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1 INNClassRoute (list)PK parameters= Cmax; Tmax; F: bioavailability; t1/2: half-life; VD: volume of distribution; Cl: clearance; PPB: plasma protein binding;(EQN means that value was calculated using VD=(Cl*t1/2)/0.693)Primary Target and PDB code of Protein-Drug complexTargets from DrugCentral Links
RILUZOLE

RILUZOLE


ATC N07XX02

NERVOUS SYSTEM
NEUROPROTECTIVE
INHIBITORY EFFECT ON GLUTAMATE RELEASE
PARTIAL INACTIVATION OF VOLTAGE-DEPENDENT SODIUM CHANNELS (PMID25548669)
SEDATIVES
MYORELAXANT
TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS (ALS)
ACTIVATES SK CHANNELS BUT NOT BK CHANNELS

ORAL

Cmax 739 NANOMOLAR

F 60 PERCENT

VD 245 LITER

PPB 96 PERCENT

HT 12 HOUR

SOLUBILITY VERY SLIGHTLY SOLUBLE IN WATER

SMALL-CONDUCTANCE CALCIUM-ACTIVATED POTASSIUM (SK) CHANNELS (PMID26311432)

PDB 5V02 (A POSITIVE ALLOSTERIC MODULATOR BINDING POCKET IN SK2 ION CHANNELS IS SHARED BY RILUZOLE AND CYPPA)

LIGAND CODE = 657 (link to the list of PDB complexes)

Download experimental 3D coordinates of 657 with added hydrogens

Sodium channel protein type 5 subunit alpha UNIPROT Q14524 SCN5A

more at DrugCentral

EMA

ANSM (in French)

Inxight Drugs
Dailymed
Drugs.com

SIDER side effects

Chemical Probes Portal

ChEMBL
BindingDB
DrugBank



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