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Items: 1 to 50 of 118

1.

An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders.

Porter JD, Vivas O, Weaver CD, Alsafran A, DiMilo E, Arnold LA, Dickson EJ, Dockendorff C.

Bioorg Med Chem Lett. 2019 Dec 1;29(23):126681. doi: 10.1016/j.bmcl.2019.126681. Epub 2019 Sep 14.

PMID:
31668424
2.

Sign Inversion in Photopharmacology: Incorporation of Cyclic Azobenzenes in Photoswitchable Potassium Channel Blockers and Openers.

Trads JB, Hüll K, Matsuura BS, Laprell L, Fehrentz T, Görldt N, Kozek KA, Weaver CD, Klöcker N, Barber DM, Trauner D.

Angew Chem Int Ed Engl. 2019 Oct 21;58(43):15421-15428. doi: 10.1002/anie.201905790. Epub 2019 Sep 12. Review.

PMID:
31441199
3.

Functional Coupling of K+-Cl- Cotransporter (KCC) to GABA-Gated Cl- Channels in the Central Nervous System of Drosophila melanogaster Leads to Altered Drug Sensitivities.

Chen R, Prael FJ 3rd, Li Z, Delpire E, Weaver CD, Swale DR.

ACS Chem Neurosci. 2019 Jun 19;10(6):2765-2776. doi: 10.1021/acschemneuro.8b00697. Epub 2019 May 3.

PMID:
30942574
4.

VU0810464, a non-urea G protein-gated inwardly rectifying K+ (Kir 3/GIRK) channel activator, exhibits enhanced selectivity for neuronal Kir 3 channels and reduces stress-induced hyperthermia in mice.

Vo BN, Abney KK, Anderson A, Marron Fernandez de Velasco E, Benneyworth MA, Daniels JS, Morrison RD, Hopkins CR, Weaver CD, Wickman K.

Br J Pharmacol. 2019 Jul;176(13):2238-2249. doi: 10.1111/bph.14671. Epub 2019 May 30.

PMID:
30924523
5.

Correction to Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models.

Abney KK, Bubser M, Du Y, Kozek KA, Bridges TM, Lindsley CW, Daniels JS, Morrison RD, Wickman K, Hopkins CR, Jones CK, Weaver CD.

ACS Chem Neurosci. 2019 May 15;10(5):2621. doi: 10.1021/acschemneuro.9b00165. Epub 2019 Mar 26. No abstract available.

PMID:
30912639
6.

Use of chemical probes to explore the toxicological potential of the K+/Cl- cotransporter (KCC) as a novel insecticide target to control the primary vector of dengue and Zika virus, Aedes aegypti.

Prael FJ 3rd, Chen R, Li Z, Reed CW, Lindsley CW, Weaver CD, Swale DR.

Pestic Biochem Physiol. 2018 Oct;151:10-17. doi: 10.1016/j.pestbp.2018.03.019. Epub 2018 Apr 6.

7.

Label-Free Whole Cell Biosensing for High-Throughput Discovery of Activators and Inhibitors Targeting G Protein-Activated Inwardly Rectifying Potassium Channels.

Krebs KM, Pfeil EM, Simon K, Grundmann M, Häberlein F, Bautista-Aguilera OM, Gütschow M, Weaver CD, Fleischmann BK, Kostenis E.

ACS Omega. 2018 Nov 30;3(11):14814-14823. doi: 10.1021/acsomega.8b02254. Epub 2018 Nov 5.

8.

Direct activation of G-protein-gated inward rectifying K+ channels promotes nonrapid eye movement sleep.

Zou B, Cao WS, Guan Z, Xiao K, Pascual C, Xie J, Zhang J, Xie J, Kayser F, Lindsley CW, Weaver CD, Fang J, Xie XS.

Sleep. 2019 Mar 1;42(3). pii: zsy244. doi: 10.1093/sleep/zsy244.

PMID:
30535004
9.

Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models.

Abney KK, Bubser M, Du Y, Kozek KA, Bridges TM, Linsdley CW, Daniels JS, Morrison RD, Wickman K, Hopkins CR, Jones CK, Weaver CD.

