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Items: 25

1.

Rat NaV1.7 loss-of-function genetic model: Deficient nociceptive and neuropathic pain behavior with retained olfactory function and intra-epidermal nerve fibers.

Grubinska B, Chen L, Alsaloum M, Rampal N, Matson DJ, Yang C, Taborn K, Zhang M, Youngblood B, Liu D, Galbreath E, Allred S, Lepherd M, Ferrando R, Kornecook TJ, Lehto SG, Waxman SG, Moyer BD, Dib-Hajj S, Gingras J.

Mol Pain. 2019 Jan-Dec;15:1744806919881846. doi: 10.1177/1744806919881846. No abstract available.

2.

Pharmacological Assessment of Sepiapterin Reductase Inhibition on Tactile Response in the Rat.

Meyer JT, Sparling BA, McCarty WJ, Zhang M, Soto M, Schneider S, Chen H, Roberts J, Tan H, Kornecook T, Andrews PS, Knutson CG.

J Pharmacol Exp Ther. 2019 Nov;371(2):476-486. doi: 10.1124/jpet.119.257105. Epub 2019 May 20.

PMID:
31110114
3.

Engineering NaV1.7 Inhibitory JzTx-V Peptides with a Potency and Basicity Profile Suitable for Antibody Conjugation To Enhance Pharmacokinetics.

Murray JK, Wu B, Tegley CM, Nixey TE, Falsey JR, Herberich B, Yin L, Sham K, Long J, Aral J, Cheng Y, Netirojjanakul C, Doherty L, Glaus C, Ikotun T, Li H, Tran L, Soto M, Salimi-Moosavi H, Ligutti J, Amagasu S, Andrews KL, Be X, Lin MJ, Foti RS, Ilch CP, Youngblood B, Kornecook TJ, Karow M, Walker KW, Moyer BD, Biswas K, Miranda LP.

ACS Chem Biol. 2019 Apr 19;14(4):806-818. doi: 10.1021/acschembio.9b00183. Epub 2019 Mar 27.

PMID:
30875193
4.

Discovery of Tarantula Venom-Derived NaV1.7-Inhibitory JzTx-V Peptide 5-Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis.

Wu B, Murray JK, Andrews KL, Sham K, Long J, Aral J, Ligutti J, Amagasu S, Liu D, Zou A, Min X, Wang Z, Ilch CP, Kornecook TJ, Lin MJ, Be X, Miranda LP, Moyer BD, Biswas K.

J Med Chem. 2018 Nov 8;61(21):9500-9512. doi: 10.1021/acs.jmedchem.8b00736. Epub 2018 Oct 22.

PMID:
30346167
5.

The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement.

La DS, Peterson EA, Bode C, Boezio AA, Bregman H, Chu-Moyer MY, Coats J, DiMauro EF, Dineen TA, Du B, Gao H, Graceffa R, Gunaydin H, Guzman-Perez A, Fremeau R Jr, Huang X, Ilch C, Kornecook TJ, Kreiman C, Ligutti J, Jasmine Lin MH, McDermott JS, Marx I, Matson DJ, McDonough SI, Moyer BD, Nho Nguyen H, Taborn K, Yu V, Weiss MM.

Bioorg Med Chem Lett. 2017 Aug 1;27(15):3477-3485. doi: 10.1016/j.bmcl.2017.05.070. Epub 2017 Jun 1.

PMID:
28629594
6.

Pharmacologic Characterization of AMG8379, a Potent and Selective Small Molecule Sulfonamide Antagonist of the Voltage-Gated Sodium Channel NaV1.7.

Kornecook TJ, Yin R, Altmann S, Be X, Berry V, Ilch CP, Jarosh M, Johnson D, Lee JH, Lehto SG, Ligutti J, Liu D, Luther J, Matson D, Ortuno D, Roberts J, Taborn K, Wang J, Weiss MM, Yu V, Zhu DXD, Fremeau RT Jr, Moyer BD.

J Pharmacol Exp Ther. 2017 Jul;362(1):146-160. doi: 10.1124/jpet.116.239590. Epub 2017 May 4.

PMID:
28473457
7.

Correction to "Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement".

