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Fosphenytoin disodium

(Synonyms: 磷苯妥英钠) 目录号 : GC33678

A prodrug of phenytoin

Fosphenytoin disodium Chemical Structure

Cas No.:92134-98-0

规格 价格 库存 购买数量
5mg
¥284.00
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10mM (in 1mL Water)
¥313.00
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25mg
¥796.00
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50mg
¥1,080.00
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100mg
¥1,710.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Animal experiment:

A total of four groups of rats, including normal (n=2), sham operated (n=2), ischemia with saline-treated (n=2), and ischemia with fosphenytoin-treated (n=2), are studied. Postischemic rats in saline-treated and fosphenytoin-treated groups receive a single i.m. injection of saline or fosphenytoin (30 mg/kg), respectively, in the right hind limb 5 minutes after resuscitation. Sham-operated animals are treated similarly except for chest compression. All rats are killed on the 7th postischemic day by decapitation. Brains are immediately removed, bisected longitudinally, and immersed in 4% buffered neutral formaldehyde containing 0.25% glutaraldehyde for a minimum of 2 days at 4°C. Portions of the brain containing the dorsal hippocampus are coronally sectioned with a vibratome at 40 μm. With the aid of a dissecting microscope, rectangular blocks of about 1 mm2 in size encompassing the mid-CA1 region from sections that approximate Bregma -3.6 are dissected, postfixed in 2% osmium tetroxide, and dehydrated in ascending concentrations of ethanol before being embedded in Araldite 502. Sections of polymerized blocks 1 μm thick are cut and toluidine blue stained for light microscopic examination.

References:

[1]. Chan SA, et al. Fosphenytoin reduces hippocampal neuronal damage in rat following transient global ischemia. Acta Neurochir (Wien). 1998;140(2):175-80.
[2]. Loscher W, et al. Anticonvulsant effect of fosphenytoin in amygdala-kindled rats: comparison with phenytoin. Epilepsy Res. 1998 Mar;30(1):69-76.

产品描述

Fosphenytoin is a prodrug of phenytoin that is rapidly converted to phenytoin, a voltage-gated sodium channel blocker, in vivo.1,2,3 It induces less tissue damage compared with two other phenytoin prodrugs in rats following subcutaneous and intramuscular administration.1 Fosphenytoin has anticonvulsant activity in a mouse model of maximal electroshock seizures similar to that of phenytoin (ED50s = 16 and 8 mg/kg, respectively).2 It also has antiarrhythmic activity in isolated guinea pig atria and in anesthetized dogs. Formulations containing fosphenytoin have been used in the treatment of status epilepticus.

1.Varia, S.A., and Stella, V.J.Phenytoin prodrugs VI: In vivo evaluation of a phosphate ester prodrug of phenytoin after parenteral administration to ratsJ. Pharm. Sci.73(8)1087-1090(1984) 2.Smith, R.D., Brown, B.S., Maher, R.W., et al.Pharmacology of ACC-9653 (phenytoin prodrug)Epilepsia30(Suppl. 2)S15-S21(1989) 3.Boucher, B.A.Fosphenytoin: A novel phenytoin prodrugPharmacotherapy16(5)777-791(1996)

Chemical Properties

Cas No. 92134-98-0 SDF
别名 磷苯妥英钠
Canonical SMILES O=C1N(COP([O-])([O-])=O)C(C(C2=CC=CC=C2)(C3=CC=CC=C3)N1)=O.[Na+].[Na+]
分子式 C16H13N2Na2O6P 分子量 406.24
溶解度 Water : ≥ 100 mg/mL (246.16 mM) 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.4616 mL 12.308 mL 24.616 mL
5 mM 0.4923 mL 2.4616 mL 4.9232 mL
10 mM 0.2462 mL 1.2308 mL 2.4616 mL
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