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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
ILOPERIDONE

ILOPERIDONE


ATC N05AX14

ANTIPSYCHOTIC
DOPAMINE ANTAGONIST
SEROTONIN ANTOGONIST
SCHIZOPHRENIA
NERVOUS SYSTEM
SEROTONIN 5-HT2A DOPAMINE D2 AND D3 RECEPTORS (KI VALUES OF 5.6, 6.3, 7.1,NM, RESPECTIVELY). MODERATE AFFINITY FOR DOPAMINE D4, SEROTONIN 5-HT6 AND 5-HT7RECEPTORS AND NOREPINEPHRINE NEAPLHA1 RECEPTORS (KI VALUES OF 25, 43, 22, AND 36 NM RESPECTIVELY), AND LOW AFFINITY FOR THE SEROTONIN 5HT1A, DOPAMINE D1, AND HISTAMINE H1 RECEPTORS (KI VALUES OF 168, 216 AND 473 NM, RESPECTIVELY). NO APPRECIABLE AFFINITY (KI>1000 NM) FOR CHOLINERGIC MUSCARINIC RECEPTORS.

ORAL

VD 2070 LITER

PPB 95 PERCENT

Cl 74.5 LITER / HOUR

HT 18 HOUR

SOLUBILITY PRACTICALLY INSOLUBLE IN WATER

DOPAMINE D2 (KI = 6.3 NANOMOLAR)
SEROTONIN 5-HT2A (KI = 5.6 NANOMOLAR)
DOPAMINE D3 (KI = 7.1 NANOMOLAR)

DOPAMINE D2 RECEPTOR ANTAGONIST CHEMBL217 DOPAMINE D2 RECEPTOR P14416 D(2) DOPAMINE RECEPTOR HOMO SAPIENS MEMBRANE RECEPTOR 7TM1 SMALLMOL MONOAMINE RECEPTOR DOPAMINE RECEPTORANSM (in French)

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