ACS Chem Neurosci. 2019 Mar 20;10(3):1294-1299. doi: 10.1021/acschemneuro.8b00370. Epub 2018 Dec 11. Erratum in: ACS Chem Neurosci. 2019 May 15;10(5):2621.

10.

Discovery and Characterization of VU0529331, a Synthetic Small-Molecule Activator of Homomeric G Protein-Gated, Inwardly Rectifying, Potassium (GIRK) Channels.

Kozek KA, Du Y, Sharma S, Prael FJ 3rd, Spitznagel BD, Kharade SV, Denton JS, Hopkins CR, Weaver CD.

ACS Chem Neurosci. 2019 Jan 16;10(1):358-370. doi: 10.1021/acschemneuro.8b00287. Epub 2018 Sep 13.

PMID:
30136838
11.

Rhodol-based thallium sensors for cellular imaging of potassium channel activity.

Dutter BF, Ender A, Sulikowski GA, Weaver CD.

Org Biomol Chem. 2018 Aug 8;16(31):5575-5579. doi: 10.1039/c8ob01098f.

12.

Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992.

Kharade SV, Kurata H, Bender AM, Blobaum AL, Figueroa EE, Duran A, Kramer M, Days E, Vinson P, Flores D, Satlin LM, Meiler J, Weaver CD, Lindsley CW, Hopkins CR, Denton JS.

Mol Pharmacol. 2018 Aug;94(2):926-937. doi: 10.1124/mol.118.112359. Epub 2018 Jun 12.

13.

Selective Activation of N,N'-Diacyl Rhodamine Pro-fluorophores Paired with Releasing Enzyme, Porcine Liver Esterase (PLE).

Abney KK, Ramos-Hunter SJ, Romaine IM, Goodwin JS, Sulikowski GA, Weaver CD.

Chemistry. 2018 Jun 26;24(36):8985-8988. doi: 10.1002/chem.201801409. Epub 2018 May 25.

14.

Thallium Flux Assay for Measuring the Activity of Monovalent Cation Channels and Transporters.

Weaver CD.

Methods Mol Biol. 2018;1684:105-114. doi: 10.1007/978-1-4939-7362-0_9.

PMID:
29058187
15.

Identification and Characterization of the First Selective Y4 Receptor Positive Allosteric Modulator.

Schubert M, Stichel J, Du Y, Tough IR, Sliwoski G, Meiler J, Cox HM, Weaver CD, Beck-Sickinger AG.

J Med Chem. 2017 Sep 14;60(17):7605-7612. doi: 10.1021/acs.jmedchem.7b00976. Epub 2017 Aug 28.

PMID:
28795803
16.

Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators.

Wieting JM, Vadukoot AK, Sharma S, Abney KK, Bridges TM, Daniels JS, Morrison RD, Wickman K, Weaver CD, Hopkins CR.

ACS Chem Neurosci. 2017 Sep 20;8(9):1873-1879. doi: 10.1021/acschemneuro.7b00217. Epub 2017 Jul 19.

17.

GIRK2 splice variants and neuronal G protein-gated K+ channels: implications for channel function and behavior.

Marron Fernandez de Velasco E, Zhang L, N Vo B, Tipps M, Farris S, Xia Z, Anderson A, Carlblom N, Weaver CD, Dudek SM, Wickman K.

Sci Rep. 2017 May 9;7(1):1639. doi: 10.1038/s41598-017-01820-2.

18.

Screening for AMPA receptor auxiliary subunit specific modulators.

Azumaya CM, Days EL, Vinson PN, Stauffer S, Sulikowski G, Weaver CD, Nakagawa T.

PLoS One. 2017 Mar 30;12(3):e0174742. doi: 10.1371/journal.pone.0174742. eCollection 2017.

19.

Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Core.

Nance KD, Days EL, Weaver CD, Coldren A, Farmer TD, Cho HP, Niswender CM, Blobaum AL, Niswender KD, Lindsley CW.

J Med Chem. 2017 Feb 23;60(4):1611-1616. doi: 10.1021/acs.jmedchem.6b01706. Epub 2017 Feb 3.

PMID:
28103022
20.

Optical control of neuronal activity using a light-operated GIRK channel opener (LOGO).

Barber DM, Schönberger M, Burgstaller J, Levitz J, Weaver CD, Isacoff EY, Baier H, Trauner D.

