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Phenytoin

MCE China：Phenytoin

Brand：MedChemExpress (MCE)

Cat. No.HY-B0448

CAS：57-41-0

Synonyms：5,5-Diphenylhydantoin

Purity：99.91%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice.

In Vitro：Phenytoin is an antiepileptic drug. It is useful to partial seizures and generalized tonic-clonic seizures but not primary generalized seizures such as absence seizures or myoclonic seizures. Phenytoin is believed to protect against seizures by causing voltage-dependent block of voltage-gated sodium channels[2]. Phenytoin has low affinity for resting sodium channels at hyperpolarized membrane potentials[3]. When neurons are depolarized and the channels transition into the open and inactivated states, greater binding and block occur. The inhibitory potency is strongly use dependent, so that block accumulates with prolonged or repetitive activation, such as occurs during a seizure discharge. The blocking of sodium channels by phenytoin is of slow onset. The time course of fast sodium currents is therefore not altered in the presence of the drug and action potentials evoked by synaptic depolarizations of ordinary duration are not blocked. Thus phenytoin is able to selectively inhibit pathological hyperexcitability in epilepsy without unduly impairing ongoing activity. Phenytoin also blocks persistent sodium current and this may be of particular importance in seizure control. Phenytoin is a class 1b antiarrhythmic[4].

In Vivo：Phenytoin can induce a model of gingival hyperplasia in mice[6]. .f12{ font-size: 12px; } .fwb{ font-weight: bold; } .lh22{ line-height: 22px;; } .lh23 { line-height: 23px; } .pl13{ padding-left: 13px;; } .part { margin-top: 18px; } .mold-first-tit { width: 100%; height: 44px; line-height: 44px; background: #F9F7FB; border-bottom: 1px solid #EBE4F6; padding-left: 16px; box-sizing: border-box; margin-bottom: 17px; } .mold-second-tit:before { content:""; width: 6px; height: 6px; display: inline-block; border-radius: 50%; background: rgba(255,102,0,0.4); margin-right: 12px; position: relative; top: -3px; } .lft-border { border-left: 1px dotted #EBE4F6; padding-right: 12px; margin-left: 3px; box-sizing: border-box; padding-bottom: 12px; } /* .part .dec:last-child { border-bottom: 0; } */ .dec { margin: 10px 15px 0; padding-bottom: 10px; border-bottom: 1px dashed #EBE4F6; } .btm-border { border-left: 1px dashed #EBE4F6; } .text-bg { margin-top: 10px; background: #FFFBF1; padding: 14px; border-bottom: 0; position: relative; } .text-note-bg { margin-top: 10px; background: #FFFDF7; padding: 12px; border-bottom: 0; position: relative; } .text-note { width: 51px; height: 20px; line-height: 20px; background: #FFE2AA; text-align: center; border-radius: 0 0 8px 0; position: absolute; top: 0; left: 0; } .text-note-dec { margin-top: 15px;; } Induction of Gingival Hyperplasia in Mice[6] Background Phenytoin induced gingival overgrowth, a side effect with multifactorial aetiology, is characterized by an increase in the volume of extracellular tissues, particularly collagenous components, with varying degrees of inflammation. Specific Mmodeling Methods Mice: BALB/cByJ • male • 8 week oldAdministration: 30 mg/kg • miniosmotic pumps • 0.5-μL/h • 2 weeks Note (1) Mice are housed for 1 week before any procedure for acclimation.(2) Pumps are replaced every 2 weeks throughout the 12-week experimental period.(3) Mice are then euthanized and heads are immediately placed in freshly made 4% paraformaldehyde for 24 hours for fixation. Modeling Indicators Morphology: Gingival overgrowth was apparent in the maxillary anterior gingival tissue of mice; Increased the papillary height and area.Histomorphometry: Increased epithelial thickness and area in the maxillary anterior zone.Molecular changes: Ccn2 is overexpressed in all regions of the epithelium; TGF-β1 and LOXL2 is overexpressed in both epithelial and connective tissues. Correlated Product(s): Cyclosporine A (HY-B0579) Opposite Product(s): Lovastatin (HY-N0504)

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References：

[1]. Michaela Nelson, et al. The sodium channel-blocking antiepileptic drug phenytoin inhibits breast tumour growth and metastasis. Mol Cancer. 2015 Jan 27;14(1):13.  [Content Brief]

[2]. Rogawski, M.A. and W. Loscher, The neurobiology of antiepileptic drugs. Nat Rev Neurosci, 2004. 5(7): p. 553-64.  [Content Brief]

[3]. Porter, R.J., et al., Mechanisms of action of antiseizure drugs. Handb Clin Neurol, 2012. 108: p. 663-81.  [Content Brief]

[4]. Balaji, S., Medical therapy for sudden death. Pediatr Clin North Am, 2004. 51(5): p. 1379-87.  [Content Brief]

[5]. Assaggaf MA, et al. Prevention of phenytoin-induced gingival overgrowth by lovastatin in mice. Am J Pathol. 2015 Jun;185(6):1588-99.  [Content Brief]