EF-1502 is a GABA reuptake inhibitor. It could potentially be used to treat seizures.

Mechanism of action

EF-1502 has been shown to inhibit the type 1 GABA transporter (GAT1)[1] and the sodium and chloride-dependent betaine transporter (BGT-1).[2]

Potential use

Tests in mice have shown that this compound possesses and anticonvulsant effect due to its GABA reuptake inhibiting properties.[3][4]

References

  1. ^ 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. ISSN 1879-016X. PMID 20026354.
  2. ^ 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. ISSN 0014-2999. PMID 15464040.
  3. ^ 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. ISSN 1573-6903. PMID 25519681.
  4. ^ 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. ISSN 0006-2952. PMID 15451399.
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