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Items: 1 to 50 of 66

1.

1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of NaV1.7 inhibition.

Boezio AA, Andrews K, Boezio C, Chu-Moyer M, Copeland KW, DiMauro EF, Foti RS, Fremeau RT Jr, Gao H, Geuns-Meyer S, Graceffa RF, Gunaydin H, Huang H, La DS, Ligutti J, Moyer BD, Peterson EA, Yu V, Weiss MM.

Bioorg Med Chem Lett. 2018 Jun 15;28(11):2103-2108. doi: 10.1016/j.bmcl.2018.04.035. Epub 2018 Apr 17.

PMID:
29709252
2.

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
3.

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.

4.

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
5.

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
6.

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.

7.

An Orally Available BACE1 Inhibitor That Affords Robust CNS Aβ Reduction without Cardiovascular Liabilities.

Cheng Y, Brown J, Judd TC, Lopez P, Qian W, Powers TS, Chen JJ, Bartberger MD, Chen K, Dunn RT 2nd, Epstein O, Fremeau RT Jr, Harried S, Hickman D, Hitchcock SA, Luo Y, Minatti AE, Patel VF, Vargas HM, Wahl RC, Weiss MM, Wen PH, White RD, Whittington DA, Zheng XM, Wood S.

ACS Med Chem Lett. 2014 Dec 29;6(2):210-5. doi: 10.1021/ml500458t. eCollection 2015 Feb 12.

8.

Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer's disease.

Chen JJ, Liu Q, Yuan C, Gore V, Lopez P, Ma V, Amegadzie A, Qian W, Judd TC, Minatti AE, Brown J, Cheng Y, Xue M, Zhong W, Dineen TA, Epstein O, Human J, Kreiman C, Marx I, Weiss MM, Hitchcock SA, Powers TS, Chen K, Wen PH, Whittington DA, Cheng AC, Bartberger MD, Hickman D, Werner JA, Vargas HM, Everds NE, Vonderfecht SL, Dunn RT 2nd, Wood S, Fremeau RT Jr, White RD, Patel VF.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):767-74. doi: 10.1016/j.bmcl.2014.12.092. Epub 2015 Jan 8.

PMID:
25613679
9.

Lead optimization and modulation of hERG activity in a series of aminooxazoline xanthene β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.

Epstein O, Bryan MC, Cheng AC, Derakhchan K, Dineen TA, Hickman D, Hua Z, Human JB, Kreiman C, Marx IE, Weiss MM, Wahl RC, Wen PH, Whittington DA, Wood S, Zheng XM, Fremeau RT Jr, White RD, Patel VF.

J Med Chem. 2014 Dec 11;57(23):9796-810. doi: 10.1021/jm501266w. Epub 2014 Nov 12.

PMID:
25389560
10.

Inhibitors of β-site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine (AMG-8718).

Dineen TA, Chen K, Cheng AC, Derakhchan K, Epstein O, Esmay J, Hickman D, Kreiman CE, Marx IE, Wahl RC, Wen PH, Weiss MM, Whittington DA, Wood S, Fremeau RT Jr, White RD, Patel VF.

J Med Chem. 2014 Dec 11;57(23):9811-31. doi: 10.1021/jm5012676. Epub 2014 Nov 14.

PMID:
25363711
11.

Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease.

Huang H, La DS, Cheng AC, Whittington DA, Patel VF, Chen K, Dineen TA, Epstein O, Graceffa R, Hickman D, Kiang YH, Louie S, Luo Y, Wahl RC, Wen PH, Wood S, Fremeau RT Jr.

J Med Chem. 2012 Nov 8;55(21):9156-69. doi: 10.1021/jm300598e. Epub 2012 Sep 11.

PMID:
22928914
12.

Chromenones as potent bradykinin B1 antagonists.

Bryan MC, Biswas K, Peterkin TA, Rzasa RM, Arik L, Lehto SG, Sun H, Hsieh FY, Xu C, Fremeau RT, Allen JR.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):619-22. doi: 10.1016/j.bmcl.2011.10.068. Epub 2011 Oct 28.