Marx IE, Dineen TA, Able J, Bode C, Bregman H, Chu-Moyer M, DiMauro EF, Du B, Foti RS, Fremeau RT Jr, Gao H, Gunaydin H, Hall BE, Huang L, Kornecook T, Kreiman CR, La DS, Ligutti J, Lin MJ, Liu D, McDermott JS, Moyer BD, Nguyen HN, Peterson EA, Roberts JT, Rose P, Wang J, Youngblood BD, Yu V, Weiss MM.

ACS Med Chem Lett. 2017 Feb 28;8(3):378. doi: 10.1021/acsmedchemlett.7b00075. eCollection 2017 Mar 9.

8.

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity.

Graceffa RF, Boezio AA, Able J, Altmann S, Berry LM, Boezio C, Butler JR, Chu-Moyer M, Cooke M, DiMauro EF, Dineen TA, Feric Bojic E, Foti RS, Fremeau RT Jr, Guzman-Perez A, Gao H, Gunaydin H, Huang H, Huang L, Ilch C, Jarosh M, Kornecook T, Kreiman CR, La DS, Ligutti J, Milgram BC, Lin MJ, Marx IE, Nguyen HN, Peterson EA, Rescourio G, Roberts J, Schenkel L, Shimanovich R, Sparling BA, Stellwagen J, Taborn K, Vaida KR, Wang J, Yeoman J, Yu V, Zhu D, Moyer BD, Weiss MM.

J Med Chem. 2017 Jul 27;60(14):5990-6017. doi: 10.1021/acs.jmedchem.6b01850. Epub 2017 Apr 20.

PMID:
28324649
9.

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities.

Weiss MM, Dineen TA, Marx IE, Altmann S, Boezio A, Bregman H, Chu-Moyer M, DiMauro EF, Feric Bojic E, Foti RS, Gao H, Graceffa R, Gunaydin H, Guzman-Perez A, Huang H, Huang L, Jarosh M, Kornecook T, Kreiman CR, Ligutti J, La DS, Lin MJ, Liu D, Moyer BD, Nguyen HN, Peterson EA, Rose PE, Taborn K, Youngblood BD, Yu V, Fremeau RT Jr.

J Med Chem. 2017 Jul 27;60(14):5969-5989. doi: 10.1021/acs.jmedchem.6b01851. Epub 2017 Apr 20.

PMID:
28287723
10.

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement.

Marx IE, Dineen TA, Able J, Bode C, Bregman H, Chu-Moyer M, DiMauro EF, Du B, Foti RS, Fremeau RT Jr, Gao H, Gunaydin H, Hall BE, Huang L, Kornecook T, Kreiman CR, La DS, Ligutti J, Lin MJ, Liu D, McDermott JS, Moyer BD, Peterson EA, Roberts JT, Rose P, Wang J, Youngblood BD, Yu V, Weiss MM.

ACS Med Chem Lett. 2016 Sep 21;7(12):1062-1067. eCollection 2016 Dec 8. Erratum in: ACS Med Chem Lett. 2017 Feb 28;8(3):378.

11.

Discovery and hit-to-lead evaluation of piperazine amides as selective, state-dependent NaV1.7 inhibitors.

Sparling BA, Yi S, Able J, Bregman H, DiMauro EF, Foti RS, Gao H, Guzman-Perez A, Huang H, Jarosh M, Kornecook T, Ligutti J, Milgram BC, Moyer BD, Youngblood B, Yu VL, Weiss MM.

Medchemcomm. 2016 Dec 2;8(4):744-754. doi: 10.1039/c6md00578k. eCollection 2017 Apr 1.

12.

Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors.

DiMauro EF, Altmann S, Berry LM, Bregman H, Chakka N, Chu-Moyer M, Bojic EF, Foti RS, Fremeau R, Gao H, Gunaydin H, Guzman-Perez A, Hall BE, Huang H, Jarosh M, Kornecook T, Lee J, Ligutti J, Liu D, Moyer BD, Ortuno D, Rose PE, Schenkel LB, Taborn K, Wang J, Wang Y, Yu V, Weiss MM.

