• 3078 Citations
  • 31 h-Index
19992020

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Enantioselective synthesis of the AB-ring system of the antitumor antibiotic tetrazomine

Wipf, P. & Hopkins, C. R., May 4 2001, In : Journal of Organic Chemistry. 66, 9, p. 3133-3139 7 p.

Research output: Contribution to journalArticle

24 Scopus citations

Further exploration of M1 allosteric agonists: Subtle structural changes abolish M1 allosteric agonism and result in pan-mAChR orthosteric antagonism

Sheffler, D. J., Sevel, C., Le, U., Lovell, K. M., Tarr, J. C., Carrington, S. J. S., Cho, H. P., Digby, G. J., Niswender, C. M., Conn, P. J., Hopkins, C. R., Wood, M. R. & Lindsley, C. W., Jan 1 2013, In : Bioorganic and Medicinal Chemistry Letters. 23, 1, p. 223-227 5 p.

Research output: Contribution to journalArticle

10 Scopus citations

Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators

Bridges, T. M., Kennedy, J. P., Hopkins, C. R., Conn, P. J. & Lindsley, C. W., Oct 1 2010, In : Bioorganic and Medicinal Chemistry Letters. 20, 19, p. 5617-5622 6 p.

Research output: Contribution to journalArticle

22 Scopus citations

Identification and characterization of a compound that protects cardiac tissue from human Ether-à-go-go-related gene (hERG)-related drug-induced arrhythmias

Potet, F., Lorinc, A. N., Chaigne, S., Hopkins, C. R., Venkataraman, R., Stepanovic, S. Z., Lewis, L. M., Days, E., Sidorov, V. Y., Engers, D. W., Zou, B., Afshartous, D., George, A. L., Campbell, C. M., Balser, J. R., Li, M., Baudenbacher, F. J., Lindsley, C. W., Weaver, C. D. & Kupershmidt, S., Nov 16 2012, In : Journal of Biological Chemistry. 287, 47, p. 39613-39625 13 p.

Research output: Contribution to journalArticle

11 Scopus citations

Identification and characterization of ml352: A novel, noncompetitive inhibitor of the presynaptic choline transporter

Ennis, E. A., Wright, J., Retzlaff, C. L., McManus, O. B., Lin, Z., Huang, X., Wu, M., Li, M., Daniels, J. S., Lindsley, C. W., Hopkins, C. R. & Blakely, R. D., Mar 18 2015, In : ACS Chemical Neuroscience. 6, 3, p. 417-427 11 p.

Research output: Contribution to journalArticle

13 Scopus citations

Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1- tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K v7.1 (KCNQ1) potassium channel activator

Mattmann, M. E., Yu, H., Lin, Z., Xu, K., Huang, X., Long, S., Wu, M., McManus, O. B., Engers, D. W., Le, U. M., Li, M., Lindsley, C. W. & Hopkins, C. R., Sep 15 2012, In : Bioorganic and Medicinal Chemistry Letters. 22, 18, p. 5936-5941 6 p.

Research output: Contribution to journalArticle

28 Scopus citations

Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels

Miller, M., Shi, J., Zhu, Y., Kustov, M., Tian, J. B., Stevens, A., Wu, M., Xu, J., Long, S., Yang, P., Zholos V, A., Salovich, J. M., Weaver, C. D., Hopkins, C. R., Lindsley, C. W., McManus, O., Li, M. & Zhu, M. X., Sep 23 2011, In : Journal of Biological Chemistry. 286, 38, p. 33436-33446 11 p.

Research output: Contribution to journalArticle

117 Scopus citations

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, J. R., Klar, R., Mattmann, M. E., Gregory, K. J., Zamorano, R., Engers, D. W., Bollinger, S. R., Weaver, C. D., Days, E. L., Lewis, L. M., Utley, T. J., Hurtado, M., Rigault, D., Acher, F., Walker, A. G., Melancon, B. J., Wood, M. R., Lindsley, C. W., Conn, P. J. & 3 others, Xiang, Z., Hopkins, C. R. & Niswender, C. M., Dec 17 2014, In : ACS Chemical Neuroscience. 5, 12, p. 1221-1237 17 p.