PMID:
22088753
13.

Discovery of potent, orally bioavailable phthalazinone bradykinin B1 receptor antagonists.

Biswas K, Peterkin TA, Bryan MC, Arik L, Lehto SG, Sun H, Hsieh FY, Xu C, Fremeau RT, Allen JR.

J Med Chem. 2011 Oct 27;54(20):7232-46. doi: 10.1021/jm200808v. Epub 2011 Sep 26.

PMID:
21902230
14.

From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1).

Cheng Y, Judd TC, Bartberger MD, Brown J, Chen K, Fremeau RT Jr, Hickman D, Hitchcock SA, Jordan B, Li V, Lopez P, Louie SW, Luo Y, Michelsen K, Nixey T, Powers TS, Rattan C, Sickmier EA, St Jean DJ Jr, Wahl RC, Wen PH, Wood S.

J Med Chem. 2011 Aug 25;54(16):5836-57. doi: 10.1021/jm200544q. Epub 2011 Jul 29.

PMID:
21707077
15.

Discovery of alpha-amidosulfones as potent and selective agonists of CB2: synthesis, SAR, and pharmacokinetic properties.

Marx IE, DiMauro EF, Cheng A, Emkey R, Hitchcock SA, Huang L, Huang MY, Human J, Lee JH, Li X, Martin MW, White RD, Fremeau RT Jr, Patel VF.

Bioorg Med Chem Lett. 2009 Jan 1;19(1):31-5. doi: 10.1016/j.bmcl.2008.11.026. Epub 2008 Nov 13.

PMID:
19062274
16.

Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists.

Cheng Y, Albrecht BK, Brown J, Buchanan JL, Buckner WH, DiMauro EF, Emkey R, Fremeau RT Jr, Harmange JC, Hoffman BJ, Huang L, Huang M, Lee JH, Lin FF, Martin MW, Nguyen HQ, Patel VF, Tomlinson SA, White RD, Xia X, Hitchcock SA.

J Med Chem. 2008 Aug 28;51(16):5019-34. doi: 10.1021/jm800463f. Epub 2008 Aug 5.

PMID:
18680277
17.

Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.

DiMauro EF, Buchanan JL, Cheng A, Emkey R, Hitchcock SA, Huang L, Huang MY, Janosky B, Lee JH, Li X, Martin MW, Tomlinson SA, White RD, Zheng XM, Patel VF, Fremeau RT Jr.

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4267-74. doi: 10.1016/j.bmcl.2008.06.096. Epub 2008 Jul 3. Erratum in: Bioorg Med Chem Lett. 2008 Sep 15;18(18):5156. Bioorg Med Chem Lett. 2009 Jan 1;19(1):284.

PMID:
18640038
18.

Vesicular glutamate transporter 1 is required for photoreceptor synaptic signaling but not for intrinsic visual functions.

Johnson J, Fremeau RT Jr, Duncan JL, Rentería RC, Yang H, Hua Z, Liu X, LaVail MM, Edwards RH, Copenhagen DR.

J Neurosci. 2007 Jul 4;27(27):7245-55.

19.

Distribution of vesicular glutamate transporters 1 and 2 in the rat spinal cord, with a note on the spinocervical tract.

Persson S, Boulland JL, Aspling M, Larsson M, Fremeau RT Jr, Edwards RH, Storm-Mathisen J, Chaudhry FA, Broman J.

J Comp Neurol. 2006 Aug 10;497(5):683-701.

PMID:
16786558
20.

Expression of the vesicular glutamate transporters during development indicates the widespread corelease of multiple neurotransmitters.

Boulland JL, Qureshi T, Seal RP, Rafiki A, Gundersen V, Bergersen LH, Fremeau RT Jr, Edwards RH, Storm-Mathisen J, Chaudhry FA.

