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179411-93-9

179411-93-9 Structure

179411-93-9 Structure
IdentificationBack Directory
[Name]

SDZ 220-581 (hydrochloride)
[CAS]

179411-93-9
[Synonyms]

SDZ 220-581 (hydrochloride)
SDZ 220-581 hydrochloride >=98% (HPLC)
(S)-α-Amino-2-chloro-5-(phosphonomethyl)[1,1-biphenyl]-3-propanoic acid hydrochloride
(S)-alpha-Amino-2'-chloro-5-(phosphonomethyl)-[1,1'-biphenyl]-3-propanoic acid hydrochloride
[Molecular Formula]

C16H18Cl2NO5P
[MDL Number]

MFCD28124389
[MOL File]

179411-93-9.mol
[Molecular Weight]

406.198
Chemical PropertiesBack Directory
[storage temp. ]

room temp
[solubility ]

DMSO: soluble5mg/mL, clear (warmed)
[form ]

powder
[color ]

white to beige
[Optical Rotation]

[α]/D -5 to -8°, c = 1 in 1 M HCl
Safety DataBack Directory
[Hazard Codes ]

Xi
[Risk Statements ]

36/37/38
[Safety Statements ]

26
[WGK Germany ]

3
Hazard InformationBack Directory
[Uses]

SDZ 220-581 hydrochloride is an orally active, potent, competitive NMDA receptor antagonist with pKi value of 7.7[1].
[Biological Activity]

sdz 220-581 hydrochloride is a potent and competitive antagonist of nmda receptor with pki value of 7.7 [1].sdz 220-581 is a biphenyl-ap7-derivative. it is potent both in vitro and in vivo. sdz 220-581 binds with high affinity to the recognition site of nmda receptor. it does not bind to the strychnine-insensitive glycine site or the mk-801 site within the nmda receptor. in addition, sdz 220-581 shows no effect on a variety of other binding assays such as for dopamine, serotonin and adenosine [1].in the in vivo assay, the administration of sdz 220-581 protects the mice against the maximal electroshock-induced seizures (mes). in the rat mes model, sdz 220-581 also shows potent efficacy. moreover, sdz 220-581 can protect brain against quinolinic acid induced neuronal degeneration in rat. furthermore, a dose of 1.25mg/kg sdz 220-581 markedly reduces the cerebral infarct size in the focal cerebral ischemia model in rat [2].
[in vivo]

SDZ 220-581 (3.2-32 mg/kg; oral administration; for 24 hours; male OF-l mice) treatment dose-dependently protects mice against maximal electroshock seizures (MES). The time-course of protection by SDZ 220-581 is characterized by a rapid onset and long duration of action[1].

Animal Model:Male OF-l mice (18-26 g)[1]
Dosage:3.2 mg/kg, 10 mg/kg, 32 mg/kg
Administration:Oral administration; for 24 hours
Result:Dose-dependently protected mice against maximal electroshock seizures (MES) upon oral administration.
[storage]

Store at -20°C
[References]

[1] urwyler et al .biphenyl-derivatives of 2-amino-7-phosphono-heptanoic acid, a novel class of potent competitive n-methyl-d-aspartate receptor antagonists - ii. pharmacological characterization in vivo. neuropharmacology 1996, 35 655.
[2] urwyler s, campbell e, fricker g, et al. biphenyl-derivatives of 2-amino-7-phosphono-heptanoic acid, a novel class of potent competitiven-methyl-d-aspartate receptor antagonists—ii. pharmacological characterization in vivo[j]. neuropharmacology, 1996, 35(6): 655-669.
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