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Cat.No.S1438
| Related Targets | Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism |
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| Other Carbonic Anhydrase Inhibitors | U-104 Indisulam (E7070) Benzenesulfonamide Tioxolone 2-Aminobenzenesulfonamide |
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In vitro |
DMSO
: 68 mg/mL
(200.37 mM)
Ethanol : 68 mg/mL Water : Insoluble |
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In vivo |
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| Molecular Weight | 339.36 | Formula | C12H21NO8S |
Storage (From the date of receipt) | |
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| CAS No. | 97240-79-4 | Download SDF | Storage of Stock Solutions |
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| Synonyms | MCN 4853, RWJ 17021 | Smiles | CC1(OC2COC3(C(C2O1)OC(O3)(C)C)COS(=O)(=O)N)C | ||
| Targets/IC50/Ki |
sodium channel
Calcium Channel
AMPA/kainate receptor
Carbonic anhydrase
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| In vitro |
Topiramate slightly inhibits the persistent fraction of Na+ current in dissociated neurons and reduces the Na+-dependent long-lasting action potential shoulders, which can be evoked in layer V pyramidal neurons after Ca+ and K+ current blockade in neocortical slices. This compound at low concentrations (IC50, approximately 0.5 mM) selectively inhibits pharmacologically isolated excitatory synaptic currents mediated by kainate receptors containing the GluR5 subunit in whole-cell voltage-clamp recordings from principal neurons of the rat basolateral amygdala. It also partially depresses predominantly AMPA-receptor-mediated EPSCs, but with lower efficacy. This chemical suppresses voltage-sensitive Na+ channels and non-N-methyl-D-aspartate (NMDA) receptors and enhances gamma-aminobutyric acid (GABA)-mediated inhibition. It selectively inhibits postsynaptic responses mediated by GluR5 kainate receptors.
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| In vivo |
Topiramate (25-100 mg/kg, i.p.) produces a dose-dependent elevation in the threshold for clonic seizures induced by infusion of ATPA, a selective agonist of GluR5 kainate receptors. This compound effectively suppresses acute seizures induced by perinatalhypoxia in a dose-related manner with a calculated ED50 of 2.1 mg/kg, i.p. It (20 and 40 mg/kg i.p.) inhibits both tonic and absence-like seizures in a dose-dependent manner, whereas Phenytoin (20 mg/kg i.p.) and Zonisamide (40 mg/kg i.p.) inhibits only the tonic seizures. This chemical inhibits sound-induced seizures in DBA/2 mice (ED50 = 8.6 mg/kg p.o.).
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06282783 | Not yet recruiting | HIV-1-infection|Hiv|HIV Infections|HIV I Infection |
Erasmus Medical Center |
September 2024 | Phase 1|Phase 2 |
| NCT05975580 | Recruiting | Obesity |
University of California Irvine|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) |
August 29 2023 | Phase 4 |
| NCT04613024 | Not yet recruiting | Weight Loss|Pain Postoperative |
Stanford University |
July 1 2023 | Early Phase 1 |
| NCT04986631 | Recruiting | Obesity Childhood |
University of Minnesota |
April 4 2022 | Early Phase 1 |
| NCT03308669 | Completed | Healthy |
Eli Lilly and Company |
October 16 2017 | Phase 1 |
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