Research output: Contribution to journalArticle

35 Scopus citations

Inhibition of BMP signaling suppresses metastasis in mammary cancer

Owens, P., Pickup, M. W., Novitskiy, S. V., Giltnane, J. M., Gorska, A. E., Hopkins, C. R., Hong, C. C. & Moses, H. L., May 7 2015, In : Oncogene. 34, 19, p. 2437-2449 13 p.

Research output: Contribution to journalArticle

55 Scopus citations

Inhibition of the TRPC5 ion channel protects the kidney filter

Schaldecker, T., Kim, S., Tarabanis, C., Tian, D., Hakroush, S., Castonguay, P., Ahn, W., Wallentin, H., Heid, H., Hopkins, C. R., Lindsley, C. W., Riccio, A., Buvall, L., Weins, A. & Greka, A., Dec 2 2013, In : Journal of Clinical Investigation. 123, 12, p. 5298-5309 12 p.

Research output: Contribution to journalArticle

96 Scopus citations

In vivo structure - Activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors

Hao, J., Ho, J. N., Lewis, J. A., Karim, K. A., Daniels, R. N., Gentry, P. R., Hopkins, C. R., Lindsley, C. W. & Hong, C. C., Feb 19 2010, In : ACS chemical biology. 5, 2, p. 245-253 9 p.

Research output: Contribution to journalArticle

241 Scopus citations

Inward rectifier potassium (Kir) channels in the soybean aphid Aphis glycines: Functional characterization, pharmacology, and toxicology

Piermarini, P. M., Inocente, E. A., Acosta, N., Hopkins, C. R., Denton, J. S. & Michel, A. P., Oct 2018, In : Journal of Insect Physiology. 110, p. 57-65 9 p.

Research output: Contribution to journalArticle

3 Scopus citations

Is there a path forward for mGlu2 positive allosteric modulators for the treatment of schizophrenia?

Hopkins, C. R., Feb 20 2013, In : ACS Chemical Neuroscience. 4, 2, p. 211-213 3 p.

Research output: Contribution to journalArticle

27 Scopus citations

Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators

Mueller, R., Dawson, E. S., Niswender, C. M., Butkiewicz, M., Hopkins, C. R., Weaver, C. D., Lindsley, C. W., Conn, P. J. & Meiler, J., Sep 2012, In : Journal of Molecular Modeling. 18, 9, p. 4437-4446 10 p.

Research output: Contribution to journalArticle

9 Scopus citations

KVA-D-88, a Novel Preferable Phosphodiesterase 4B Inhibitor, Decreases Cocaine-Mediated Reward Properties in Vivo

Burkovetskaya, M. E., Liu, Q., Vadukoot, A. K., Gautam, N., Alnouti, Y., Kumar, S., Miczek, K., Buch, S., Hopkins, C. R. & Guo, M., Aug 5 2020, In : ACS Chemical Neuroscience. 11, 15, p. 2231-2242 12 p.

Research output: Contribution to journalArticle

MGlu7 potentiation rescues cognitive, social, and respiratory phenotypes in a mouse model of Rett syndrome

Gogliotti, R. G., Senter, R. K., Fisher, N. M., Adams, J., Zamorano, R., Walker, A. G., Blobaum, A. L., Engers, D. W., Hopkins, C. R., Daniels, J. S., Jones, C. K., Lindsley, C. W., Xiang, Z., Conn, P. J. & Niswender, C. M., Aug 16 2017, In : Science translational medicine. 9, 403, eaai7459.

Research output: Contribution to journalArticle

Open Access
27 Scopus citations

ML418: The First Selective, Sub-Micromolar Pore Blocker of Kir7.1 Potassium Channels

Swale, D. R., Kurata, H., Kharade, S. V., Sheehan, J., Raphemot, R., Voigtritter, K. R., Figueroa, E. E., Meiler, J., Blobaum, A. L., Lindsley, C. W., Hopkins, C. R. & Denton, J. S., Jul 20 2016, In : ACS Chemical Neuroscience. 7, 7, p. 1013-1023 11 p.

