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Items: 27

1.

Benzoxazolinone aryl sulfonamides as potent, selective Nav1.7 inhibitors with in vivo efficacy in a preclinical pain model.

Pero JE, Rossi MA, Lehman HDGF, Kelly MJ 3rd, Mulhearn JJ, Wolkenberg SE, Cato MJ, Clements MK, Daley CJ, Filzen T, Finger EN, Gregan Y, Henze DA, Jovanovska A, Klein R, Kraus RL, Li Y, Liang A, Majercak JM, Panigel J, Urban MO, Wang J, Wang YH, Houghton AK, Layton ME.

Bioorg Med Chem Lett. 2017 Jun 15;27(12):2683-2688. doi: 10.1016/j.bmcl.2017.04.040. Epub 2017 Apr 22.

PMID:
28465103
2.

Discovery of selective, orally bioavailable, N-linked arylsulfonamide Nav1.7 inhibitors with pain efficacy in mice.

Roecker AJ, Egbertson M, Jones KLG, Gomez R, Kraus RL, Li Y, Koser AJ, Urban MO, Klein R, Clements M, Panigel J, Daley C, Wang J, Finger EN, Majercak J, Santarelli V, Gregan I, Cato M, Filzen T, Jovanovska A, Wang YH, Wang D, Joyce LA, Sherer EC, Peng X, Wang X, Sun H, Coleman PJ, Houghton AK, Layton ME.

Bioorg Med Chem Lett. 2017 May 15;27(10):2087-2093. doi: 10.1016/j.bmcl.2017.03.085. Epub 2017 Mar 30.

PMID:
28389149
3.

Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications.

de Lera Ruiz M, Kraus RL.

J Med Chem. 2015 Sep 24;58(18):7093-118. doi: 10.1021/jm501981g. Epub 2015 May 14. Review.

PMID:
25927480
4.

Discovery of a pharmacologically active antagonist of the two-pore-domain potassium channel K2P9.1 (TASK-3).

Coburn CA, Luo Y, Cui M, Wang J, Soll R, Dong J, Hu B, Lyon MA, Santarelli VP, Kraus RL, Gregan Y, Wang Y, Fox SV, Binns J, Doran SM, Reiss DR, Tannenbaum PL, Gotter AL, Meinke PT, Renger JJ.

ChemMedChem. 2012 Jan 2;7(1):123-33. doi: 10.1002/cmdc.201100351. Epub 2011 Sep 14.

PMID:
21916012
5.

TASK-3 as a potential antidepressant target.

Gotter AL, Santarelli VP, Doran SM, Tannenbaum PL, Kraus RL, Rosahl TW, Meziane H, Montial M, Reiss DR, Wessner K, McCampbell A, Stevens J, Brunner JI, Fox SV, Uebele VN, Bayliss DA, Winrow CJ, Renger JJ.

Brain Res. 2011 Oct 6;1416:69-79. doi: 10.1016/j.brainres.2011.08.021. Epub 2011 Aug 16.

6.

Pyridyl amides as potent inhibitors of T-type calcium channels.

Reger TS, Yang ZQ, Schlegel KA, Shu Y, Mattern C, Cube R, Rittle KE, McGaughey GB, Hartman GD, Tang C, Ballard J, Kuo Y, Prueksaritanont T, Nuss CE, Doran SM, Fox SV, Garson SL, Li Y, Kraus RL, Uebele VN, Renger JJ, Barrow JC.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1692-6. doi: 10.1016/j.bmcl.2011.01.089. Epub 2011 Jan 26.

PMID:
21316226
7.

Short-acting T-type calcium channel antagonists significantly modify sleep architecture in rodents.

Yang ZQ, Schlegel KA, Shu Y, Reger TS, Cube R, Mattern C, Coleman PJ, Small J, Hartman GD, Ballard J, Tang C, Kuo Y, Prueksaritanont T, Nuss CE, Doran S, Fox SV, Garson SL, Li Y, Kraus RL, Uebele VN, Taylor AB, Zeng W, Fang W, Chavez-Eng C, Troyer MD, Luk JA, Laethem T, Cook WO, Renger JJ, Barrow JC.

ACS Med Chem Lett. 2010 Aug 24;1(9):504-9. doi: 10.1021/ml100170e. eCollection 2010 Dec 9.

8.

In vitro characterization of T-type calcium channel antagonist TTA-A2 and in vivo effects on arousal in mice.

