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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
CARIPRAZINE (has an active metabolite)

CARIPRAZINE


ATC N05AX15

NERVOUS SYSTEM
ANTIPSYCHOTIC
TREATMENT OF SCHIZOPHRENIA
PARTIAL AGONIST DOPAMINE D2 RECEPTOR (KI = 0.49 NANOMOLAR)
PARTIAL AGONIST SEROTONIN 5-HT1A RECEPTOR (KI = 2.6 NANOMOLAR)
ANTAGONIST 5-HT2A RECEPTOR (KI = 18.8 NANOMOLAR)
HISTAMINE H1 RECEPTOR (KI = 23.2 NANOMOLAR)

ORAL

Cmax 20 NANOMOLAR

Tmax 4.5 HOUR

PPB 94 PERCENT

HT 72 HOUR

DOPAMINE D2 RECEPTOR
5-HT1A RECEPTOR

PDB 7VOD (CRYSTAL STRUCTURE OF 5-HT2AR IN COMPLEX WITH CARIPRAZINE)

LIGAND CODE = 7RU (link to the list of PDB complexes)

Download experimental 3D coordinates of 7RU with added hydrogens

D(2) dopamine receptor UNIPROT P14416 DRD2 -- 5-hydroxytryptamine receptor 1A UNIPROT P08908 HTR1A

more at DrugCentral

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ANSM (in French)

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SIDER side effects

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ChEMBL
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