EF-1502
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| IUPAC name
4-[4,4-bis(3-methylthiophen-2-yl)but-3-enyl-methylamino]-4,5,6,7-tetrahydro-1,2-benzoxazol-3-one
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3D model (JSmol)
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| ChEMBL | |
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PubChemCID
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| Properties | |
| C22H26N2O2S2 | |
| Molar mass | 414.58g·mol−1 |
Except where otherwise noted, data are given for materials in theirstandard state(at 25 °C [77 °F], 100 kPa).
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EF-1502is aGABA reuptake inhibitor.It could potentially be used to treat seizures.
Mechanism of action
[edit]EF-1502 has been shown to inhibit thetype 1 GABA transporter(GAT1)[1]and thesodium and chloride-dependent betaine transporter(BGT-1).[2]
Potential use
[edit]Tests in mice have shown that this compound possesses and anticonvulsant effect due to its GABA reuptake inhibiting properties.[3][4]
References
[edit]- ^Madsen, Karsten K.; White, H. Steve; Schousboe, Arne (March 2010)."Neuronal and non-neuronal GABA transporters as targets for antiepileptic drugs".Pharmacology & Therapeutics.125(3): 394–401.doi:10.1016/j.pharmthera.2009.11.007.ISSN1879-016X.PMID20026354.
- ^Schousboe, Arne; Larsson, Orla M.; Sarup, Alan; White, H. Steve (2004-10-01)."Role of the betaine/GABA transporter (BGT-1/GAT2) for the control of epilepsy".European Journal of Pharmacology.500(1–3): 281–287.doi:10.1016/j.ejphar.2004.07.032.ISSN0014-2999.PMID15464040.
- ^Madsen, Karsten K.; Hansen, Gert H.; Danielsen, E. Michael; Schousboe, Arne (February 2015)."The subcellular localization of GABA transporters and its implication for seizure management".Neurochemical Research.40(2): 410–419.doi:10.1007/s11064-014-1494-9.ISSN1573-6903.PMID25519681.
- ^Schousboe, Arne; Sarup, Alan; Larsson, Orla M.; White, H. Steve (2004-10-15)."GABA transporters as drug targets for modulation of GABAergic activity".Biochemical Pharmacology.68(8): 1557–1563.doi:10.1016/j.bcp.2004.06.041.ISSN0006-2952.PMID15451399.