Kraus RL, Li Y, Gregan Y, Gotter AL, Uebele VN, Fox SV, Doran SM, Barrow JC, Yang ZQ, Reger TS, Koblan KS, Renger JJ.

J Pharmacol Exp Ther. 2010 Nov;335(2):409-17. doi: 10.1124/jpet.110.171058. Epub 2010 Aug 3.

PMID:
20682849
9.

Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists.

Schlegel KA, Yang ZQ, Reger TS, Shu Y, Cube R, Rittle KE, Bondiskey P, Bock MG, Hartman GD, Tang C, Ballard J, Kuo Y, Prueksaritanont T, Nuss CE, Doran SM, Fox SV, Garson SL, Kraus RL, Li Y, Uebele VN, Renger JJ, Barrow JC.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5147-52. doi: 10.1016/j.bmcl.2010.07.010. Epub 2010 Jul 8.

PMID:
20673719
10.

Discovery of 4,4-Disubstituted Quinazolin-2-ones as T-Type Calcium Channel Antagonists.

Barrow JC, Rittle KE, Reger TS, Yang ZQ, Bondiskey P, McGaughey GB, Bock MG, Hartman GD, Tang C, Ballard J, Kuo Y, Prueksaritanont T, Nuss CE, Doran SM, Fox SV, Garson SL, Kraus RL, Li Y, Marino MJ, Kuzmick Graufelds V, Uebele VN, Renger JJ.

ACS Med Chem Lett. 2010 Feb 1;1(2):75-9. doi: 10.1021/ml100004r. eCollection 2010 May 13.

11.

Positive allosteric interaction of structurally diverse T-type calcium channel antagonists.

Uebele VN, Nuss CE, Fox SV, Garson SL, Cristescu R, Doran SM, Kraus RL, Santarelli VP, Li Y, Barrow JC, Yang ZQ, Schlegel KA, Rittle KE, Reger TS, Bednar RA, Lemaire W, Mullen FA, Ballard JE, Tang C, Dai G, McManus OB, Koblan KS, Renger JJ.

Cell Biochem Biophys. 2009;55(2):81-93. doi: 10.1007/s12013-009-9057-4. Epub 2009 Jul 7.

PMID:
19582593
12.

Antagonism of T-type calcium channels inhibits high-fat diet-induced weight gain in mice.

Uebele VN, Gotter AL, Nuss CE, Kraus RL, Doran SM, Garson SL, Reiss DR, Li Y, Barrow JC, Reger TS, Yang ZQ, Ballard JE, Tang C, Metzger JM, Wang SP, Koblan KS, Renger JJ.

J Clin Invest. 2009 Jun;119(6):1659-67. doi: 10.1172/JCI36954. Epub 2009 May 18.

13.

Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n,n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats.

Whitman DB, Cox CD, Breslin MJ, Brashear KM, Schreier JD, Bogusky MJ, Bednar RA, Lemaire W, Bruno JG, Hartman GD, Reiss DR, Harrell CM, Kraus RL, Li Y, Garson SL, Doran SM, Prueksaritanont T, Li C, Winrow CJ, Koblan KS, Renger JJ, Coleman PJ.

ChemMedChem. 2009 Jul;4(7):1069-74. doi: 10.1002/cmdc.200900069.

PMID:
19418500
14.

T-type calcium channels regulate cortical plasticity in-vivo. [corrected].

Uebele VN, Nuss CE, Santarelli VP, Garson SL, Kraus RL, Barrow JC, Stauffer SR, Koblan KS, Renger JJ, Aton S, Seibt J, Dumoulin M, Jha SK, Coleman T, Frank MG.

Neuroreport. 2009 Feb 18;20(3):257-62. doi: 10.1097/WNR.0b013e3283200111. Erratum in: Neuroreport. 2009 Jul 1;20(10):973. Kraus, Richard L [added].

15.

Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.

Yang ZQ, Barrow JC, Shipe WD, Schlegel KA, Shu Y, Yang FV, Lindsley CW, Rittle KE, Bock MG, Hartman GD, Uebele VN, Nuss CE, Fox SV, Kraus RL, Doran SM, Connolly TM, Tang C, Ballard JE, Kuo Y, Adarayan ED, Prueksaritanont T, Zrada MM, Marino MJ, Graufelds VK, DiLella AG, Reynolds IJ, Vargas HM, Bunting PB, Woltmann RF, Magee MM, Koblan KS, Renger JJ.

