| Identification | Back Directory | [Name]
Gamma-homolinolenic-acid | [CAS]
916214-57-8 | [Synonyms]
Neu2000potassium
640290-67-1 (free)
Nelonemdaz (potassium)
Salfaprodil 916214-57-8
Gamma-homolinolenic-acid | [Molecular Formula]
C15H9F7KNO3 | [MDL Number]
MFCD32874126 | [MOL File]
916214-57-8.mol | [Molecular Weight]
423.33 |
| Hazard Information | Back Directory | [Uses]
Nelonemdaz (Salfaprodil) potassium is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz potassium is also a free radical scavenger. Nelonemdaz potassium has excellent neuroprotection against NMDA- and free radical-induced cell death[1][2]. | [in vivo]
Nelonemdaz potassium (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].
Nelonemdaz potassium (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.
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| 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.
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| [IC 50]
NMDA Receptor | [References]
[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. DOI:10.1038/sj.jcbfm.9600418
[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. DOI:10.1358/dnp.2010.23.9.1513493
[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. DOI:10.1016/j.tiv.2012.12.011 |
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