Chem Sci. 2016;7(3):2347-2352. doi: 10.1039/C5SC04084A. Epub 2015 Nov 23.

21.

Challenges of Finding Novel Drugs Targeting the K-Cl Cotransporter.

Delpire E, Weaver CD.

ACS Chem Neurosci. 2016 Dec 21;7(12):1624-1627. Epub 2016 Nov 8.

22.

Optical control of GIRK channels using visible light.

Trads JB, Burgstaller J, Laprell L, Konrad DB, de la Osa de la Rosa L, Weaver CD, Baier H, Trauner D, Barber DM.

Org Biomol Chem. 2016 Dec 20;15(1):76-81.

PMID:
27901161
23.

Selective Small Molecule Activators of TREK-2 Channels Stimulate Dorsal Root Ganglion c-Fiber Nociceptor Two-Pore-Domain Potassium Channel Currents and Limit Calcium Influx.

Dadi PK, Vierra NC, Days E, Dickerson MT, Vinson PN, Weaver CD, Jacobson DA.

ACS Chem Neurosci. 2017 Mar 15;8(3):558-568. doi: 10.1021/acschemneuro.6b00301. Epub 2016 Nov 23.

24.

Inhibitors of 7-Dehydrocholesterol Reductase: Screening of a Collection of Pharmacologically Active Compounds in Neuro2a Cells.

Kim HY, Korade Z, Tallman KA, Liu W, Weaver CD, Mirnics K, Porter NA.

Chem Res Toxicol. 2016 May 16;29(5):892-900. doi: 10.1021/acs.chemrestox.6b00054. Epub 2016 Apr 28.

25.

GIRK Channels Modulate Opioid-Induced Motor Activity in a Cell Type- and Subunit-Dependent Manner.

Kotecki L, Hearing M, McCall NM, Marron Fernandez de Velasco E, Pravetoni M, Arora D, Victoria NC, Munoz MB, Xia Z, Slesinger PA, Weaver CD, Wickman K.

J Neurosci. 2015 May 6;35(18):7131-42. doi: 10.1523/JNEUROSCI.5051-14.2015.

26.

Development and validation of a thallium flux-based functional assay for the sodium channel NaV1.7 and its utility for lead discovery and compound profiling.

Du Y, Days E, Romaine I, Abney KK, Kaufmann K, Sulikowski G, Stauffer S, Lindsley CW, Weaver CD.

ACS Chem Neurosci. 2015 Jun 17;6(6):871-8. doi: 10.1021/acschemneuro.5b00004. Epub 2015 Apr 30.

PMID:
25879403
27.

The discovery and characterization of a centrally penetrant (ML396) and a peripherally restricted (ML397) pan-Group III mGlu positive allosteric modulators.

Jalan-Sakrikar N, Roper-Field J, Klar R, Mattman M, Walker AG, Zamorano R, Xiang Z, Byers CF, Blobaum AL, Engers D, Weaver CD, Days E, Utley TJ, Melancon B, Daniels JS, Wood MR, Lindsley CW, Conn PJ, Hopkins CR, Niswender CM.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2014 Apr 15 [updated 2015 Jan 16].

28.

Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM).

Morris LC, Nance KD, Gentry PR, Days EL, Weaver CD, Niswender CM, Thompson AD, Jones CK, Locuson CW, Morrison RD, Daniels JS, Niswender KD, Lindsley CW.

J Med Chem. 2014 Dec 11;57(23):10192-7. doi: 10.1021/jm501375c. Epub 2014 Dec 2.

29.

Controversies in ASSAY and drug development technologies: a focus on assessing irreproducibility.

Glickman JF, Lundbäck T, Napper AD, Niles WD, Simeonov A, Weaver CD, Yin HH, Zaman GJ, Osada H.

Assay Drug Dev Technol. 2014 Oct;12(8):443-51. doi: 10.1089/adt.2014.1501.

PMID:
25383720
30.

Discovery and characterization of a potent and selective inhibitor of Aedes aegypti inward rectifier potassium channels.

Raphemot R, Rouhier MF, Swale DR, Days E, Weaver CD, Lovell KM, Konkel LC, Engers DW, Bollinger SR, Hopkins C, Piermarini PM, Denton JS.

