Nelonemdaz (Salfaprodil) 钾是 N-甲基-D-天冬氨酸 (NMDA) 的 NR2B 选择性和非竞争性拮抗剂。
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].
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].
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]
[1]. Gwag BJ, et al. Marked prevention of ischemic brain injury by Neu2000, an NMDA antagonist and antioxidant derived from aspirin and sulfasalazine. J Cereb Blood Flow Metab. 2007 Jun;27(6):1142-51. [2]. Sung IC, et, al. Neu2000, an NR2B-selective, Moderate NMDA Receptor Antagonist and Potent Spin Trapping Molecule for Stroke. Drug News Perspect. 2010 Nov; 23(9): 549-56. [3]. Nishant PV, et, al. Antioxidant Properties of Neu2000 on Mitochondrial Free Radicals and Oxidative Damage. Toxicol In Vitro. 2013 Mar; 27(2): 788-97. [4]. Nishant PV, et, al. Antioxidant Properties of Neu2000 on Mitochondrial Free Radicals and Oxidative Damage. Toxicol In Vitro. 2013 Mar; 27(2): 788-97.
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