J Comp Neurol. 2004 Dec 13;480(3):264-80.

PMID:
15515175
21.

Vesicular glutamate transporter 3 expression identifies glutamatergic amacrine cells in the rodent retina.

Johnson J, Sherry DM, Liu X, Fremeau RT Jr, Seal RP, Edwards RH, Copenhagen DR.

J Comp Neurol. 2004 Sep 27;477(4):386-98.

22.

Endocannabinoid-independent retrograde signaling at inhibitory synapses in layer 2/3 of neocortex: involvement of vesicular glutamate transporter 3.

Harkany T, Holmgren C, Härtig W, Qureshi T, Chaudhry FA, Storm-Mathisen J, Dobszay MB, Berghuis P, Schulte G, Sousa KM, Fremeau RT Jr, Edwards RH, Mackie K, Ernfors P, Zilberter Y.

J Neurosci. 2004 May 26;24(21):4978-88.

23.

Vesicular glutamate transporters 1 and 2 target to functionally distinct synaptic release sites.

Fremeau RT Jr, Kam K, Qureshi T, Johnson J, Copenhagen DR, Storm-Mathisen J, Chaudhry FA, Nicoll RA, Edwards RH.

Science. 2004 Jun 18;304(5678):1815-9. Epub 2004 Apr 29.

24.

VGLUTs define subsets of excitatory neurons and suggest novel roles for glutamate.

Fremeau RT Jr, Voglmaier S, Seal RP, Edwards RH.

Trends Neurosci. 2004 Feb;27(2):98-103. Review.

PMID:
15102489
25.

Localization of vesicular glutamate transporters and neuronal nitric oxide synthase in rat nucleus tractus solitarii.

Lin LH, Edwards RH, Fremeau RT, Fujiyama F, Kaneko T, Talman WT.

Neuroscience. 2004;123(1):247-55.

PMID:
14667459
26.
27.

The identification of vesicular glutamate transporter 3 suggests novel modes of signaling by glutamate.

Fremeau RT Jr, Burman J, Qureshi T, Tran CH, Proctor J, Johnson J, Zhang H, Sulzer D, Copenhagen DR, Storm-Mathisen J, Reimer RJ, Chaudhry FA, Edwards RH.

Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14488-93. Epub 2002 Oct 18.

28.

The expression of vesicular glutamate transporters defines two classes of excitatory synapse.

Fremeau RT Jr, Troyer MD, Pahner I, Nygaard GO, Tran CH, Reimer RJ, Bellocchio EE, Fortin D, Storm-Mathisen J, Edwards RH.

Neuron. 2001 Aug 2;31(2):247-60.

29.

The essence of excitation.

Reimer RJ, Fremeau RT Jr, Bellocchio EE, Edwards RH.

Curr Opin Cell Biol. 2001 Aug;13(4):417-21. Review.

PMID:
11454446
30.

Uptake of glutamate into synaptic vesicles by an inorganic phosphate transporter.

Bellocchio EE, Reimer RJ, Fremeau RT Jr, Edwards RH.

Science. 2000 Aug 11;289(5481):957-60.

31.
33.
34.

Components of a calmodulin-dependent protein kinase cascade. Molecular cloning, functional characterization and cellular localization of Ca2+/calmodulin-dependent protein kinase kinase beta.

Anderson KA, Means RL, Huang QH, Kemp BE, Goldstein EG, Selbert MA, Edelman AM, Fremeau RT, Means AR.

J Biol Chem. 1998 Nov 27;273(48):31880-9.

35.

In situ hybridization: identification of rare mRNAs in human tissues.

Wilson KH, Schambra UB, Smith MS, Page SO, Richardson CD, Fremeau RT, Schwinn DA.

Brain Res Brain Res Protoc. 1997 May;1(2):175-85.

PMID:
9385082
37.

A novel nonopioid action of enkephalins: competitive inhibition of the mammalian brain high affinity L-proline transporter.

