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Page 1
Senicapoc: Repurposing a Drug to Target Microglia K(Ca)3.1 in Stroke.
Staal RGW, Weinstein JR, Nattini M, Cajina M, Chandresana G, Möller T. Staal RGW, et al. Neurochem Res. 2017 Sep;42(9):2639-2645. doi: 10.1007/s11064-017-2223-y. Epub 2017 Mar 31. Neurochem Res. 2017. PMID: 28364331 Free PMC article. Review.
Here we describe the potential of repurposing Senicapoc, a K(Ca)3.1 inhibitor, to intervene in the inflammation cascade that follows ischemia/reperfusion....
Here we describe the potential of repurposing Senicapoc, a K(Ca)3.1 inhibitor, to intervene in the inflammation cascade that follows …
Senicapoc treatment in COVID-19 patients with severe respiratory insufficiency-A randomized, open-label, phase II trial.
Granfeldt A, Andersen LW, Vallentin MF, Hilberg O, Hasselstrøm JB, Sørensen LK, Mogensen S, Christensen S, Grejs AM, Rasmussen BS, Kristiansen KT, Strøm T, Johansen IS, Schjørring OL, Simonsen U. Granfeldt A, et al. Acta Anaesthesiol Scand. 2022 Aug;66(7):838-846. doi: 10.1111/aas.14072. Epub 2022 May 13. Acta Anaesthesiol Scand. 2022. PMID: 35403225 Free PMC article. Clinical Trial.
The median senicapoc concentration at 72 h was 62.1 ng/ml (IQR 46.7-71.2). The primary outcome, PaO(2) /FiO(2) ratio at 72 h, was significantly lower in the senicapoc group (mean 19.5 kPa, SD 6.6) than in the control group (mean 24.4 kPa, SD 9.2) (mean difference -5 …
The median senicapoc concentration at 72 h was 62.1 ng/ml (IQR 46.7-71.2). The primary outcome, PaO(2) /FiO(2) ratio at 72 h, was sig …
Senicapoc (ICA-17043): a potential therapy for the prevention and treatment of hemolysis-associated complications in sickle cell anemia.
Ataga KI, Stocker J. Ataga KI, et al. Expert Opin Investig Drugs. 2009 Feb;18(2):231-9. doi: 10.1517/13543780802708011. Expert Opin Investig Drugs. 2009. PMID: 19236269 Review.
The hydration state (and intracellular hemoglobin concentration) of the sickle erythrocyte depends on the loss of solute and osmotically obliged water through specific pathways. Senicapoc (also known as ICA-17043) is a potent blocker of the Gardos channel, a calcium-activa …
The hydration state (and intracellular hemoglobin concentration) of the sickle erythrocyte depends on the loss of solute and osmotically obl …
Treatment with senicapoc in a porcine model of acute respiratory distress syndrome.
Petersen AG, Lind PC, Jensen AB, Eggertsen MA, Granfeldt A, Simonsen U. Petersen AG, et al. Intensive Care Med Exp. 2021 Apr 19;9(1):20. doi: 10.1186/s40635-021-00381-z. Intensive Care Med Exp. 2021. PMID: 33870468 Free PMC article.
Animals were then randomly assigned to vehicle (n = 9) or intravenous senicapoc (10 mg, n = 9) and received lung-protective ventilation for 6 h. RESULTS: Final senicapoc plasma concentrations were 67 18 nM (n = 9). Senicapoc failed to change the primary endpo …
Animals were then randomly assigned to vehicle (n = 9) or intravenous senicapoc (10 mg, n = 9) and received lung-protective ventilati …
Treatment with senicapoc, a K(Ca) 3.1 channel blocker, alleviates hypoxaemia in a mouse model of acute respiratory distress syndrome.
Petersen AG, Lind PC, Mogensen S, Jensen AB, Granfeldt A, Simonsen U. Petersen AG, et al. Br J Pharmacol. 2022 May;179(10):2175-2192. doi: 10.1111/bph.15704. Epub 2022 Feb 17. Br J Pharmacol. 2022. PMID: 34623632 Free article.
Senicapoc (30 mg.kg(-1) ) reduced histopathological lung injury score and neutrophils in BALF. ...Moreover, senicapoc directly affects lung epithelial cells and blocks neutrophil infiltration in the injured lung. ...
