Brivaracetam: Rationale for discovery and preclinical profile of a selective SV2A ligand for epilepsy treatment (Q38752407)

6 September 2017

title

Brivaracetam: Rationale for discovery and preclinical profile of a selective SV2A ligand for epilepsy treatment (English)

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6 September 2017

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ChEBI release 2020-05-28

Henrik Klitgaard

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6 September 2017

Alain Matagne

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6 September 2017

Jean-Marie Nicolas

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6 September 2017

Michel Gillard

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6 September 2017

Yves Lamberty

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6 September 2017

Marc De Ryck

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6 September 2017

Rafal M Kaminski

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6 September 2017

Karine Leclercq

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6 September 2017

Isabelle Niespodziany

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6 September 2017

Christian Wolff

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6 September 2017

Martyn Wood

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6 September 2017

Jonas Hannestad

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6 September 2017

Sophie Kervyn

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6 September 2017

Benoit Kenda

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6 September 2017

publication date

26 February 2016

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6 September 2017

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6 September 2017

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6 September 2017

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6 September 2017

page(s)

538-548

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Prognosis of epilepsy: a review and further analysis of the first nine years of the British National General Practice Study of Epilepsy, a prospective population-based study

6 September 2017

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A randomized, double-blind, placebo-controlled, multicenter, parallel-group study to evaluate the efficacy and safety of adjunctive brivaracetam in adult patients with uncontrolled partial-onset seizures

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Discovery of 4-substituted pyrrolidone butanamides as new agents with significant antiepileptic activity

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Profile of ucb L059, a novel anticonvulsant drug, in models of partial and generalized epilepsy in mice and rats

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Evidence for a unique profile of levetiracetam in rodent models of seizures and epilepsy

21 January 2018

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New avenues for anti-epileptic drug discovery and development

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The novel antiepileptic drug levetiracetam (ucb L059) appears to act via a specific binding site in CNS membranes

21 January 2018

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SV2A protein is a broad-spectrum anticonvulsant target: functional correlation between protein binding and seizure protection in models of both partial and generalized epilepsy

21 January 2018

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The synaptic vesicle protein SV2A is the binding site for the antiepileptic drug levetiracetam

21 January 2018

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Proepileptic phenotype of SV2A-deficient mice is associated with reduced anticonvulsant efficacy of levetiracetam.

21 January 2018

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Abnormal neurotransmission in mice lacking synaptic vesicle protein 2A (SV2A)

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SV2 modulates the size of the readily releasable pool of secretory vesicles

21 January 2018

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Binding characteristics of brivaracetam, a selective, high affinity SV2A ligand in rat, mouse and human brain: relationship to anti-convulsant properties.

21 January 2018

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Binding characteristics of levetiracetam to synaptic vesicle protein 2A (SV2A) in human brain and in CHO cells expressing the human recombinant protein

21 January 2018

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Levetiracetam has a time- and stimulation-dependent effect on synaptic transmission

21 January 2018

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Brivaracetam augments short-term depression and slows vesicle recycling

21 January 2018

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Levetiracetam accelerates the onset of supply rate depression in synaptic vesicle trafficking.

21 January 2018

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Modulation of the conformational state of the SV2A protein by an allosteric mechanism as evidenced by ligand binding assays

21 January 2018

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Brivaracetam (ucb 34714) inhibits Na(+) current in rat cortical neurons in culture.

21 January 2018

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Brivaracetam differentially affects voltage-gated sodium currents without impairing sustained repetitive firing in neurons

21 January 2018

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Levetiracetam inhibits the high-voltage-activated Ca(2+) current in pyramidal neurones of rat hippocampal slices

21 January 2018

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The synaptic vesicle glycoprotein 2A ligand levetiracetam inhibits presynaptic Ca2+ channels through an intracellular pathway

21 January 2018

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Selective blockade of N-type calcium channels by levetiracetam

21 January 2018

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Modulation of AMPA receptors in cultured cortical neurons induced by the antiepileptic drug levetiracetam

21 January 2018

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An open-label, prospective, exploratory study of patients with epilepsy switching from levetiracetam to brivaracetam

21 January 2018

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Brivaracetam, a selective high-affinity synaptic vesicle protein 2A (SV2A) ligand with preclinical evidence of high brain permeability and fast onset of action

21 January 2018

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Estimation of blood-brain barrier crossing of drugs using molecular size and shape, and H-bonding descriptors.

21 January 2018

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Pharmacokinetics and metabolism of 14C-brivaracetam, a novel SV2A ligand, in healthy subjects

21 January 2018

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The pharmacokinetics, CNS pharmacodynamics and adverse event profile of brivaracetam after multiple increasing oral doses in healthy men

21 January 2018

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Effect of gemfibrozil on the metabolism of brivaracetam in vitro and in human subjects

21 January 2018

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21 January 2018

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Anti-convulsive and anti-epileptic properties of brivaracetam (ucb 34714), a high-affinity ligand for the synaptic vesicle protein, SV2A.

21 January 2018

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Brivaracetam is superior to levetiracetam in a rat model of post-hypoxic myoclonus.

21 January 2018

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The potential of antiseizure drugs and agents that act on novel molecular targets as antiepileptogenic treatments

21 January 2018

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Antihyperalgesic effect of levetiracetam in neuropathic pain models in rats

21 January 2018

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Brivaracetam inhibits spreading depression in rat neocortical slices in vitro

21 January 2018

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Use of epileptic animals for adverse effect testing

21 January 2018

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Validation of corneally kindled mice: a sensitive screening model for partial epilepsy in man.

21 January 2018

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Kindling Increases the Sensitivity of Rats to Adverse Effects of Certain Antiepileptic Drugs

21 January 2018

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Cognitive disorders associated with epilepsy: diagnosis and treatment.

21 January 2018

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Absence of negative impact of levetiracetam on cognitive function and memory in normal and amygdala-kindled rats.

21 January 2018

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Brivaracetam does not alter spatial learning and memory in both normal and amygdala-kindled rats

21 January 2018

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Intracellular calcium increase in epileptiform activity: modulation by levetiracetam and lamotrigine

21 January 2018

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21 January 2018

Identifiers

DOI

10.1111/EPI.13340

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6 September 2017

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