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19992019
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Research Output 1999 2019

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Article
2019
1 Citation (Scopus)

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

Acute Pain
Opioid Receptors
Morphine
Analgesics
G Protein-Coupled Inwardly-Rectifying Potassium Channels
5 Citations (Scopus)
Transient Receptor Potential Channels
Amines
Chronic Renal Insufficiency
Podocytes
Scaffolds
5 Citations (Scopus)

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

Cytochrome P-450 CYP1A2
Structure-Activity Relationship
Catalepsy
Haloperidol
Parkinson Disease

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

G Protein-Coupled Inwardly-Rectifying Potassium Channels
Acetamides
Inwardly Rectifying Potassium Channel
Potassium Channels
GTP-Binding Proteins

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

Aedes
Culicidae
Malpighian Tubules
Dengue
Ion Channels

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

G Protein-Coupled Inwardly-Rectifying Potassium Channels
Inwardly Rectifying Potassium Channel
Ivermectin
GTP-Binding Proteins
Molecules
Loop of Henle
Pharmaceutical Chemistry
Potassium Channels
Diuretics
Potassium
5 Citations (Scopus)

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

Pulse amplitude modulation
Toxicology
Modulators
Parkinson Disease
Pharmacology
2 Citations (Scopus)

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

Modulators

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

Induced Hyperthermia
Nervous System Diseases
GTP-Binding Proteins
Inwardly Rectifying Potassium Channel
Electrophysiology
2018
4 Citations (Scopus)

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

Potassium Channel Blockers
Electrolytes
Electrophysiology
Kidney
Stria Vascularis
3 Citations (Scopus)

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

Cytochrome P-450 CYP1A2
Scaffolds
Modulators
Amines
Chemical activation
2 Citations (Scopus)

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

Inwardly Rectifying Potassium Channel
Aphis glycines
Aphids
potassium channels
toxicology
1 Citation (Scopus)

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., Jan 1 2018, In : Insects. 9, 4, 163.

Research output: Contribution to journalArticle

potassium channels
Aedes aegypti
Culicidae
osmolality
mannitol
2017
35 Citations (Scopus)

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

Focal Segmental Glomerulosclerosis
Kidney Diseases
Ion Channels
Podocytes
Animal Models
1 Citation (Scopus)

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

Benzeneacetamides
G Protein-Coupled Inwardly-Rectifying Potassium Channels
Pharmacokinetics
Potassium Channels
Physiological Phenomena
22 Citations (Scopus)

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
Rett Syndrome
Phenotype
Long-Term Potentiation
Methyl-CpG-Binding Protein 2
Hippocampus
11 Citations (Scopus)

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

G-Protein-Coupled Receptors
Pain
Nociceptors
Aptitude
Peripheral Nervous System
2016
27 Citations (Scopus)

An insecticide resistance-breaking mosquitocide targeting inward rectifier potassium channels in vectors of Zika virus and malaria

Swale, D. R., Engers, D. W., Bollinger, S. R., Gross, A., Inocente, E. A., Days, E., Kanga, F., Johnson, R. M., Yang, L., Bloomquist, J. R., Hopkins, C. R., Piermarini, P. M. & Denton, J. S., Nov 16 2016, In : Scientific reports. 6, 36954.

Research output: Contribution to journalArticle

Insecticide Resistance
Inwardly Rectifying Potassium Channel
Culicidae
Malaria
Insecticides
13 Citations (Scopus)

Bone morphogenetic protein signaling promotes tumorigenesis in a murine model of high-grade glioma

Hover, L. D., Owens, P., Munden, A. L., Wang, J., Chambless, L. B., Hopkins, C. R., Hong, C. C., Moses, H. L. & Abel, T. W., Jul 1 2016, In : Neuro-Oncology. 18, 7, p. 928-938 11 p.

