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Salfaprodil free base

CAS No. : 640290-67-1

MCE 站：Salfaprodil free base

产品活性：Salfaprodil free base (Neu2000) 是一种 NR2B 选择性和非竞争性的 N- 甲基 -D- 天冬氨酸 (NMDA) 受体拮抗剂，也是一种自由基清除剂。Salfaprodil free base 对 NMDA 和自由基诱导的细胞死亡具有出色的神经保护作用。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：iGluR

In Vitro: Salfaprodil (10-300 μM) shows apparent neuroprotection against 300 μM N-methyl-d-aspartate (NMDA) at doses as low as 30 μM.
Salfaprodil (10-500 μM) inhibits the electrophysiologic response of cultured cortical neurons to 300 μM NMDA in a concentration-dependent manner.
Salfaprodil (0.1-1 μM) produces a marked reduction of Fe²⁺-induced neurotoxicity, even at doses of 0.1 to 0.3 μM.
Salfaprodil (0.1-1 μM) blocks the degeneration of neurons and glia in cortical cell cultures.
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).
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.
Salfaprodil (0.19-12.5 μM) inhibits malondialdehyde (MDA) formation with an IC₅₀ of 2.72±0.26 μM.
Salfaprodil (0-125 μM) effectively reduces iron-ascorbate-induced lipid peroxidation (IC₅₀=24.56±0.07 μM).

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.
Salfaprodil (5 mg/kg; i.v.) protects white matter such as axons and myelin as well as gray matter from ischemic brain injury.

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