PLoS One. 2014 Nov 6;9(11):e110772. doi: 10.1371/journal.pone.0110772. eCollection 2014. Erratum in: PLoS One. 2015;10(3):e0119883. Bollinger, Sean F [corrected to Bollinger, Sean R].

31.

Cellular manganese content is developmentally regulated in human dopaminergic neurons.

Kumar KK, Lowe EW Jr, Aboud AA, Neely MD, Redha R, Bauer JA, Odak M, Weaver CD, Meiler J, Aschner M, Bowman AB.

Sci Rep. 2014 Oct 28;4:6801. doi: 10.1038/srep06801.

32.

Discovery of potent and selective GIRK1/2 modulators via 'molecular switches' within a series of 1-(3-cyclopropyl-1-phenyl-1H-pyrazol-5-yl)ureas.

Wen W, Wu W, Weaver CD, Lindsley CW.

Bioorg Med Chem Lett. 2014 Nov 1;24(21):5102-6. doi: 10.1016/j.bmcl.2014.08.061. Epub 2014 Sep 16.

PMID:
25264075
33.

Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor 7.

Jalan-Sakrikar N, Field JR, Klar R, Mattmann ME, Gregory KJ, Zamorano R, Engers DW, Bollinger SR, Weaver CD, Days EL, Lewis LM, Utley TJ, Hurtado M, Rigault D, Acher F, Walker AG, Melancon BJ, Wood MR, Lindsley CW, Conn PJ, Xiang Z, Hopkins CR, Niswender CM.

ACS Chem Neurosci. 2014 Dec 17;5(12):1221-37. doi: 10.1021/cn500153z. Epub 2014 Oct 9.

34.

Mechanisms underlying the activation of G-protein-gated inwardly rectifying K+ (GIRK) channels by the novel anxiolytic drug, ML297.

Wydeven N, Marron Fernandez de Velasco E, Du Y, Benneyworth MA, Hearing MC, Fischer RA, Thomas MJ, Weaver CD, Wickman K.

Proc Natl Acad Sci U S A. 2014 Jul 22;111(29):10755-60. doi: 10.1073/pnas.1405190111. Epub 2014 Jul 7.

35.

Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅).

Turlington M, Malosh C, Jacobs J, Manka JT, Noetzel MJ, Vinson PN, Jadhav S, Herman EJ, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Martín-Martín ML, Tong HM, López S, MacDonald GJ, Steckler T, Daniels JS, Weaver CD, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR.

J Med Chem. 2014 Jul 10;57(13):5620-37. doi: 10.1021/jm500259z. Epub 2014 Jun 25.

36.

A Duplexed High-Throughput Screen to Identify Allosteric Modulators of the Glucagon-Like Peptide 1 and Glucagon Receptors.

Morris LC, Days EL, Turney M, Mi D, Lindsley CW, Weaver CD, Niswender KD.

J Biomol Screen. 2014 Jul;19(6):847-58. doi: 10.1177/1087057114520971. Epub 2014 Feb 13.

37.

Development and validation of fluorescence-based and automated patch clamp-based functional assays for the inward rectifier potassium channel Kir4.1.

Raphemot R, Kadakia RJ, Olsen ML, Banerjee S, Days E, Smith SS, Weaver CD, Denton JS.

Assay Drug Dev Technol. 2013 Nov-Dec;11(9-10):532-43. doi: 10.1089/adt.2013.544. Epub 2013 Nov 22.

38.

N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement.

Gregory KJ, Herman EJ, Ramsey AJ, Hammond AS, Byun NE, Stauffer SR, Manka JT, Jadhav S, Bridges TM, Weaver CD, Niswender CM, Steckler T, Drinkenburg WH, Ahnaou A, Lavreysen H, Macdonald GJ, Bartolomé JM, Mackie C, Hrupka BJ, Caron MG, Daigle TL, Lindsley CW, Conn PJ, Jones CK.

J Pharmacol Exp Ther. 2013 Nov;347(2):438-57. doi: 10.1124/jpet.113.206623. Epub 2013 Aug 21.

39.

Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor.

