The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.
TAK-242, an Antagonist for Toll-like Receptor 4, Protects against Acute Cerebral Ischemia/Reperfusion Injury in Mice
Open accessAbstract
Toll-like receptor 4 (TLR4) contributes to cerebral ischemia/reperfusion (I/R) injury and is a potential target for the treatment of ischemic stroke. This experiment is to evaluate the effect of an exogenous TLR4 antagonist, TAK-242, against acute cerebral I/R injury. A mouse model of cerebral I/R was induced by transient middle cerebral artery occlusion. TAK-242 (3 mg/kg body weight) was injected intraperitoneally 1 hour after ischemia. Our results showed that the concentration of TAK-242 in plasma increased to 52.0 ng/mL 3 hours after injection, was maintained at 54.1 ng/mL 8 hours after injection, and decreased to 22.6 ng/mL 24 hours after injection. The concentration of TAK-242 in brain tissue increased to 26.1 ng/mL in ischemic hemisphere and 14.2 ng/mL in nonischemic hemisphere 3 hours after injection, and was maintained at the similar levels 24 hours after injection. We found that TAK-242 significantly reduced cerebral infarction compared with vehicle control, improved neurologic function, inhibited the phosphorylation of downstream protein kinases in TLR4 signaling pathway, and downregulated the expression of inflammatory cytokines. We conclude that TAK-242 is able to cross blood-brain barrier, blocks TLR4 signaling, mediates the expression of inflammatory cytokines, and protects the brain from acute damage induced by I/R.
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A randomized, double-blind, placebo-controlled trial of TAK-242 for the treatment of severe sepsis*
Rice, T. W., Wheeler, A. P., Bernard, G. R., Vincent, J.-L., Angus, D. C., Aikawa, N., Demeyer, I., Sainati, S., Amlot, N., Cao, C., et al. (2010) · Critical Care Medicine · doi:10.1097/ccm.0b013e3181e7c5c9 · Cited by 512
Cited by
Toll-like Receptors in the Vascular System: Sensing the Dangers Within
Goulopoulou, S., McCarthy, C. G., & Webb, R. C. (2016) · Pharmacological Reviews · doi:10.1124/pr.114.010090 · Cited by 263
Cui, W., Sun, C., Ma, Y., Wang, S., Wang, X., & Zhang, Y. (2020) · Frontiers in Neuroscience · doi:10.3389/fnins.2020.00444 · Cited by 220
Zheng, Y., Zhang, X., Zhang, R., Wang, Z., Gan, J., Gao, Q., Yang, L., Xu, P., & Jiang, X. (2023) · International Journal of Molecular Medicine · doi:10.3892/ijmm.2023.5314 · Cited by 52
Zhou, C., Sun, X., Hu, Y., Song, J., Dong, S., Kong, D., Wang, Y., Hua, X., Han, J., Zhou, Y., et al. (2019) · Aging · doi:10.18632/aging.102260 · Cited by 50
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Metadata
- Authors
- Hua, F., Tang, H., Wang, J., Prunty, M. C., Hua, X., Sayeed, I., & Stein, D. G.
- Venue
- Journal of Cerebral Blood Flow & Metabolism
- Publisher
- SAGE Publications
- Published
- 2015-01-14
- Volume
- 35
- Issue
- 4
- Pages
- 536-542
- ISSN
- 0271-678X (ISSN-L)
- 1559-7016
- OpenAlex
- W2005695657
- Cited by
- 194
- References
- 1
- FWCI
- 8.60
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- CoChat. (2026). Citation check: TAK-242, an Antagonist for Toll-like Receptor 4, Protects against Acute Cerebral Ischemia/Reperfusion Injury in Mice. https://app.cochat.ai/papers/10.1038/jcbfm.2014.240
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- Hua, F., Tang, H., Wang, J., Prunty, M. C., Hua, X., Sayeed, I., & Stein, D. G. (2015). TAK-242, an Antagonist for Toll-like Receptor 4, Protects against Acute Cerebral Ischemia/Reperfusion Injury in Mice. Journal of Cerebral Blood Flow & Metabolism. https://doi.org/10.1038/jcbfm.2014.240
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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