• 3078 Citations
  • 31 h-Index
19992020

Research output per year

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Research Output

2017

A small-molecule inhibitor of TRPC5 ion channels suppresses progressive kidney disease in animal models

Zhou, Y., Castonguay, P., Sidhom, E. H., Clark, A. R., Dvela-Levitt, M., Kim, S., Sieber, J., Wieder, N., Jung, J. Y., Andreeva, S., Reichardt, J., Dubois, F., Hoffmann, S. C., Basgen, J. M., Montesinos, M. S., Weins, A., Johnson, A. C., Lander, E. S., Garrett, M. R., Hopkins, C. R. & 1 others, Greka, A., Dec 8 2017, In : Science. 358, 6368, p. 1332-1336 5 p.

Research output: Contribution to journalArticle

45 Scopus citations

CHAPTER 8: Muscarinic Receptors Allosteric Modulation

Melancon, B. J. & Hopkins, C. R., 2017, Allosterism in Drug Discovery. Doller, D. (ed.). 56 ed. Royal Society of Chemistry, p. 175-193 19 p. (RSC Drug Discovery Series; vol. 2017-January, no. 56).

Research output: Chapter in Book/Report/Conference proceedingChapter

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

Wieting, J. M., Vadukoot, A. K., Sharma, S., Abney, K. K., Bridges, T. M., Daniels, J. S., Morrison, R. D., Wickman, K., Weaver, C. D. & Hopkins, C. R., Sep 20 2017, In : ACS Chemical Neuroscience. 8, 9, p. 1873-1879 7 p.

Research output: Contribution to journalArticle

3 Scopus citations

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

Return of D4 Dopamine Receptor Antagonists in Drug Discovery

Lindsley, C. W. & Hopkins, C. R., 2017, In : Journal of Medicinal Chemistry. 60, 17, p. 7233-7243 11 p.

Research output: Contribution to journalReview article

17 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
2018

Discovery, characterization, and effects on renal fluid and electrolyte excretion of the Kir4.1 potassium channel pore blocker, VU0134992

Kharade, S. V., Kurata, H., Bender, A. M., Blobaum, A. L., Figueroa, E. E., Duran, A., Kramer, M., Days, E., Vinson, P., Flores, D., Satlin, L. M., Meiler, J., Weaver, C. D., Lindsley, C. W., Hopkins, C. R. & Denton, J. S., Aug 2018, In : Molecular pharmacology. 94, 2, p. 926-937 12 p.

Research output: Contribution to journalArticle

9 Scopus citations

Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu4 positive allosteric modulators that mitigate CYP1A2 induction liability

Engers, D. W., Bollinger, S. R., Engers, J. L., Panarese, J. D., Breiner, M. M., Gregro, A., Blobaum, A. L., Bronson, J. J., Wu, Y. J., Macor, J. E., Rodriguez, A. L., Zamorano, R., Conn, P. J., Lindsley, C. W., Niswender, C. M. & Hopkins, C. R., Aug 15 2018, In : Bioorganic and Medicinal Chemistry Letters. 28, 15, p. 2641-2646 6 p.

Research output: Contribution to journalArticle

3 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

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
2019

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

Abney, K. K., Bubser, M., Du, Y., Kozek, K. A., Bridges, T. M., Linsdley, C. W., Daniels, J. S., Morrison, R. D., Wickman, K., Hopkins, C. R., Jones, C. K. & Weaver, C. D., Mar 20 2019, In : ACS Chemical Neuroscience. 10, 3, p. 1294-1299 6 p.

Research output: Contribution to journalArticle

3 Scopus citations

Correction to: Analgesic effects of the GIRK activator, VU0466551, Alone and in combination with morphine in acute and persistent pain models (ACS Chemical Neuroscience (2019) 10:3 (1294-1299) DOI: 10.1021/acschemneuro.8b00370)

Abney, K. K., Bubser, M., Du, Y., Kozek, K. A., Bridges, T. M., Lindsley, C. W., Daniels, J. S., Morrison, R. D., Wickman, K., Hopkins, C. R., Jones, C. K. & Weaver, C. D., May 15 2019, In : ACS Chemical Neuroscience. 10, 5, p. 2621 1 p.