Research output: Contribution to journalArticle

Bone Morphogenetic Proteins
Glioma
Carcinogenesis
Astrocytes
Type I Bone Morphogenetic Protein Receptors
26 Citations (Scopus)

Development and Antiparkinsonian Activity of VU0418506, a Selective Positive Allosteric Modulator of Metabotropic Glutamate Receptor 4 Homomers without Activity at mGlu2/4 Heteromers

Niswender, C. M., Jones, C. K., Lin, X., Bubser, M., Thompson Gray, A., Blobaum, A. L., Engers, D. W., Rodriguez, A. L., Loch, M. T., Daniels, J. S., Lindsley, C. W., Hopkins, C. R., Javitch, J. A. & Conn, P. J., Sep 21 2016, In : ACS Chemical Neuroscience. 7, 9, p. 1201-1211 11 p.

Research output: Contribution to journalArticle

Antiparkinson Agents
Modulators
Pulse amplitude modulation
Parkinson Disease
Glutamic Acid
2 Citations (Scopus)

Discovery, characterization and biological evaluation of a novel (R)-4,4-difluoropiperidine scaffold as dopamine receptor 4 (D4R) antagonists

Jeffries, D. E., Witt, J. O., McCollum, A. L., Temple, K. J., Hurtado, M. A., Harp, J. M., Blobaum, A. L., Lindsley, C. W. & Hopkins, C. R., Jan 1 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 23, p. 5757-5764 8 p.

Research output: Contribution to journalArticle

Dopamine Antagonists
Dopamine Receptors
Scaffolds
X-Rays
Enantiomers
20 Citations (Scopus)

Discovery, Synthesis, and Preclinical Characterization of N-(3-Chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506), a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu4)

Engers, D. W., Blobaum, A. L., Gogliotti, R. D., Cheung, Y. Y., Salovich, J. M., Garcia-Barrantes, P. M., Daniels, J. S., Morrison, R., Jones, C. K., Soars, M. G., Zhuo, X., Hurley, J., Macor, J. E., Bronson, J. J., Conn, P. J., Lindsley, C. W., Niswender, C. M. & Hopkins, C. R., Sep 21 2016, In : ACS Chemical Neuroscience. 7, 9, p. 1192-1200 9 p.

Research output: Contribution to journalArticle

Modulators
Amines
Pharmacokinetics
Scaffolds
Amides
4 Citations (Scopus)

Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4)

Gogliotti, R. D., Blobaum, A. L., Morrison, R. M., Daniels, J. S., Salovich, J. M., Cheung, Y. Y., Rodriguez, A. L., Loch, M. T., Conn, P. J., Lindsley, C. W., Niswender, C. M. & Hopkins, C. R., Jul 1 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 13, p. 2984-2987 4 p.

Research output: Contribution to journalArticle

Pyrroles
Modulators
Pulse amplitude modulation
Sulfones
Sulfonamides
17 Citations (Scopus)

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core

Wood, M. R., Noetzel, M. J., Engers, J. L., Bollinger, K. A., Melancon, B. J., Tarr, J. C., Han, C., West, M., Gregro, A. R., Lamsal, A., Chang, S., Ajmera, S., Smith, E., Chase, P., Hodder, P. S., Bubser, M., Jones, C. K., Hopkins, C. R., Emmitte, K. A., Niswender, C. M. & 5 others, Wood, M. W., Duggan, M. E., Conn, P. J., Bridges, T. M. & Lindsley, C. W., Jul 1 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 13, p. 3029-3033 5 p.

Research output: Contribution to journalArticle

Modulators
Rats
Brain
Muscarinic Receptors
Plasmas
1 Citation (Scopus)

Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy

Gogliotti, R. D., Engers, D. W., Garcia-Barrantes, P. M., Panarese, J. D., Gentry, P. R., Blobaum, A. L., Morrison, R. D., Daniels, J. S., Thompson, A. D., Jones, C. K., Conn, P. J., Niswender, C. M., Lindsley, C. W. & Hopkins, C. R., Jun 15 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 12, p. 2915-2919 5 p.

