Chimeric agents derived from the functionalized amino acid, lacosamide, and the α-aminoamide, safinamide: evaluation of their inhibitory actions on voltage-gated sodium channels, and antiseizure and antinociception activities and comparison with lac

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Chimeric agents derived from the functionalized amino acid, lacosamide, and the α-aminoamide, safinamide: evaluation of their inhibitory actions on voltage-gated sodium channels, and antiseizure and antinociception activities and comparison with lac is …
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scholarly articleQ13442814

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P356DOI10.1021/CN5002182
P932PMC publication ID4372064
P698PubMed publication ID25418676
P5875ResearchGate publication ID268788563

P50authorErik T DustrudeQ89207878
Matthew S RipschQ115615314
Rajesh KhannaQ48357681
P2093author name stringFletcher A White
Yuying Wang
Harold Kohn
Ki Duk Park
Xiao-Fang Yang
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An atypical role for collapsin response mediator protein 2 (CRMP-2) in neurotransmitter release via interaction with presynaptic voltage-gated calcium channelsQ28579315
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Merging the structural motifs of functionalized amino acids and alpha-aminoamides: compounds with significant anticonvulsant activitiesQ33840785
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Substituted N-(biphenyl-4'-yl)methyl (R)-2-acetamido-3-methoxypropionamides: potent anticonvulsants that affect frequency (use) dependence and slow inactivation of sodium channelsQ33951922
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In silico docking and electrophysiological characterization of lacosamide binding sites on collapsin response mediator protein-2 identifies a pocket important in modulating sodium channel slow inactivationQ34055749
The formalin test: scoring properties of the first and second phases of the pain response in rats.Q34058687
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Synthesis and Anticonvulsant Activity of a New Class of 2-[(Arylalkyl)amino]alkanamide DerivativesQ34458402
Slow inactivation in voltage-gated sodium channels: molecular substrates and contributions to channelopathiesQ34562464
Lacosamide, a novel anti-convulsant drug, shows efficacy with a wide safety margin in rodent models for epilepsyQ34618958
The investigational anticonvulsant lacosamide selectively enhances slow inactivation of voltage-gated sodium channels.Q34701722
Development and characterization of novel derivatives of the antiepileptic drug lacosamide that exhibit far greater enhancement in slow inactivation of voltage-gated sodium channels.Q34865999
Merging Structural Motifs of Functionalized Amino Acids and α-Aminoamides Results in Novel Anticonvulsant Compounds with Significant Effects on Slow and Fast Inactivation of Voltage-gated Sodium Channels and in the Treatment of Neuropathic PainQ35099293
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The persistent release of HMGB1 contributes to tactile hyperalgesia in a rodent model of neuropathic painQ36369795
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(Biphenyl-4-yl)methylammonium chlorides: potent anticonvulsants that modulate Na+ currentsQ37347379
The Na(V)1.7 sodium channel: from molecule to man.Q38066723
Pharmacological characterization of the 6 Hz psychomotor seizure model of partial epilepsyQ39222620
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Differential block of sensory neuronal voltage-gated sodium channels by lacosamide [(2R)-2-(acetylamino)-N-benzyl-3-methoxypropanamide], lidocaine, and carbamazepineQ39996628
Voltage-dependent ion channels in CAD cells: A catecholaminergic neuronal line that exhibits inducible differentiationQ40838391
Long-term efficacy and safety of safinamide as add-on therapy in early Parkinson's diseaseQ43620394
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The anti-nociceptive agent ralfinamide inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive Na+ currents in dorsal root ganglion neuronsQ46373509
Lacosamide displays potent antinociceptive effects in animal models for inflammatory painQ46537390
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Subthreshold sodium currents and pacemaking of subthalamic neurons: modulation by slow inactivationQ48259982
Biochemical and electrophysiological studies on the mechanism of action of PNU-151774E, a novel antiepileptic compoundQ48278287
Cdk5-mediated phosphorylation of CRMP-2 enhances its interaction with CaV2.2.Q48357626
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Slow inactivation of the sodium conductance in squid giant axons. Pronase resistanceQ54579818
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Selective and potent monoamine oxidase type B inhibitors: 2-substituted 5-aryltetrazole derivativesQ71566488
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A note on a simple apparatus for detecting neurological deficit in rats and miceQ74784538
P433issue2
P407language of work or nameEnglishQ1860
P921main subjectsodium channel activityQ14905710
P304page(s)316-330
P577publication date2014-12-09
P1433published inACS Chemical NeuroscienceQ2819059
P1476titleChimeric agents derived from the functionalized amino acid, lacosamide, and the α-aminoamide, safinamide: evaluation of their inhibitory actions on voltage-gated sodium channels, and antiseizure and antinociception activities and comparison with lac
P478volume6

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cites work (P2860)
Q35706539Chimeric derivatives of functionalized amino acids and α-aminoamides: compounds with anticonvulsant activity in seizure models and inhibitory actions on central, peripheral, and cardiac isoforms of voltage-gated sodium channels.
Q26740905Emerging approaches in Parkinson's disease - adjunctive role of safinamide
Q50934270Lacosamide Inhibition of Nav1.7 Voltage-Gated Sodium Channels: Slow Binding to Fast-Inactivated States
Q28074736Monoaminergic Mechanisms in Epilepsy May Offer Innovative Therapeutic Opportunity for Monoaminergic Multi-Target Drugs

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