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LY3130481

an AMPA receptor antagonist with anticonvulsant activity; structure in first source

Also Known As:

6-(1-(1-(5-(2-hydroxyethoxy)pyridin-2-yl)-1H-pyrazol-3-yl)ethyl)-3H-1,3-benzothiazol-2-one

Networked: 4 relevant articles (1 outcomes, 0 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Azoles: 2138
    - Thiazoles: 392
      - Benzothiazoles: 40
        LY3130481: 4
    - Pyrazoles: 61
      - LY3130481: 4
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Benzothiazoles: 40
      - LY3130481: 4

Experts

1.	Kato, Akihiko S: 4 articles (01/2019 - 01/2017)
2.	Witkin, Jeffrey M: 4 articles (01/2019 - 01/2017)
3.	Gardinier, Kevin M: 3 articles (01/2019 - 01/2017)
4.	Reel, Jon: 3 articles (01/2019 - 01/2017)
5.	Gernert, Douglas L: 2 articles (01/2019 - 01/2017)
6.	Gleason, Scott D: 2 articles (11/2017 - 01/2017)
7.	Porter, Warren J: 2 articles (11/2017 - 01/2017)
8.	Adams, Benjamin L: 1 article (01/2019)
9.	Barth, Vanessa: 1 article (01/2019)
10.	Bredt, David S: 1 article (01/2019)

Related Diseases

1.	Seizures (Absence Seizure) 01/01/2017 - "In addition, LY3130481 was effective against absence seizures in the GAERS genetic model and in the Frings mouse model. " 01/01/2017 - "Likewise, LY3130481 attenuated convulsions in mice and rats with long-term induction of seizures (e.g., corneal, pentylenetetrazole, hippocampal, and amygdala kindled seizures). "
2.	Epilepsy (Aura) 01/01/2018 - "Utilizing these auxiliary proteins in compound screening led to the discovery of the TARP-dependent-AMPA forebrain selective receptor antagonist (TDAA), LY3130481/CERC-611 that is currently in clinical development for epilepsy." 01/01/2017 - "6-[(1S)-1-[1-[5-(2-hydroxyethoxy)-2-pyridyl]pyrazol-3-yl]ethyl]- 3H-1,3-benzothiazol-2-one (LY3130481 or CERC-611) is a selective antagonist of AMPA receptors containing transmembrane AMPA receptor regulatory protein (TARP) γ-8 that is under development for epilepsy. " 11/01/2017 - "6-[(1S)-1-[1-[5-(2-hydroxyethoxy)-2-pyridyl]pyrazol-3-yl]ethyl]-3H-1,3-benzothiazol-2-one (LY3130481 or CERC-611) is a selective antagonist of AMPA receptors containing transmembrane AMPA receptor regulatory protein (TARP) γ-8. This molecule has been characterized as a potent and efficacious anticonvulsant in an array of acute and chronic epilepsy models in rodents. "
3.	Chronic Pain 01/01/2019 - "Collectively, these data demonstrate that LY3130481 can suppress excitatory synaptic transmission and plasticity in pain pathways containing γ8/AMPA receptors and significantly reduce nocifensive behaviors, suggesting a novel, effective, and safer therapy for chronic pain conditions."
4.	Pain (Aches) 01/01/2019 - "Collectively, these data demonstrate that LY3130481 can suppress excitatory synaptic transmission and plasticity in pain pathways containing γ8/AMPA receptors and significantly reduce nocifensive behaviors, suggesting a novel, effective, and safer therapy for chronic pain conditions." 01/01/2019 - "Recently, LY3130481 has been shown to selectively block AMPA receptors coassembled with the auxiliary protein, transmembrane AMPA receptor regulatory protein (TARP) γ8, which is highly expressed in the hippocampus but also in pain pathways, including anterior cingulate (ACC) and somatosensory cortices and the spinal cord, suggesting that selective blockade of γ8/AMPA receptors may suppress nociceptive signaling with fewer CNS side effects. "
5.	Hyperalgesia 01/01/2019 - "In addition, LY3130481 dose-dependently attenuated established gait impairment after joint damage and tactile allodynia after spinal nerve ligation, all in the absence of motor side effects. "

Related Drugs and Biologics

1.	Proteins (Proteins, Gene)
2.	TARP
3.	AMPA Receptors (AMPA Receptor)
4.	alpha- Amino- 3- hydroxy- 5- methyl- 4- isoxazolepropionic Acid (AMPA)
5.	Pentylenetetrazole (Metrazol)
6.	Anticonvulsants (Antiepileptic Drugs)

Related Therapies and Procedures

1.	Therapeutics
2.	Ligation