Research output: Contribution to journalArticle

8 Scopus citations

"Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology

Wood, M. R., Hopkins, C. R., Brogan, J. T., Conn, P. J. & Lindsley, C. W., Apr 5 2011, In : Biochemistry. 50, 13, p. 2403-2410 8 p.

Research output: Contribution to journalArticle

125 Scopus citations

Novel pyrazinone inhibitors of mast cell tryptase: Synthesis and SAR evaluation

Hopkins, C., Neuenschwander, K., Scotese, A., Jackson, S., Nieduzak, T., Pauls, H., Liang, G., Sides, K., Cramer, D., Cairns, J., Maignan, S. & Mathieu, M., Oct 4 2004, In : Bioorganic and Medicinal Chemistry Letters. 14, 19, p. 4819-4823 5 p.

Research output: Contribution to journalArticle

28 Scopus citations

Pharmacological inhibition of inward rectifier potassium channels induces lethality in larval Aedes aegypti

Trigueros, R. R., Hopkins, C. R., Denton, J. S. & Piermarini, P. M., 2018, In : Insects. 9, 4, 163.

Research output: Contribution to journalArticle

1 Scopus citations

Pharmacological stimulation of metabotropic glutamate receptor type 4 in a rat model of Parkinson's disease and l-DOPA-induced dyskinesia: Comparison between a positive allosteric modulator and an orthosteric agonist

Iderberg, H., Maslava, N., Thompson, A. D., Bubser, M., Niswender, C. M., Hopkins, C. R., Lindsley, C. W., Conn, P. J., Jones, C. K. & Cenci, M. A., Aug 2015, In : Neuropharmacology. 95, p. 121-129 9 p., 5768.

Research output: Contribution to journalArticle

25 Scopus citations

Re-exploration of the PHCCC scaffold: Discovery of improved positive allosteric modulators of mGluR4

Williams, R., Zhou, Y., Niswender, C. M., Luo, Q., Conn, P. J., Lindsley, C. W. & Hopkins, C. R., Jun 16 2010, In : ACS Chemical Neuroscience. 1, 6, p. 411-419 9 p.

Research output: Contribution to journalArticle

41 Scopus citations

Reversible inhibitors of regulators of G-protein signaling identified in a high-throughput cell-based calcium signaling assay

Storaska, A. J., Mei, J. P., Wu, M., Li, M., Wade, S. M., Blazer, L. L., Sjögren, B., Hopkins, C. R., Lindsley, C. W., Lin, Z., Babcock, J. J., McManus, O. B. & Neubig, R. R., Dec 2013, In : Cellular Signalling. 25, 12, p. 2848-2855 8 p.

Research output: Contribution to journalArticle

17 Scopus citations

Selective inhibition of the K ir2 family of inward rectifier potassium channels by a small molecule probe: The discovery, SAR, and pharmacological characterization of ML133

Wang, H. R., Wu, M., Yu, H., Long, S., Stevens, A., Engers, D. W., Sackin, H., Daniels, J. S., Dawson, E. S., Hopkins, C. R., Lindsley, C. W., Li, M. & McManus, O. B., Aug 19 2011, In : ACS chemical biology. 6, 8, p. 845-856 12 p.

Research output: Contribution to journalArticle

48 Scopus citations

Separation of Cdc25 dual specificity phosphatase inhibition and DNA cleaving activities in a focused library of analogs of the antitumor antibiotic Dnacin

Wipf, P., Hopkins, C. R., Phillips, E. O. & Lazo, J. S., Aug 5 2002, In : Tetrahedron. 58, 32, p. 6367-6372 6 p.

Research output: Contribution to journalArticle

17 Scopus citations

Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu4

Cheung, Y. Y., Zamorano, R., Blobaum, A. L., Weaver, C. D., Conn, P. J., Lindsley, C. W., Niswender, C. M. & Hopkins, C. R., Mar 14 2011, In : ACS Combinatorial Science. 13, 2, p. 159-165 7 p.

