EF1502

selective gamma-aminobutyric acid transport inhibitor; structure in first source

Also Known As:

EF 1502; N-(4,4-bis(3-methyl-2-thienyl)-3-butenyl)-3-hydroxy-4-(methylamino)-4,5,6,7-tetrahydrobenzo(d)isoxazol-3-ol

Networked: 6 relevant articles (0 outcomes, 2 trials/studies)

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Azoles: 2138
    - Isoxazoles: 155
      - EF1502: 6

Experts

1.	Schousboe, Arne: 6 articles (07/2020 - 02/2005)
2.	White, H Steve: 5 articles (07/2020 - 02/2005)
3.	Clausen, Rasmus P: 4 articles (07/2020 - 02/2005)
4.	Krogsgaard-Larsen, Povl: 3 articles (07/2011 - 02/2005)
5.	Madsen, Karsten K: 3 articles (07/2011 - 05/2009)
6.	Ecker, Gerhard F: 2 articles (07/2020 - 12/2019)
7.	Kickinger, Stefanie: 2 articles (07/2020 - 12/2019)
8.	Wellendorph, Petrine: 2 articles (07/2020 - 12/2019)
9.	Frølund, Bente: 2 articles (12/2019 - 02/2005)
10.	Larsson, Orla M: 2 articles (05/2009 - 02/2005)

Related Diseases

1.	Epilepsy (Aura) 12/15/2019 - "BGT1 has emerged as an interesting target for treating epilepsy due to animal studies that reported anticonvulsant effects for the GAT1/BGT1 selective inhibitor EF1502 and the BGT1 selective inhibitor RPC-425. " 07/01/2020 - "Synergistic anti-seizure effects achieved by inhibition of both GAT1 and the betaine/GABA transporter (BGT1) by tiagabine and EF1502, compared to tiagabine alone, suggest BGT1 as a target in epilepsy. " 03/01/2010 - "It is suggested that the betaine-GABA transporter BGT1 should receive particular interest in this context as the GABA analogue EF 1502 (N-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-4-(methylamino)-4,5,6,7-tetrahydrobenzo[d]isoxazol-3-ol) has been shown to possess a novel anticonvulsant profile in animal models of epilepsy, involving the ability to inhibit GABA transport mediated by GAT1 and BGT1 at the same time."
2.	Partial Epilepsies (Epilepsy, Partial) 02/01/2005 - "In the present study, EF1502 was found to possess a broad-spectrum anticonvulsant profile in animal models of generalized and partial epilepsy. " 05/01/2009 - "These findings support anatomical evidence that GAT2/3 are most likely located at the synapse in close proximity to GAT1; whereas BGT-1 is located some distance away from the synapse and GAT1 and GAT2/3. Lastly, EF1502 and tiagabine were evaluated alone, and in combination, in the corneal kindled mouse model of partial epilepsy. "
3.	Reflex Epilepsy (Photosensitive Epilepsy) 05/01/2009 - "When combined with the GAT1 selective inhibitor tiagabine, EF1502 was found to possess a synergistic anti-convulsant action in the Frings audiogenic seizure-susceptible mouse model of reflex epilepsy. "
4.	Ataxia (Dyssynergia) 07/01/2011 - "Selective GABA transporter inhibitors tiagabine and EF1502 exhibit mechanistic differences in their ability to modulate the ataxia and anticonvulsant action of the extrasynaptic GABA(A) receptor agonist gaboxadol."

Related Drugs and Biologics

1.	Anticonvulsants (Antiepileptic Drugs)
2.	GABA Plasma Membrane Transport Proteins
3.	Tiagabine (Gabitril)
4.	Betaine (C.B.B.)
5.	GABA-A Receptor Agonists
6.	gamma-Aminobutyric Acid (GABA)
7.	Convulsants
8.	azastene
9.	gaboxadol (THIP)