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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
DARIDOREXANT

DARIDOREXANT


ATC N05CJ03

NERVOUS SYSTEM
OREXIN RECEPTOR ANTAGONIST
TREATMENT OF INSOMNIA
OREXIN-1 RECEPTOR (KI=0.47 NANOMOLAR) OREXIN-2 RECEPTOR (KI=0.93 NANOMOLAR)

ORAL

Tmax 1.5 HOUR

F 62 PERCENT

VD 31 LITER

PPB 99.7 PERCENT

HT 8 HOUR

SOLUBILITY VERY SLIGHTLY SOLUBLE IN WATER

OREXIN-1 RECEPTOR (OX1R)
OREXIN-2 RECEPTOR (OX2R)

PDB 6TP3 (CRYSTAL STRUCTURE OF THE OREXIN-1 RECEPTOR IN COMPLEX WITH DARIDOREXANT)

LIGAND CODE = NS2 (link to the list of PDB complexes)

Download experimental 3D coordinates of NS2 with added hydrogens

Orexin Hypocretin receptor type 1 UNIPROT O43613 HCRTR1 -- Orexin receptor type 2 UNIPROT O43614 HCRTR2

more at DrugCentral

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