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1960 2
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1977 1
1978 1
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1982 2
1984 1
1986 1
1988 1
1989 1
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1993 1
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1998 1
1999 2
2000 1
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73 results

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Page 1
Clemizole and La(3+) salts ameliorate angiotensin II-induced glomerular hyperpermeability in vivo.
Dolinina J, Rippe A, Öberg CM. Dolinina J, et al. Physiol Rep. 2021 May;9(10):e14781. doi: 10.14814/phy2.14781. Physiol Rep. 2021. PMID: 34042270 Free PMC article.
Anesthetized male Sprague-Dawley rats were infused with Ang II (80 ng kg(-1 ) min(-1) ) alone, or together with clemizole or low-dose La(3+) (activates TRPC5, blocks TRPC6) or high-dose La(3+) (blocks both TRPC5 and TRPC6). ...In conclusion, our data show that both clem
Anesthetized male Sprague-Dawley rats were infused with Ang II (80 ng kg(-1 ) min(-1) ) alone, or together with clemizole or low-dose …
Clemizole hydrochloride is a novel and potent inhibitor of transient receptor potential channel TRPC5.
Richter JM, Schaefer M, Hill K. Richter JM, et al. Mol Pharmacol. 2014 Nov;86(5):514-21. doi: 10.1124/mol.114.093229. Epub 2014 Aug 19. Mol Pharmacol. 2014. PMID: 25140002
Electrophysiological whole-cell recordings revealed that the block was mostly reversible. Moreover, clemizole was still effective in blocking TRPC5 single channels in excised inside-out membrane patches, hinting to a direct block of TRPC5 by clemizole. ...TRPM3 and …
Electrophysiological whole-cell recordings revealed that the block was mostly reversible. Moreover, clemizole was still effective in …
Clemizole hydrochloride blocks cardiac potassium currents stably expressed in HEK 293 cells.
Jie LJ, Wu WY, Li G, Xiao GS, Zhang S, Li GR, Wang Y. Jie LJ, et al. Br J Pharmacol. 2017 Feb;174(3):254-266. doi: 10.1111/bph.13679. Epub 2017 Jan 12. Br J Pharmacol. 2017. PMID: 27886373 Free PMC article.
The S631A, S636A, Y652A and F656V hERG mutant channels reduced the inhibitory effect of clemizole (IC(50) : 0.82, 0.89, 1.49 and 2.98 muM, respectively), suggesting that clemizole is a pore blocker of hERG channels. Clemizole also moderately decreased I(Ks) a …
The S631A, S636A, Y652A and F656V hERG mutant channels reduced the inhibitory effect of clemizole (IC(50) : 0.82, 0.89, 1.49 and 2.98 …
Targeted Molecular Strategies for Genetic Neurodevelopmental Disorders: Emerging Lessons from Dravet Syndrome.
Lersch R, Jannadi R, Grosse L, Wagner M, Schneider MF, von Stülpnagel C, Heinen F, Potschka H, Borggraefe I. Lersch R, et al. Neuroscientist. 2023 Dec;29(6):732-750. doi: 10.1177/10738584221088244. Epub 2022 Apr 13. Neuroscientist. 2023. PMID: 35414300 Free PMC article. Review.
Drug-repurposing approaches for SCN1A-related Dravet syndrome are currently under investigation (i.e., lorcaserin, clemizole, and ataluren). New therapeutic concepts also arise from the field of precision medicine by upregulating functional SCN1A or by activating Na(v)1.1. …
Drug-repurposing approaches for SCN1A-related Dravet syndrome are currently under investigation (i.e., lorcaserin, clemizole, and ata …
Pharmacological diversity amongst approved and emerging antiseizure medications for the treatment of developmental and epileptic encephalopathies.
Sills GJ. Sills GJ. Ther Adv Neurol Disord. 2023 Aug 30;16:17562864231191000. doi: 10.1177/17562864231191000. eCollection 2023. Ther Adv Neurol Disord. 2023. PMID: 37655228 Free PMC article. Review.
Putative ASMs currently in clinical development for use in DEEs include soticlestat, carisbamate, verapamil, radiprodil, clemizole and lorcaserin....
