Fosphenytoin
Fosphenytoin is a prodrug of Phenytoin (HY-B0448). Fosphenytoin can be converted to Phenytoin in vivo, which blocks voltage-gated sodium channels in a voltage- and use-dependent manner, prolonging inactivation and slowing recovery. Fosphenytoin enhances GABA responses and, at higher concentrations, mildly modulates calcium channels and increases sodium-potassium ATPase activity. Fosphenytoin raises the afterdischarge threshold, reduces the severity and duration of seizures, alleviates pain-like behavior, and protects hippocampal pyramidal neurons after ischemia without altering GFAP immunoreactivity. Fosphenytoin can be used in research on acute herpes zoster pain, epilepsy, and cerebral ischemia.
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- CAS. Nr.: 93390-81-9
- Formel: C16H15N2O6P
- Molecular Weight:362.27
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Fosphenytoin (30 mg/kg; i.m.; single injection at 5 minutes after resuscitation) preserves hippocampal CA1 pyramidal neurons in rats after transient global ischemia[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (female, 6 weeks old at start, 18-20 g) bearing acute herpes zoster pain[2]
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Dosage:15 mg/kg; 30 mg/kg
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Administration:i.v.; single administration on day 6 after HSV-1 inoculation; before behavioral testing
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Result:On day 6 after HSV-1 inoculation, 15 mg/kg i.v. suppressed 0.17-g mechanical allodynia at 3 h after administration; both 15 and 30 mg/kg inhibited 1.20-g mechanical hyperalgesia around 2-4 h after administration.
Table 1 reported mean differences from vehicle for the 0.17-g ipsilateral response of 0.180 (15 mg/kg) and 0.119 (30 mg/kg), and for the 1.20-g ipsilateral response of 0.405 (15 mg/kg) and 0.299 (30 mg/kg).
15 and 30 mg/kg reduced HSV-1-induced spontaneous licking in a dose-dependent manner; the 30 mg/kg dose produced the greatest numerical suppression among all trial drugs.
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Animal Model:Wistar (female; Harlan-Winkelmann, Borchen, Germany)[4]
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Dosage:6.25, 12.5, 25, and 50 mg/kg (Phenytoin equivalents); 10.5 mg/kg (6.25 mg/kg Phenytoin equivalent), 20.9 mg/kg (12.5 mg/kg Phenytoin equivalent), 83.5 mg/kg (50 mg/kg Phenytoin equivalent)
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Administration:i.p.; single injection; 60 min before ADT determination
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Result:Dose-dependently increased the ADT.
The 10.5 mg/kg dose (6.25 mg/kg phenytoin equivalent) was without effect on ADT, whereas 20.9 mg/kg (12.5 mg/kg phenytoin equivalent) increased ADT by almost 100%.
At the highest dose tested (83.5 mg/kg; 50 mg/kg phenytoin equivalent), seizure severity and seizure duration at threshold were reduced; the decrease in seizure severity was small, and generalized seizures were still seen in most rats at ADT current.
Afterdischarge duration was not changed.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 93390-81-9
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Molecular Weight 362.27
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Formel C16H15N2O6P
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SMILES
O=C1N(COP(O)(O)=O)C(C(C2=CC=CC=C2)(C3=CC=CC=C3)N1)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Varia SA, et al. Phenytoin prodrugs III: water-soluble prodrugs for oral and/or parenteral use. J Pharm Sci. 1984;73(8):1068-1073. [Content Brief]
[2]. Takasaki I, et al. Fosphenytoin Alleviates Herpes Simplex Virus Infection-Induced Provoked and Spontaneous Pain-Like Behaviors in Mice. Biol Pharm Bull. 2022 Mar 1;45(3):360-363. [Content Brief]
[3]. Aleyadeh R, et al. Fosphenytoin. 2023 Aug 28. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2023 Jan–. [Content Brief]
[4]. Löscher W, et al. Anticonvulsant effect of fosphenytoin in amygdala-kindled rats: comparison with phenytoin. Epilepsy Res. 1998 Mar;30(1):69-76. [Content Brief]
[5]. Chan SA, et al. Fosphenytoin reduces hippocampal neuronal damage in rat following transient global ischemia. Acta Neurochir (Wien). 1998;140(2):175-80. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Fosphenytoin Related Classifications
HY-B1657 Related Classifications
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