PeraMpanel Struktur

PeraMpanel

Bezeichnung:PeraMpanel

CAS-Nr380917-97-5

Englisch Name:PeraMpanel

CBNumberCB12598797

SummenformelC23H15N3O

Molgewicht349.38

MOL-Datei380917-97-5.mol

PeraMpanel physikalisch-chemischer Eigenschaften

Siedepunkt	619.1±55.0 °C(Predicted)
Dichte	1.31±0.1 g/cm3(Predicted)
Löslichkeit	Soluble in DMSO
Aggregatzustand	Powder
pka	4.73±0.19(Predicted)

Gefahreninformationscode (GHS)

PeraMpanel Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
In October 2012, the US FDA approved perampanel for the treatment of partial onset seizures in epileptic patients who are at least 12 years old. Perampanel is the first AMPA receptor antagonist to receive FDA approval as an AED. AMPA glutamate receptors are found primarily on postsynaptic neurons in the brain. As a selective, noncompetitive antagonist of AMPA, parampanel prevents ion channel opening and reduces propagation of action potential. Parampanel was discovered through lead optimization of a commercially available compound, 2,4-diphenyl-4H-[1,3,4]oxadiazin-5-one, which was identified by high-throughput screening of a compound collection employing a rat cortical neuron AMPA-induced cell-death assay. Modifications of aromatic rings at positions 1, 3, and 5 while changing the core to pyridone led to parampanel which inhibited AMPA-induced calcium influx (IC₅₀=60 nM). Parampanel had a minimum effective oral dose of 2 mg/kg in an AMPA-induced mouse seizure model. The synthesis of parampanel was accomplished via a 6-step route utilizing Suzuki–Miyaura couplings and modified Ullmann reactions for incorporation of aryl groups.
Originator
Eisai (Japan)
Verwenden
Isotope labelled Perampanel (P285520), is an antiepileptic drug. It inhibits α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA)-induced increases in intracellular Ca2+ and selectively blocks AMPA receptor-mediated synaptic transmission, thus reducing neuronal excitation.
Definition
ChEBI: A member of the class of bipyridines that is 2,3'-bipyridin-6'-one substituted at positions 1' and 5' by phenyl and 2-cyanophenyl groups respectively. Used as an adjunctive therapy for the treatment of partial-onset seizures in patients with epilepsy.
Trademarks
Fycompa
Clinical Use
Selective AMPA-type glutamate receptor antagonist:
Antiepileptic
Arzneimittelwechselwirkung
Potentially hazardous interactions with other drugs
Antidepressants: anticonvulsant effect antagonised; avoid with St John’s wort.
Antiepileptics: concentration reduced by carbamazepine, fosphenytoin, oxcarbazepine and phenytoin.
Antimalarials: anticonvulsant effect antagonised by mefloquine.
Antipsychotics: anticonvulsant effect antagonised.
Orlistat: possibly increased risk of convulsions.
Progestogens: high-dose perampanel reduces plasma concentration of progestogens (possibly reduced contraceptive effect).
Stoffwechsel
Extensively metabolised via primary oxidation via the cytochrome P450 isoenzyme CYP3A sub family and sequential glucuronidation.
Perampanel is excreted in the urine and faeces mainly as oxidative and conjugated metabolites.

PeraMpanel Upstream-Materialien And Downstream Produkte

PeraMpanel Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

380917-97-5, PeraMpanel Verwandte Suche:

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