Putative ASMs currently in clinical development for use in DEEs include soticlestat, carisbamate, verapamil, radiprodil, clemizole an …
Clemizole and trazodone are effective antiseizure treatments in a zebrafish model of STXBP1 disorder.
Moog M, Baraban SC. Moog M, et al. Epilepsia Open. 2022 Sep;7(3):504-511. doi: 10.1002/epi4.12604. Epub 2022 May 17. Epilepsia Open. 2022. PMID: 35451230 Free PMC article.
Phenytoin (PHT), valproate (VPA), ethosuximide (ESX), levetiracetam (LEV), and diazepam (DZP) had no effect on the ictal-like event frequency in stxbp1b mutant zebrafish. Clemizole and trazodone decreased ictal-like event frequency in stxbp1b mutant zebrafish by 80% and 83 …
Phenytoin (PHT), valproate (VPA), ethosuximide (ESX), levetiracetam (LEV), and diazepam (DZP) had no effect on the ictal-like event frequenc …
Structural basis for human TRPC5 channel inhibition by two distinct inhibitors.
Song K, Wei M, Guo W, Quan L, Kang Y, Wu JX, Chen L. Song K, et al. Elife. 2021 Mar 8;10:e63429. doi: 10.7554/eLife.63429. Elife. 2021. PMID: 33683200 Free PMC article.
Here, we present the cryo-EM structures of human TRPC5 in complex with two distinct inhibitors, namely clemizole and HC-070, to the resolution of 2.7 A. The structures reveal that clemizole binds inside the voltage sensor-like domain of each subunit. ...Moreover, we …
Here, we present the cryo-EM structures of human TRPC5 in complex with two distinct inhibitors, namely clemizole and HC-070, to the r …
Antihistaminic and anticholinergic activities of mequitazine in comparison with clemizole.
Martinez-Mir I, Estañ L, Rubio E, Morales-Olivas FJ. Martinez-Mir I, et al. J Pharm Pharmacol. 1988 Sep;40(9):655-6. doi: 10.1111/j.2042-7158.1988.tb05331.x. J Pharm Pharmacol. 1988. PMID: 2907038
The antihistamine and anticholinergic properties of mequitazine have been investigated and compared with those of clemizole. Both mequitazine and clemizole antagonized the effect of histamine in guinea-pig ileum competitively, the pA2 values calculated by Schild plo …
The antihistamine and anticholinergic properties of mequitazine have been investigated and compared with those of clemizole. Both meq …
Amelioration of Parkinson's disease by pharmacological inhibition and knockdown of redox sensitive TRPC5 channels: Focus on mitochondrial health.
Vaidya B, Gupta P, Laha JK, Roy I, Sharma SS. Vaidya B, et al. Life Sci. 2023 Sep 1;328:121871. doi: 10.1016/j.lfs.2023.121871. Epub 2023 Jun 21. Life Sci. 2023. PMID: 37352915
Additionally, SH-SY5Y neurons were exposed to 1-methyl-4-phenylpyridinium (MPP(+)) to further determine the role of TRPC5 channels in PD. KEY FINDINGS: We used clemizole hydrochloride, a potent TRPC5 channel blocker, to reverse the behavioural deficits, molecular changes a …
Additionally, SH-SY5Y neurons were exposed to 1-methyl-4-phenylpyridinium (MPP(+)) to further determine the role of TRPC5 channels in PD. KE …
The hepatitis C virus (HCV) NS4B RNA binding inhibitor clemizole is highly synergistic with HCV protease inhibitors.
Einav S, Sobol HD, Gehrig E, Glenn JS. Einav S, et al. J Infect Dis. 2010 Jul 1;202(1):65-74. doi: 10.1086/653080. J Infect Dis. 2010. PMID: 20486856 Free PMC article.
Finally, no cross-resistance to clemizole of SCH503034-resistant mutants (or vice versa) was observed. CONCLUSIONS: Clemizole can yield high-level synergy with the protease inhibitor class. ...
Finally, no cross-resistance to clemizole of SCH503034-resistant mutants (or vice versa) was observed. CONCLUSIONS: Clemizole
73 results