Research output: Contribution to journalArticle

Pulse amplitude modulation
Metabotropic Glutamate Receptors
Modulators
Catalepsy
Haloperidol
7 Citations (Scopus)

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

Potassium Channels
Physiology
Microsomes
Brain
Potassium
10 Citations (Scopus)

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

Dopamine Receptors
Dopamine D4 Receptors
Dopamine Antagonists
Structure-Activity Relationship
morpholine
17 Citations (Scopus)

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

Dopamine Antagonists
Dyskinesias
3-((4-(4-chlorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo(2,3-b)pyridine
Raclopride
Medial Forebrain Bundle
2015
19 Citations (Scopus)

Activation of metabotropic glutamate receptor 7 is required for induction of long-term potentiation at SCCA1 synapses in the hippocampus

Klar, R., Walker, A. G., Ghose, D., Grueter, B. A., Engers, D. W., Hopkins, C. R., Lindsley, C. W., Xiang, Z., Conn, P. J. & Niswender, C. M., May 13 2015, In : Journal of Neuroscience. 35, 19, p. 7600-7615 16 p.

Research output: Contribution to journalArticle

Long-Term Potentiation
Synapses
Hippocampus
Metabotropic Glutamate Receptors
Excitatory Amino Acid Agonists
2 Citations (Scopus)

Discovery and characterization of 2-(cyclopropanesulfonamido)-n-(2-ethoxyphenyl)benzamide, ML382: A potent and selective positive allosteric modulator of MrgX1

Wen, W., Wang, Y., Li, Z., Tseng, P. Y., McManus, O. B., Wu, M., Li, M., Lindsley, C. W., Dong, X. & Hopkins, C. R., Jan 2015, In : ChemMedChem. 10, 1, p. 57-61 5 p.

Research output: Contribution to journalArticle

Chronic Pain
Modulators
Structure-Activity Relationship
G-Protein-Coupled Receptors
Chemical activation
10 Citations (Scopus)

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

Choline
Cholinergic Agents
Hemicholinium 3
Norepinephrine Plasma Membrane Transport Proteins
Serotonin Plasma Membrane Transport Proteins
52 Citations (Scopus)

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

Bone Morphogenetic Proteins
Breast Neoplasms
Neoplasm Metastasis
Tumor Microenvironment
Neoplasms
22 Citations (Scopus)

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

Dyskinesias
Parkinson Disease
Pharmacology
Catalepsy
Aptitude
3 Citations (Scopus)

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

Benzamides
Lead compounds
Pharmaceutical Chemistry
Structure-Activity Relationship
Scaffolds
2014
29 Citations (Scopus)

Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics

Cho, H. P., Garcia-Barrantes, P. M., Brogan, J. T., Hopkins, C. R., Niswender, C. M., Rodriguez, A. L., Venable, D. F., Morrison, R. D., Bubser, M., Daniels, J. S., Jones, C. K., Conn, P. J. & Lindsley, C. W., Oct 17 2014, In : ACS Chemical Biology. 9, 10, p. 2334-2346 13 p.

Research output: Contribution to journalArticle

Modulators
Schizophrenia
Pulse amplitude modulation
Modulation
Mutation
26 Citations (Scopus)

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

Raphemot, R., Rouhier, M. F., Swale, D. R., Days, E., Weaver, C. D., Lovell, K. M., Konkel, L. C., Engers, D. W., Bollinger, S. F., Hopkins, C., Piermarini, P. M. & Denton, J. S., Nov 6 2014, In : PloS one. 9, 11, 110772.

Research output: Contribution to journalArticle

Inwardly Rectifying Potassium Channel
Aedes
potassium channels
Insecticides
Aedes aegypti
9 Citations (Scopus)

Discovery and characterization of ML398, a potent and selective antagonist of the D4 receptor with in vivo activity

Berry, C. B., Bubser, M., Jones, C. K., Hayes, J. P., Wepy, J. A., Locuson, C. W., Daniels, J. S., Lindsley, C. W. & Hopkins, C. R., Sep 11 2014, In : ACS Medicinal Chemistry Letters. 5, 9, p. 1060-1064 5 p.