Fremeau RT Jr, Velaz-Faircloth M, Miller JW, Henzi VA, Cohen SM, Nadler JV, Shafqat S, Blakely RD, Domin B.

Mol Pharmacol. 1996 Jun;49(6):1033-41.

PMID:
8649341
38.

Characterization and distribution of the neuronal glutamate transporter EAAC1 in rat brain.

Velaz-Faircloth M, McGraw TS, alandro MS, Fremeau RT Jr, Kilberg MS, Anderson KJ.

Am J Physiol. 1996 Jan;270(1 Pt 1):C67-75.

PMID:
8772431
39.

Human brain-specific L-proline transporter: molecular cloning, functional expression, and chromosomal localization of the gene in human and mouse genomes.

Shafqat S, Velaz-Faircloth M, Henzi VA, Whitney KD, Yang-Feng TL, Seldin MF, Fremeau RT Jr.

Mol Pharmacol. 1995 Aug;48(2):219-29.

PMID:
7651355
40.

Mammalian brain-specific L-proline transporter. Neuronal localization of mRNA and enrichment of transporter protein in synaptic plasma membranes.

Velaz-Faircloth M, Guadaño-Ferraz A, Henzi VA, Fremeau RT Jr.

J Biol Chem. 1995 Jun 30;270(26):15755-61.

41.

Distribution of beta 3-adrenoceptor mRNA in human tissues.

Berkowitz DE, Nardone NA, Smiley RM, Price DT, Kreutter DK, Fremeau RT, Schwinn DA.

Eur J Pharmacol. 1995 Apr 28;289(2):223-8.

PMID:
7621895
42.

Ontogeny of D1A and D2 dopamine receptor subtypes in rat brain using in situ hybridization and receptor binding.

Schambra UB, Duncan GE, Breese GR, Fornaretto MG, Caron MG, Fremeau RT Jr.

Neuroscience. 1994 Sep;62(1):65-85.

PMID:
7816213
44.

Distribution of alpha 2-adrenergic receptor subtype gene expression in rat brain.

Scheinin M, Lomasney JW, Hayden-Hixson DM, Schambra UB, Caron MG, Lefkowitz RJ, Fremeau RT Jr.

Brain Res Mol Brain Res. 1994 Jan;21(1-2):133-49.

PMID:
8164514
45.

Molecular characterization of neurotransmitter transporters.

Shafqat S, Velaz-Faircloth M, Guadaño-Ferraz A, Fremeau RT Jr.

Mol Endocrinol. 1993 Dec;7(12):1517-29. Review. No abstract available.

PMID:
7908408
46.

D1 dopamine receptor binding and mRNA levels are not altered after neonatal 6-hydroxydopamine treatment: evidence against dopamine-mediated induction of D1 dopamine receptors during postnatal development.

Duncan GE, Breese GR, Criswell HE, Johnson KB, Schambra UB, Mueller RA, Caron MG, Fremeau RT Jr.

J Neurochem. 1993 Oct;61(4):1255-62.

PMID:
8376983
47.

Cloning and expression of a novel Na(+)-dependent neutral amino acid transporter structurally related to mammalian Na+/glutamate cotransporters.

Shafqat S, Tamarappoo BK, Kilberg MS, Puranam RS, McNamara JO, Guadaño-Ferraz A, Fremeau RT Jr.

J Biol Chem. 1993 Jul 25;268(21):15351-5.

48.

Identification, characterization, and molecular cloning of a novel transporter-like protein localized to the central nervous system.

Gingrich JA, Andersen PH, Tiberi M, el Mestikawy S, Jorgensen PN, Fremeau RT Jr, Caron MG.

FEBS Lett. 1992 Nov 9;312(2-3):115-22.

49.
50.

Location and molecular cloning of D1 dopamine receptor.

Gingrich JA, Dearry A, Falardeau P, Bates MD, Fremeau RT Jr, Caron MG.

Neurochem Int. 1992 Mar;20 Suppl:9S-15S.

PMID:
1365464

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