) potassium channels.

Gribkoff VK, Starrett JE Jr, Dworetzky SI.

Adv Pharmacol. 1997;37:319-48. Review. No abstract available.

PMID:
8891106
50.

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