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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
LUMATEPERONE

LUMATEPERONE


ATC N05AD10

NERVOUS SYSTEM
ANTIPSYCHOTIC INDICATED FOR THE TREATMENT OF SCHIZOPHRENIA IN ADULTS
ACTIVITY COULD BE ANTAGONISTIC ACTIVITY AT CENTRAL SEROTONIN 5-HT2A RECEPTORS (KI = 0.54 NM) AND DOPAMINE D2 RECEPTORS (KI = 32 NM)

ORAL

Tmax 1.5 HOUR

F 4.4 PERCENT

VD 266.5 LITER (65 KILOGRAM)

PPB 97.4 PERCENT

Cl 27.9 LITER / HOUR

HT 18 HOUR

5-HT2A RECEPTORS
DOPAMINE D2 RECEPTORS

PDB 7WC8 (CRYSTAL STRUCTURE OF SEROTONIN 2A RECEPTOR IN COMPLEX WITH LUMATEPERONE)

LIGAND CODE = 92S (link to the list of PDB complexes)

Download experimental 3D coordinates of 92S with added hydrogens

D(2) dopamine receptor UNIPROT P14416 DRD2 -- 5-hydroxytryptamine receptor 2A UNIPROT P28223 HTR2A

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