J Med Chem. 2016 Sep 8;59(17):7818-39. doi: 10.1021/acs.jmedchem.6b00425. Epub 2016 Aug 29.

PMID:
27441383
13.

Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).

Hu E, Chen N, Bourbeau MP, Harrington PE, Biswas K, Kunz RK, Andrews KL, Chmait S, Zhao X, Davis C, Ma J, Shi J, Lester-Zeiner D, Danao J, Able J, Cueva M, Talreja S, Kornecook T, Chen H, Porter A, Hungate R, Treanor J, Allen JR.

J Med Chem. 2014 Aug 14;57(15):6632-41. doi: 10.1021/jm500713j. Epub 2014 Aug 4.

PMID:
25062128
14.

MK-7128, a novel CB1 receptor inverse agonist, improves scopolamine-induced learning and memory deficits in mice.

Dillon GM, Lubbers LS, Ferguson MT, Lao JZ, Huang RR, Xiao JC, Fong TM, Hale JJ, Rupprecht K, Miao S, Rowe BA, Kornecook TJ, Dodart JC.

Behav Pharmacol. 2011 Apr;22(2):91-100. doi: 10.1097/FBP.0b013e3283423d7e.

PMID:
21301326
15.

Isoform-specific effects of apolipoprotein E on cognitive performance in targeted-replacement mice overexpressing human APP.

Kornecook TJ, McKinney AP, Ferguson MT, Dodart JC.

Genes Brain Behav. 2010 Mar 1;9(2):182-92. doi: 10.1111/j.1601-183X.2009.00545.x. Epub 2009 Oct 8.

16.

Prefrontal cortex lesions and scopolamine impair attention performance of C57BL/6 mice in a novel 2-choice visual discrimination task.

Dillon GM, Shelton D, McKinney AP, Caniga M, Marcus JN, Ferguson MT, Kornecook TJ, Dodart JC.

Behav Brain Res. 2009 Dec 1;204(1):67-76. doi: 10.1016/j.bbr.2009.04.036. Epub 2009 May 4.

PMID:
19416740
17.

Glucose increases hippocampal extracellular acetylcholine levels upon activation of septal GABA receptors.

Degroot A, Kornecook T, Quirion R, DeBow S, Parent MB.

Brain Res. 2003 Jul 25;979(1-2):71-7.

PMID:
12850573
18.

Alzheimer's disease and the basal forebrain cholinergic system: relations to beta-amyloid peptides, cognition, and treatment strategies.

Auld DS, Kornecook TJ, Bastianetto S, Quirion R.

Prog Neurobiol. 2002 Oct;68(3):209-45. Review.

PMID:
12450488
19.

Application of in vivo microdialysis to the study of cholinergic systems.

Day JC, Kornecook TJ, Quirion R.

Methods. 2001 Jan;23(1):21-39. Review.

PMID:
11162147
20.

Reversible lesions of the rhinal cortex produce delayed non-matching-to-sample deficits in rats.

Barnes SJ, Floresco SB, Kornecook TJ, Pinel JP.

Neuroreport. 2000 Feb 7;11(2):351-4.

PMID:
10674485
21.

Rhinal cortex, but not medial thalamic, lesions cause retrograde amnesia for objects in rats.

Kornecook TJ, Anzarut A, Pinel JP.

Neuroreport. 1999 Sep 9;10(13):2853-8.

PMID:
10511452
22.

Basal forebrain damage and object-recognition in rats.

Kornecook TJ, Kippin TE, Pinel JP.

Behav Brain Res. 1999 Jan;98(1):67-76.

PMID:
10210523
23.
24.

Object-recognition and spatial learning and memory in rats prenatally exposed to ethanol.

Kim CK, Kalynchuk LE, Kornecook TJ, Mumby DG, Dadgar NA, Pinel JP, Weinberg J.

Behav Neurosci. 1997 Oct;111(5):985-95.

PMID:
9383519
25.

Ischemia-induced object-recognition deficits in rats are attenuated by hippocampal ablation before or soon after ischemia.

Mumby DG, Wood ER, Duva CA, Kornecook TJ, Pinel JP, Phillips AG.

Behav Neurosci. 1996 Apr;110(2):266-81.

PMID:
8731053

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