Senicapoc (30 mg.kg(-1) ) reduced histopathological lung injury score and neutrophils in BALF. ...Moreover, senicapoc directly
Role of thalidomide, senicapoc, and sodium butyrate in choroidal neovascularization.
Lyzogubov V, Dasso M, Bora N, Bora PS. Lyzogubov V, et al. Biochem Biophys Res Commun. 2020 Sep 17;530(2):367-373. doi: 10.1016/j.bbrc.2020.07.140. Epub 2020 Aug 13. Biochem Biophys Res Commun. 2020. PMID: 32800337
Thalidomide (24 mug), senicapoc (4 mug), or sodium butyrate (100 mug) was intravitreally injected the day after CNV induction. Thalidomide, senicapoc, and sodium butyrate inhibited CNV size by 56%, 24%, and 21% respectively on day 7 post-laser. ...
Thalidomide (24 mug), senicapoc (4 mug), or sodium butyrate (100 mug) was intravitreally injected the day after CNV induction. Thalid …
Repurposing the K(Ca)3.1 Blocker Senicapoc for Ischemic Stroke.
Lee RD, Chen YJ, Nguyen HM, Singh L, Dietrich CJ, Pyles BR, Cui Y, Weinstein JR, Wulff H. Lee RD, et al. Transl Stroke Res. 2024 Jun;15(3):518-532. doi: 10.1007/s12975-023-01152-6. Epub 2023 Apr 24. Transl Stroke Res. 2024. PMID: 37088858 Free PMC article.
A different treatment paradigm with senicapoc started at 3 h and MRI on day 3 and day 8 revealed that senicapoc reduces secondary infarct growth and suppresses expression of inflammation markers, including T cell cytokines in the brain. Lastly, we demonstrated that …
A different treatment paradigm with senicapoc started at 3 h and MRI on day 3 and day 8 revealed that senicapoc reduces second …
Repurposing the KCa3.1 inhibitor senicapoc for Alzheimer's disease.
Jin LW, Lucente JD, Nguyen HM, Singh V, Singh L, Chavez M, Bushong T, Wulff H, Maezawa I. Jin LW, et al. Ann Clin Transl Neurol. 2019 Mar 18;6(4):723-738. doi: 10.1002/acn3.754. eCollection 2019 Apr. Ann Clin Transl Neurol. 2019. PMID: 31019997 Free PMC article.
To investigate the role of KCa3.1 in AD pathology, we resynthesized senicapoc, a clinically tested KCa3.1 blocker, and determined its pharmacokinetic properties and its effect on microglial activation, Abeta deposition and hippocampal long-term potentiation (hLTP) in 5xFAD …
To investigate the role of KCa3.1 in AD pathology, we resynthesized senicapoc, a clinically tested KCa3.1 blocker, and determined its …
The Clinically Tested Gardos Channel Inhibitor Senicapoc Exhibits Antimalarial Activity.
Tubman VN, Mejia P, Shmukler BE, Bei AK, Alper SL, Mitchell JR, Brugnara C, Duraisingh MT. Tubman VN, et al. Antimicrob Agents Chemother. 2015 Oct 12;60(1):613-6. doi: 10.1128/AAC.01668-15. Print 2016 Jan. Antimicrob Agents Chemother. 2015. PMID: 26459896 Free PMC article.
We tested the hypothesis that senicapoc-induced blockade of the Gardos channel inhibits Plasmodium growth. Senicapoc inhibited in vitro growth of human and primate plasmodia during the clinical blood stage. Senicapoc treatment suppressed P. yoelii parasitemia …
We tested the hypothesis that senicapoc-induced blockade of the Gardos channel inhibits Plasmodium growth. Senicapoc inhibited …
A validated UHPLC-MS/MS method for rapid determination of senicapoc in plasma samples.
Sørensen LK, Petersen A, Granfeldt A, Simonsen U, Hasselstrøm JB. Sørensen LK, et al. J Pharm Biomed Anal. 2021 Apr 15;197:113956. doi: 10.1016/j.jpba.2021.113956. Epub 2021 Feb 8. J Pharm Biomed Anal. 2021. PMID: 33626443 Free PMC article.
The clinically tested KCa3.1 channel blocker, senicapoc, has been proven to have excellent pharmacological properties and prior clinical trials found it to be safe for use in patients with sickle cell anaemia. Currently, several preclinical projects are aiming to repurpose …
The clinically tested KCa3.1 channel blocker, senicapoc, has been proven to have excellent pharmacological properties and prior clini …
81 results