1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. iGluR
  3. Salfaprodil

Salfaprodil (Synonyms: Neu2000 potassium)

Cat. No.: HY-106408A
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Salfaprodil (Neu2000 potassium) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA), and a free radical scavenger. Salfaprodil has excellent neuroprotection against NMDA- and free radical-induced cell death.

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Salfaprodil Chemical Structure

Salfaprodil Chemical Structure

CAS No. : 916214-57-8

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Description

Salfaprodil (Neu2000 potassium) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA), and a free radical scavenger. Salfaprodil has excellent neuroprotection against NMDA- and free radical-induced cell death[1][2].

IC50 & Target

NMDA[1]

In Vitro

Salfaprodil (10-300 μM) shows apparent neuroprotection against 300 μM N-methyl-d-aspartate (NMDA) at doses as low as 30 μM[1].
Salfaprodil (10-500 μM) inhibits the electrophysiologic response of cultured cortical neurons to 300 μM NMDA in a concentration-dependent manner[1].
Salfaprodil (0.1-1 μM) produces a marked reduction of Fe2+-induced neurotoxicity, even at doses of 0.1 to 0.3 μM[1].
Salfaprodil (0.1-1 μM) blocks the degeneration of neurons and glia in cortical cell cultures[1].
Salfaprodil (0-350 μM) effectively scavenges superoxide radicals (IC50=63.07±1.44 μM), nitric oxide (IC50=155.8±4.88 μM), and hydroxyl radicals (IC50=58.45±1.74 μM)[3].
Salfaprodil (0.78-12.5 μM) decreases the amount of antimycin A-induced ROS/RNS formation in a dose-dependent manner, with an IC50 of 2.21±0.11 μM[3].
Salfaprodil (0.19-12.5 μM) inhibits malondialdehyde (MDA) formation with an IC50 of 2.72±0.26 μM[3].
Salfaprodil (0-125 μM) effectively reduces iron-ascorbate-induced lipid peroxidation (IC50=24.56±0.07 μM)[3].

In Vivo

Salfaprodil (0.5-20 mg/kg; i.v.) reduces cerebral infarct evolving 24 h after 60-mins occlusion of the middle cerebral artery occlusion (MCAO) substantially and dose dependently[1].
Salfaprodil (5 mg/kg; i.v.) protects white matter such as axons and myelin as well as gray matter from ischemic brain injury[1].

Animal Model: Male Sprague-Dawley rats (260 to 300 g) (clip occlusion model)[1]
Dosage: 0.5-20 mg/kg
Administration: I.v. administration 5 mins after reperfusion
Result: Produced a large neuroprotective effect, with a maximal reduction in infarct volume of 66% at doses of 2.5 to 5 mg/kg.
Not observed neuronal damage in the most vulnerable cortical area after administration of 5 mg/kg.
Animal Model: Male Sprague-Dawley rats (260 to 300 g) (intraluminal thread occlusion model)[1]
Dosage: 5 mg/kg
Administration: I.v. administration 30 mins after reperfusion
Result: Did not change physiologic variables such as arterial pH, PCO2, PO2, and hematocrit.
Reduced infarct volume evolving in the cortex and the striatum substantially.
Reduced white matter damage in the striatum and external capsule markedly.
Molecular Weight

421.31

Formula

C₁₅H₇F₇KNO₃

CAS No.

916214-57-8

SMILES

OC1=CC=C(C=C1C(O[K])=O)NCC2=C(C(F)=C(C(F)=C2F)C(F)(F)F)F

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

SalfaprodilNeu2000Neu 2000Neu-2000iGluRIonotropic glutamate receptorsNMDAneuroprotectionantioxidantfreeradicalscavengerInhibitorinhibitorinhibit

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