J Med Chem. 2008 Oct 23;51(20):6471-7. doi: 10.1021/jm800830n. Epub 2008 Sep 26.

PMID:
18817368
16.

Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.

Shipe WD, Barrow JC, Yang ZQ, Lindsley CW, Yang FV, Schlegel KA, Shu Y, Rittle KE, Bock MG, Hartman GD, Tang C, Ballard JE, Kuo Y, Adarayan ED, Prueksaritanont T, Zrada MM, Uebele VN, Nuss CE, Connolly TM, Doran SM, Fox SV, Kraus RL, Marino MJ, Graufelds VK, Vargas HM, Bunting PB, Hasbun-Manning M, Evans RM, Koblan KS, Renger JJ.

J Med Chem. 2008 Jul 10;51(13):3692-5. doi: 10.1021/jm800419w. Epub 2008 Jun 10.

PMID:
18540666
17.

Inhibition of sodium channel gating by trapping the domain II voltage sensor with protoxin II.

Sokolov S, Kraus RL, Scheuer T, Catterall WA.

Mol Pharmacol. 2008 Mar;73(3):1020-8. Epub 2007 Dec 21.

PMID:
18156314
18.

Trazodone inhibits T-type calcium channels.

Kraus RL, Li Y, Jovanovska A, Renger JJ.

Neuropharmacology. 2007 Aug;53(2):308-17. Epub 2007 May 26.

PMID:
17610910
19.

Antioxidant properties of minocycline: neuroprotection in an oxidative stress assay and direct radical-scavenging activity.

Kraus RL, Pasieczny R, Lariosa-Willingham K, Turner MS, Jiang A, Trauger JW.

J Neurochem. 2005 Aug;94(3):819-27.

20.

Fyx is associated with two missense point mutations in its gene and can be detected by PCR-SSP.

Gassner C, Kraus RL, Dovc T, Kilga-Nogler S, Utz I, Mueller TH, Schunter F, Schoenitzer D.

Immunohematology. 2000;16(2):61-7.

PMID:
15373620
21.

Two tarantula peptides inhibit activation of multiple sodium channels.

Middleton RE, Warren VA, Kraus RL, Hwang JC, Liu CJ, Dai G, Brochu RM, Kohler MG, Gao YD, Garsky VM, Bogusky MJ, Mehl JT, Cohen CJ, Smith MM.

Biochemistry. 2002 Dec 17;41(50):14734-47.

PMID:
12475222
22.

Functional consequences of P/Q-type Ca2+ channel Cav2.1 missense mutations associated with episodic ataxia type 2 and progressive ataxia.

Wappl E, Koschak A, Poteser M, Sinnegger MJ, Walter D, Eberhart A, Groschner K, Glossmann H, Kraus RL, Grabner M, Striessnig J.

J Biol Chem. 2002 Mar 1;277(9):6960-6. Epub 2001 Dec 12.

23.

Three new familial hemiplegic migraine mutants affect P/Q-type Ca(2+) channel kinetics.

Kraus RL, Sinnegger MJ, Koschak A, Glossmann H, Stenirri S, Carrera P, Striessnig J.

J Biol Chem. 2000 Mar 31;275(13):9239-43.

24.

Molecular mechanism of diltiazem interaction with L-type Ca2+ channels.

Kraus RL, Hering S, Grabner M, Ostler D, Striessnig J.

J Biol Chem. 1998 Oct 16;273(42):27205-12.

25.

Molecular basis of drug interaction with L-type Ca2+ channels.

Mitterdorfer J, Grabner M, Kraus RL, Hering S, Prinz H, Glossmann H, Striessnig J.

J Bioenerg Biomembr. 1998 Aug;30(4):319-34. Review.

PMID:
9758329
26.

Familial hemiplegic migraine mutations change alpha1A Ca2+ channel kinetics.

Kraus RL, Sinnegger MJ, Glossmann H, Hering S, Striessnig J.

J Biol Chem. 1998 Mar 6;273(10):5586-90.

27.

Molecular mechanism of use-dependent calcium channel block by phenylalkylamines: role of inactivation.

Hering S, Aczél S, Kraus RL, Berjukow S, Striessnig J, Timin EN.

Proc Natl Acad Sci U S A. 1997 Nov 25;94(24):13323-8.

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