Research output: Contribution to journalArticle

4 Scopus citations

Specific activin receptor-like kinase 3 inhibitors enhance liver regeneration

Tsugawa, D., Oya, Y., Masuzaki, R., Ray, K., Engers, D. W., Dib, M., Do, N., Kuramitsu, K., Ho, K., Frist, A., Yu, P. B., Bloch, K. D., Lindsley, C. W., Hopkins, C. R., Hong, C. C. & Karp, S. J., Dec 1 2014, In : Journal of Pharmacology and Experimental Therapeutics. 351, 3, p. 549-558 10 p.

Research output: Contribution to journalArticle

18 Scopus citations

Synthesis and characterization of a series of chiral alkoxymethyl morpholine analogs as dopamine receptor 4 (D4R) antagonists

Witt, J. O., McCollum, A. L., Hurtado, M. A., Huseman, E. D., Jeffries, D. E., Temple, K. J., Plumley, H. C., Blobaum, A. L., Lindsley, C. W. & Hopkins, C. R., May 1 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 10, p. 2481-2488 8 p.

Research output: Contribution to journalArticle

10 Scopus citations

Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs)

Engers, D. W., Niswender, C. M., Weaver, C. D., Jadhav, S., Menon, U. N., Zamorano, R., Conn, P. J., Lindsley, C. W. & Hopkins, C. R., Jul 23 2009, In : Journal of Medicinal Chemistry. 52, 14, p. 4115-4118 4 p.

Research output: Contribution to journalArticle

63 Scopus citations

Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu 4) antagonist: Unexpected 'molecular switch' from a closely related mGlu 4 positive allosteric modulator

Utley, T., Haddenham, D., Salovich, J. M., Zamorano, R., Vinson, P. N., Lindsley, C. W., Hopkins, C. R. & Niswender, C. M., Dec 1 2011, In : Bioorganic and Medicinal Chemistry Letters. 21, 23, p. 6955-6959 5 p.

Research output: Contribution to journalArticle

16 Scopus citations

Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4)

Williams, R., Johnson, K. A., Gentry, P. R., Niswender, C. M., Weaver, C. D., Conn, P. J., Lindsley, C. W. & Hopkins, C. R., Sep 1 2009, In : Bioorganic and Medicinal Chemistry Letters. 19, 17, p. 4967-4970 4 p.

Research output: Contribution to journalArticle

25 Scopus citations

Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu 4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)

Engers, D. W., Gentry, P. R., Williams, R., Bolinger, J. D., Weaver, C. D., Menon, U. N., Conn, P. J., Lindsley, C. W., Niswender, C. M. & Hopkins, C. R., Sep 1 2010, In : Bioorganic and Medicinal Chemistry Letters. 20, 17, p. 5175-5178 4 p.

Research output: Contribution to journalArticle

20 Scopus citations
47 Scopus citations

Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter

Bollinger, S. R., Engers, D. W., Ennis, E. A., Wright, J., Locuson, C. W., Lindsley, C. W., Blakely, R. D. & Hopkins, C. R., Apr 15 2015, In : Bioorganic and Medicinal Chemistry Letters. 25, 8, p. 1757-1760 4 p.

Research output: Contribution to journalArticle

3 Scopus citations

Synthesis of 1,3-diarylsubstituted indazoles utilizing a Suzuki cross-coupling/deprotection/N-arylation sequence

Salovich, J. M., Lindsley, C. W. & Hopkins, C. R., Jul 21 2010, In : Tetrahedron Letters. 51, 29, p. 3796-3799 4 p.

Research output: Contribution to journalArticle

18 Scopus citations

Synthesis of 6,7-disubstituted-5H-pyrrolo[2,3-b]pyrazines via palladium-catalyzed heteroannulation

Hopkins, C. R. & Collar, N., Mar 14 2005, In : Tetrahedron Letters. 46, 11, p. 1845-1848 4 p.

