Antiemetic Receptor & Blood-Brain Barrier Simulator

Drug Presets

Pharmacokinetic Parameters

Dosage (mg) 10.0

Lipophilicity (LogP) 0.62

D2 Affinity Ki (nM) 28.3

5-HT3 Affinity Ki (nM) 820.0

P-Glycoprotein Substrate

Mechanism Notice: Fenestrated capillaries in the Area Postrema allow direct drug access to peripheral D2/5-HT3 receptors without crossing the Blood-Brain Barrier (BBB). High central D2 occupancy (>80%) triggers extrapyramidal symptoms, akathisia, and dysphoria.

Drug Molecule

Area Postrema (CTZ D2)

Central Brain (Central D2)

Nausea Inhibition (CTZ)

84.5%

CTZ D2/5-HT3 Combined Efficacy

CTZ D2 Occupancy

78.4%

Peripheral Receptor Saturation

Central D2 Occupancy

71.2%

BBB Crossing Penetration

CNS Side-Effect Risk

Moderate (Threshold Near)

BBB Crossing: 2.14 mg/hr