Discovery and Characterization of VU0529331, a Synthetic Small-Molecule Activator of Homomeric G Protein-Gated, Inwardly Rectifying, Potassium (GIRK) Channels
Open accessAbstract
3.1-4 (GIRK1-4) subunits. Different subunit combinations are expressed throughout the central nervous system (CNS) and the periphery, and most of these combinations contain a GIRK1 subunit. For example, the predominance of GIRK channels in the CNS are composed of GIRK1 and GIRK2 subunits, while the GIRK channels in cardiac atrial myocytes are made up mostly of GIRK1 and GIRK4 subunits. Although the vast majority of GIRK channels contain a GIRK1 subunit, discrete populations of cells that express non-GIRK1-containing GIRK (non-GIRK1/X) channels do exist. For instance, dopaminergic neurons in the ventral tegmental area of the brain, associated with addiction and reward, do not express the GIRK1 subunit. Targeting these non-GIRK1/X channels with subunit-selective pharmacological probes could lead to important insights into how GIRK channels are involved in reward and addiction. Such insights may, in turn, reveal therapeutic opportunities for the treatment or prevention of addiction. Previously, our laboratory discovered small molecules that can specifically modulate the activity of GIRK1-containing GIRK channels. However, efforts to generate compounds active on non-GIRK1/X channels from these scaffolds have been unsuccessful. Recently, ivermectin was shown to modulate non-GIRK1/X channels, and historically, ivermectin is known to modulate a wide variety of neuronal channels and receptors. Further, ivermectin is a complex natural product, which makes it a challenging starting point for development of more selective, effective, and potent compounds. Thus, while ivermectin provides proof-of-concept as a non-GIRK1/X channel activator, it is of limited utility. Therefore, we sought to discover a synthetic small molecule that would serve as a starting point for the development of non-GIRK1/X channel modulators. To accomplish this, we used a high-throughput thallium flux assay to screen a 100 000-compound library in search of activators of homomeric GIRK2 channels. Using this approach, we discovered VU0529331, the first synthetic small molecule reported to activate non-GIRK1/X channels, to our knowledge. This discovery represents the first step toward developing potent and selective non-GIRK1/X channel probes. Such molecules will help elucidate the role of GIRK channels in addiction, potentially establishing a foundation for future development of therapies utilizing targeted GIRK channel modulation.
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In hippocampal and cortical circuits, GIRK-dependent inhibition supports forms of plasticity that require stable excitability set points, and selective perturbation of GIRK activity in CA1 pyramidal neurons disrupts learning.
“In hippocampal and cortical circuits, GIRK-dependent inhibition supports forms of plasticity that require stable excitability set points, and selective perturbation of GIRK activity in CA1 pyramidal neurons disrupts learning, highlighting its role in cognitive control [304,305,309].”
From Synaptic Plasticity—Intrinsic Excitability and Antidepressant Discovery (2026) · cites this paper as [309]
The Introduction (page not available in our copy) says GIRK channels inhibit cellular excitability and identifies memory as a process in which GIRK function is important. It does not establish that GIRK-dependent inhibition supports plasticity requiring stable excitability set points in hippocampal and cortical circuits, or that selectively perturbing GIRK activity in CA1 pyramidal neurons disrupts learning. (LLM, conf=0.83)
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Jeremic, D., Sanchez-Rodriguez, I., Jimenez-Diaz, L., & Navarro-Lopez, J. D. (2021) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2021.107808 · Cited by 89 · see citing works
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Synaptic Plasticity—Intrinsic Excitability and Antidepressant Discovery
Tanaka, M. (2026) · Biomedicines · doi:10.3390/biomedicines14061265
- Authors
- 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.
- Affiliations
- Vanderbilt University (US)
- University of Nebraska Medical Center (US)
- Corresponding author
- Weaver, C. David
- ORCID
- Venue
- ACS Chemical Neuroscience
- Publisher
- American Chemical Society (ACS)
- Published
- 2018-08-23
- Volume
- 10
- Issue
- 1
- Pages
- 358-370
- ISSN
- 1948-7193 (ISSN-L)
- PMC
- PMC6528656
- OpenAlex
- W2888113078
- Cited by
- 26
- References
- 81
- Citations by year
- 2026: 3 · 2025: 1 · 2024: 4 · 2023: 1 · 2022: 5 · 2021: 7 · 2020: 5
- FWCI
- 1.07
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- ACS Chemical Neuroscience (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- University of Nebraska Medical Center
- Pharmaceutical Research and Manufacturers of America Foundation
- National Institute of Mental Health (5 R21 MH099363)
- Vanderbilt Institute of Chemical Biology, Vanderbilt University
- Department of Pharmacology, Vanderbilt University
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion channel regulation and function
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
- Keywords
- GIRK channels, inwardly rectifying potassium channels, GIRK2, ivermectin, high-throughput screening, small molecule activators, addiction, reward, dopaminergic neurons, ventral tegmental area
- MeSH terms
- Dose-Response Relationship, Drug, Humans, Neurons, Pyrazines, Ion Channel Gating, G Protein-Coupled Inwardly-Rectifying Potassium Channels, Drug Discovery, HEK293 Cells
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
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