Research output: Contribution to journalArticle

12 Scopus citations

Targeting human Mas-related G protein-coupled receptor X1 to inhibit persistent pain

Li, Z., Tseng, P. Y., Tiwari, V., Xu, Q., He, S. Q., Wang, Y., Zheng, Q., Han, L., Wu, Z., Blobaum, A. L., Cui, Y., Tiwari, V., Sun, S., Cheng, Y., Huang-Lionnet, J. H. Y., Geng, Y., Xiao, B., Peng, J., Hopkins, C., Raja, S. N. & 2 others, Guan, Y. & Dong, X., Mar 7 2017, In : Proceedings of the National Academy of Sciences of the United States of America. 114, 10, p. E1996-E2005

Research output: Contribution to journalArticle

14 Scopus citations

The discovery and characterization of ML218: A novel, centrally active T-Type calcium channel inhibitor with robust effects in STN neurons and in a rodent model of Parkinson's disease

Xiang, Z., Thompson, A. D., Brogan, J. T., Schulte, M. L., Melancon, B. J., Mi, D., Lewis, L. M., Zou, B., Yang, L., Morrison, R., Santomango, T., Byers, F., Brewer, K., Aldrich, J. S., Yu, H., Dawson, E. S., Li, M., McManus, O., Jones, C. K., Daniels, J. S. & 5 others, Hopkins, C. R., Xie, X. S., Conn, P. J., Weaver, C. D. & Lindsley, C. W., Dec 21 2011, In : ACS Chemical Neuroscience. 2, 12, p. 730-742 13 p.

Research output: Contribution to journalArticle

49 Scopus citations

The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate

Panarese, J. D., Engers, D. W., Wu, Y. J., Guernon, J. M., Chun, A., Gregro, A. R., Bender, A. M., Capstick, R. A., Wieting, J. M., Bronson, J. J., Macor, J. E., Westphal, R., Soars, M., Engers, J. E., Felts, A. S., Rodriguez, A. L., Emmitte, K. A., Jones, C. K., Blobaum, A. L., Jeffrey Conn, P. & 3 others, Niswender, C. M., Hopkins, C. R. & Lindsley, C. W., Jan 15 2019, In : Bioorganic and Medicinal Chemistry Letters. 29, 2, p. 342-346 5 p.

Research output: Contribution to journalArticle

2 Scopus citations

The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease

Jones, C. K., Bubser, M., Thompson, A. D., Dickerson, J. W., Turle-Lorenzo, N., Amalric, M., Blobaum, A. L., Bridges, T. M., Morrison, R. D., Jadhav, S., Engers, D. W., Italiano, K., Bode, J., Daniels, J. S., Lindsley, C. W., Hopkins, C. R., Conn, P. J. & Niswender, C. M., Feb 2012, In : Journal of Pharmacology and Experimental Therapeutics. 340, 2, p. 404-421 18 p.

Research output: Contribution to journalArticle

74 Scopus citations

U000328, a novel ALK2/3 kinase inhibitor, represses hepcidin and significantly improves the phenotype of IRIDA

Belot, A., Gourbeyre, O., Fay, A., Palin, A., Besson-Fournier, C., Latour, C., Hopkins, C. R., Tidmarsh, G. F., Coppin, H., Roth, M. P., Ritter, M. R., Hong, C. C. & Meynard, D., Mar 1 2020, In : Haematologica. 105, 3

Research output: Contribution to journalArticle

Open Access
1 Scopus citations

Validation of an improved scale for rating L-DOPA-induced dyskinesia in the mouse and effects of specific dopamine receptor antagonists

Sebastianutto, I., Maslava, N., Hopkins, C. R. & Cenci, M. A., Dec 1 2016, In : Neurobiology of Disease. 96, p. 156-170 15 p.

Research output: Contribution to journalArticle

21 Scopus citations

VU0810464, a non-urea G protein-gated inwardly rectifying K+ (Kir3/GIRK) channel activator, exhibits enhanced selectivity for neuronal Kir3 channels and reduces stress-induced hyperthermia in mice

Vo, B. N., Abney, K. K., Anderson, A., Marron Fernandez de Velasco, E., Benneyworth, M. A., Daniels, J. S., Morrison, R. D., Hopkins, C. R., Weaver, C. D. & Wickman, K., Jul 2019, In : British Journal of Pharmacology. 176, 13, p. 2238-2249 12 p.

Research output: Contribution to journalArticle

1 Scopus citations