Bartolomé-Nebreda JM, Conde-Ceide S, Delgado F, Iturrino L, Pastor J, Pena MÁ, Trabanco AA, Tresadern G, Wassvik CM, Stauffer SR, Jadhav S, Gogi K, Vinson PN, Noetzel MJ, Days E, Weaver CD, Lindsley CW, Niswender CM, Jones CK, Conn PJ, Rombouts F, Lavreysen H, Macdonald GJ, Mackie C, Steckler T.

J Med Chem. 2013 Sep 26;56(18):7243-59. doi: 10.1021/jm400650w. Epub 2013 Sep 4.

40.

Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators.

Ramos-Hunter SJ, Engers DW, Kaufmann K, Du Y, Lindsley CW, Weaver CD, Sulikowski GA.

Bioorg Med Chem Lett. 2013 Sep 15;23(18):5195-8. doi: 10.1016/j.bmcl.2013.07.002. Epub 2013 Jul 18.

41.

Discovery of 'molecular switches' within a GIRK activator scaffold that afford selective GIRK inhibitors.

Wen W, Wu W, Romaine IM, Kaufmann K, Du Y, Sulikowski GA, Weaver CD, Lindsley CW.

Bioorg Med Chem Lett. 2013 Aug 15;23(16):4562-6. doi: 10.1016/j.bmcl.2013.06.023. Epub 2013 Jun 20.

42.

Scaffold Hopping Affords a Highly Selective in vitro and in vivo T-Type Calcium Inhibitor Probe Free From IP Issues.

Xie X, Brogan JT, Schulte ML, Mi D, Yu H, Dawson ES, Li M, McManus O, Engers J, Lewis LM, Thompson A, Jones CK, Weaver CD, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Mar 31 [updated 2013 Mar 22].

43.

Discovery of a potent, selective and orally active in vivo mGlu4 positive allosteric modulator.

Hopkins CR, Engers DW, Niswender CM, Jones CK, Dawson E, Weaver CD, Daniels JS, Conn PJ, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Oct 29 [updated 2013 Mar 14].

44.

Development of the First Highly Selective mAChR 5 (M5) Positive Allosteric Modulator (PAM).

Bridges TM, Lewis LM, Weaver CD, Wood MR, Daniels JS, Conn PJ, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Aug 31 [updated 2013 Mar 14].

45.

Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity.

Bridges TM, Niswender CM, Jones CK, Lewis LM, Weaver CD, Wood MR, Daniels JS, Conn PJ, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Aug 31 [updated 2013 Mar 14].

46.

Discovery and Characterization of a Selective Activator of the G-Protein Activated Inward-Rectifying Potassium (GIRK) Channel.

Days E, Kaufmann K, Romaine I, Niswender C, Lewis M, Utley T, Du Y, Sliwoski G, Morrison R, Dawson ES, Engers JL, Denton J, Daniels JS, Sulikowski GA, Lindsley CW, Weaver CD.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Apr 6 [updated 2013 Mar 14].

47.

ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice.

Kaufmann K, Romaine I, Days E, Pascual C, Malik A, Yang L, Zou B, Du Y, Sliwoski G, Morrison RD, Denton J, Niswender CM, Daniels JS, Sulikowski GA, Xie XS, Lindsley CW, Weaver CD.

ACS Chem Neurosci. 2013 Sep 18;4(9):1278-86. doi: 10.1021/cn400062a. Epub 2013 Jun 13.

48.

High-throughput screening for small-molecule modulators of inward rectifier potassium channels.

Raphemot R, Weaver CD, Denton JS.

J Vis Exp. 2013 Jan 27;(71). pii: 4209. doi: 10.3791/4209.

49.

Benchmarking ligand-based virtual High-Throughput Screening with the PubChem database.

Butkiewicz M, Lowe EW Jr, Mueller R, Mendenhall JL, Teixeira PL, Weaver CD, Meiler J.

Molecules. 2013 Jan 8;18(1):735-56. doi: 10.3390/molecules18010735.

50.

Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold.

Rodriguez AL, Zhou Y, Williams R, Weaver CD, Vinson PN, Dawson ES, Steckler T, Lavreysen H, Mackie C, Bartolomé JM, Macdonald GJ, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7388-92. doi: 10.1016/j.bmcl.2012.10.068. Epub 2012 Oct 23.

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