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Receptor occupancy thresholds

Interactive data visualization

RECEPTOR / TRANSPORTERHUMAN PET RECEPTOR OCCUPANCY (%)CLINICAL EFFECTS0%10%20%30%40%50%60%70%80%90%100%D2 Striatal (Antagonist)78–95%Loose binding (clozapine/quetiapine)Antipsychotic windowEPS & hyperprolactinemiaD2 Striatal (Partial Agonist)80–95%Aripiprazole/cariprazine window (no EPS)5-HT1A (Partial Agonist)Raphe suppression & anxiolysisAutoreceptor blockade (pindolol)5-HT2A (Antagonist)80–95%Slow-wave sleep restorationSGA / pimavanserin saturationAlpha-1 (Antagonist)70–95%Orthostasis & hyperarousal bluntingMarked orthostatic hypotensionMuscarinic M1 (Antagonist)50–90%Cognitive blunting onsetDelirium & anticholinergic toxicityH1 Histamine (Antagonist)50–95%Non-sedatingMild drowsinessHeavy sedation & hangoverSERT (Transporter)75–90%Multimodal antidepressant synergySSRI/SNRI monotherapy thresholdNET (Transporter)70–90%SNRI antidepressant synergyAtomoxetine ADHD efficacyDAT (Transporter)Bupropion rangeADHD efficacy (fast IV: euphoria)VMAT2 (Transporter)88–98%Tardive dyskinesia efficacyParkinsonism & akathisiaGABA-A (BZD PAM)Anxiolysis & anticonvulsantHypnosis, amnesia & ataxiaMu-Opioid MOR (Buprenorphine)Opioid withdrawal suppressionAgonist euphoria blockadeOrexin OX2R (DORA)Morning wakefulnessNighttime sleep maintenanceNK1 (Substance P)90–98%Central antiemetic saturation90%

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