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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
ASENAPINE

ASENAPINE


ATC N05AH05

ANTIPSYCHOTICS
5-HT2A RECEPTOR AGONIST
NERVOUS SYSTEM
SCHIZOPHRENIA
BIPOLAR DISORDER
HIGH AFFINITY FOR SEROTONIN 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT5, 5-HT6, AND 5-HT7 RECEPTORS (KI VALUES OF 2.5, 4.0, 0.06, 0.16, 0.03, 1.6, 0.25, AND 0.13 NM), DOPAMINE D2, D3, D4, AND D1 RECEPTORS (KI VALUES OF 1.3, 0.42, 1.1, AND 1.4 NM), ALPHA1 AND ALPHA2-ADRENERGIC RECEPTORS (KI VALUES OF 1.2 AND 1.2 NM), AND HISTAMINE H1 RECEPTORS (KI VALUE 1.0 NM), AND MODERATE AFFINITY FOR H2 RECEPTORS (KI VALUE OF 6.2 NM)

SUBLINGUAL TRANSDERMAL

Cmax 14 NANOMOLAR (5 MILLIGRAM)

F 35 PERCENT (5 MILLIGRAM)

VD 1462 LITER (65 KILOGRAM)

PPB 95 PERCENT

Cl 52 LITER / HOUR

HT 24 HOUR

5-HT2A RECEPTOR (KI = 0.06 NANOMOLAR)
D2 RECEPTOR (KI = 1.3 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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