Research output: Contribution to journalArticle

Dopamine Antagonists
Dopamine Receptors
Dopamine
Structure-Activity Relationship
Cocaine
28 Citations (Scopus)

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

Modulators
Synapses
Autistic Disorder
Nervous System Diseases
Polymorphism
16 Citations (Scopus)

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

Type I Bone Morphogenetic Protein Receptors
Liver Regeneration
Bone Morphogenetic Proteins
Bone Morphogenetic Protein Receptors
Hepatectomy
2013
22 Citations (Scopus)

Discovery of a selective M4 positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: Development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia

Le, U., Melancon, B. J., Bridges, T. M., Vinson, P. N., Utley, T. J., Lamsal, A., Rodriguez, A. L., Venable, D., Sheffler, D. J., Jones, C. K., Blobaum, A. L., Wood, M. R., Daniels, J. S., Conn, P. J., Niswender, C. M., Lindsley, C. W. & Hopkins, C. R., Jan 1 2013, In : Bioorganic and Medicinal Chemistry Letters. 23, 1, p. 346-350 5 p.

Research output: Contribution to journalArticle

Muscarinic Receptors
Scaffolds (biology)
Modulators
Rats
Brain
33 Citations (Scopus)

Dynamic subunit stoichiometry confers a progressive continuum of pharmacological sensitivity by KCNQ potassium channels

Yu, H., Lin, Z., Mattmann, M. E., Zou, B., Terrenoire, C., Zhang, H., Wu, M., McManus, O. B., Kass, R. S., Lindsley, C. W., Hopkins, C. R. & Li, M., May 21 2013, In : Proceedings of the National Academy of Sciences of the United States of America. 110, 21, p. 8732-8737 6 p.

Research output: Contribution to journalArticle

KCNQ Potassium Channels
KCNQ1 Potassium Channel
Pharmacology
Cardiac Myocytes
Voltage-Gated Potassium Channels
40 Citations (Scopus)

Eliciting Renal Failure in Mosquitoes with a Small-Molecule Inhibitor of Inward-Rectifying Potassium Channels

Raphemot, R., Rouhier, M. F., Hopkins, C. R., Gogliotti, R. D., Lovell, K. M., Hine, R. M., Ghosalkar, D., Longo, A., Beyenbach, K. W., Denton, J. S. & Piermarini, P. M., May 29 2013, In : PloS one. 8, 5, e64905.

Research output: Contribution to journalArticle

Potassium Channels
potassium channels
renal failure
Insecticides
Culicidae
10 Citations (Scopus)

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

Allosteric Site
Ligands
Scaffolds
Chemical activation
Binding Sites
87 Citations (Scopus)

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

Podocytes
Albuminuria
Ion Channels
rac1 GTP-Binding Protein
Kidney Glomerulus
27 Citations (Scopus)

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

Modulators
Schizophrenia
Safety
Research
Therapeutics
16 Citations (Scopus)

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 1 2013, In : Cellular Signalling. 25, 12, p. 2848-2855 8 p.

Research output: Contribution to journalArticle

RGS Proteins
GTP-Binding Protein Regulators
Calcium Signaling
GTP-Binding Proteins
Muscarinic M3 Receptors
43 Citations (Scopus)
Bone Morphogenetic Protein Receptors
Molecular Probes
Structure-Activity Relationship
Scaffolds
Molecules
2012
15 Citations (Scopus)
Acetamides
Libraries
Hydrogen
Pharmacology
Brain
27 Citations (Scopus)

Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor

Salovich, J. M., Vinson, P. N., Sheffler, D. J., Lamsal, A., Utley, T. J., Blobaum, A. L., Bridges, T. M., Le, U., Jones, C. K., Wood, M. R., Scott Daniels, J., Jeffrey Conn, P., Niswender, C. M., Lindsley, C. W. & Hopkins, C. R., Aug 1 2012, In : Bioorganic and Medicinal Chemistry Letters. 22, 15, p. 5084-5088 5 p.

Research output: Contribution to journalArticle

Muscarinic Receptors
Cholinergic Agents
Modulators
Brain
Rats