Research output: Contribution to journalComment/debate

Open Access
8 Scopus citations

Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu 4 )

Bollinger, S. R., Engers, D. W., Panarese, J. D., West, M., Engers, J. L., Loch, M. T., Rodriguez, A. L., Blobaum, A. L., Jones, C. K., Thompson Gray, A., Conn, P. J., Lindsley, C. W., Niswender, C. M. & Hopkins, C. R., Oct 1 2019, In : Journal of Medicinal Chemistry. 62, 1, p. 342-358 17 p.

Research output: Contribution to journalArticle

6 Scopus citations

Discovery, synthesis and characterization of a series of (1-alkyl-3-methyl-1H-pyrazol-5-yl)-2-(5-aryl-2H-tetrazol-2-yl)acetamides as novel GIRK1/2 potassium channel activators

Sharma, S., Kozek, K. A., Abney, K. K., Kumar, S., Gautam, N., Alnouti, Y., David Weaver, C. & Hopkins, C. R., Mar 15 2019, In : Bioorganic and Medicinal Chemistry Letters. 29, 6, p. 791-796 6 p.

Research output: Contribution to journalArticle

Discovery and Characterization of 2-Nitro-5-(4-(phenylsulfonyl)piperazin-1-yl)- N-(pyridin-4-ylmethyl)anilines as Novel Inhibitors of the Aedes aegypti Kir1 (AeKir1) Channel

Aretz, C. D., Morwitzer, M. J., Sanford, A. G., Hogan, A. M., Portillo, M. V., Kharade, S. V., Kramer, M., McCarthey, J. B., Trigueros, R. R., Piermarini, P. M., Denton, J. S. & Hopkins, C. R., Jun 14 2019, In : ACS infectious diseases. 5, 6, p. 917-931 15 p.

Research output: Contribution to journalArticle

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

Kozek, K. A., Du, Y., Sharma, S., Prael, F. J., Spitznagel, B. D., Kharade, S. V., Denton, J. S., Hopkins, C. R. & Weaver, C. D., Jan 16 2019, In : ACS Chemical Neuroscience. 10, 1, p. 358-370 13 p.

Research output: Contribution to journalArticle

3 Scopus citations
1 Scopus citations

Discovery of VU2957 (Valiglurax): An mGlu 4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease

Panarese, J. D., Engers, D. W., Wu, Y. J., Bronson, J. J., Macor, J. E., Chun, A., Rodriguez, A. L., Felts, A. S., Engers, J. L., Loch, M. T., Emmitte, K. A., Castelhano, A. L., Kates, M. J., Nader, M. A., Jones, C. K., Blobaum, A. L., Conn, P. J., Niswender, C. M., Hopkins, C. R. & Lindsley, C. W., Mar 14 2019, In : ACS Medicinal Chemistry Letters. 10, 3, p. 255-260 6 p.

Research output: Contribution to journalArticle

6 Scopus citations

Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases

Sharma, S. & Hopkins, C. R., Sep 12 2019, In : Journal of Medicinal Chemistry. 62, 17, p. 7589-7602 14 p.

Research output: Contribution to journalReview article

5 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

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
2020

Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors

Engers, D. W., Bollinger, S. R., Felts, A. S., Vadukoot, A. K., Williams, C. H., Blobaum, A. L., Lindsley, C. W., Hong, C. C. & Hopkins, C. R., Sep 15 2020, In : Bioorganic and Medicinal Chemistry Letters. 30, 18, 127418.

Research output: Contribution to journalArticle

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

Selective α7 nicotinic receptor agonists and positive allosteric modulators for the treatment of schizophrenia–a review

Antonio-Tolentino, K. & Hopkins, C. R., Jun 2 2020, In : Expert Opinion on Investigational Drugs. 29, 6, p. 603-610 8 p.

Research output: Contribution to journalReview article

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