Table 1.
Receptor-binding profile and metabolic risk of antipsychotic drugs.
| RECEPTOR BINDING PROFILE | RISK | |||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| D1 | D2 | D3 | D4 | H1 | H2 | H3 | 5-HT1A | 5-HT1B | 5-HT2A | 5-HT2B | 5-HT2C | 5-HT6 | 5-HT7 | M1 | M3 | α1 | α2A | α2B | α2C | Transporter | Weight Gain | Glucose Abn | Lipid Abn | |
| Olanzapine | ++ | ++ | ++ | ++ | +++ | ++ | + | + | +++ | ++ | ++ | +++ | ++ | ++ | ++ | ++ | + | ++ | ++ | ++++ | ++ | ++ | ||
| Zotepine | ++ | +++ | +++ | + | +++ | + | + | ++ | +++ | +++ | +++ | ++ | + | + | +++ | + | +++ | ++ | SERT, NET | +++/++++ | (LD) | (LD) | ||
| Clozapine | + | + | + | ++ | +++ | + | + | + | ++ | +++ | ++ | ++ | ++ | +++ | ++ | +++ | ++ | ++ | ++ | +++/++++ | ++ | ++ | ||
| Chlorpromazine | ++ | +++ | +++ | +++ | +++ | + | + | +++ | +++ | ++ | +++ | +++ | ++ | ++ | +++ | + | ++ | ++ | +++/++++ | +/++ | +/++ | |||
| Sertindole | +++ | +++ | +++ | + | + | ++ | ++++ | +++ | ++ | +++ | + | + | + | +++/++++ | +/++ | +/++ | ||||||||
| Iloperidone | + | +++ | +++ | ++ | + | ++ | ++ | +++ | ++ | + | + | +++ | + | + | ++ | +++/++++ | +/++ | +/++ | ||||||
| Risperidone | + | +++ | +++ | +++ | +++ | + | + | ++ | ++++ | ++ | ++ | +++ | +++ | ++ | ++ | +++ | +++ | +/++ | +/++ | |||||
| (Nor)quetiapine | + | + | + | +++ | ++ | ++ | + | + | ++ | + | + | ++ | + | + | ++ | NET | +++ | +/++ | ++ | |||||
| Paliperidone | + | +++ | +++ | +++ | ++ | + | + | ++ | +++ | ++ | + | +++ | +++ | +++ | +++ | +++ | +++ | +/++ | +/++ | |||||
| Asenapine | +++ | +++ | ++++ | +++ | +++ | +++ | +++ | +++ | ++++ | ++++ | ++++ | ++++ | ++++ | +++ | +++ | ++++ | +++ | ++ | + | + | ||||
| Amisulpride | +++ | +++ | +++ | ++ | ++ | ++ | + | ++(LD) | ||||||||||||||||
| Aripiprazole | +++ | +++ | + | ++ | +++ | + | ++ | ++++ | ++ | + | ++ | ++ | ++ | ++ | ++ | SERT | ++ | + | + | |||||
| Brexpiprazole | + | ++++ | +++ | +++ | ++ | ++++ | ++ | ++++ | +++ | + | ++ | +++ | +++ | ++ | ++ | ++++ | SERT, NET | +(LD) | +(LD) | +(LD) | ||||
| Cariprazine | ++++ | ++++ | ++ | +++ | ++ | ++++ | + | + | + | +(LD) | +(LD) | +(LD) | ||||||||||||
| Haloperidol | + | +++ | +++ | +++ | + | + | + | + | ++ | + | + | + | + | + | + | |||||||||
| Lurasidone | + | +++ | +++ | +++ | + | ++++ | ++ | ++ | +++ | + | + | + | ||||||||||||
| Ziprasidone | + | +++ | +++ | ++ | ++ | +++ | +++ | ++++ | ++ | ++++ | ++ | +++ | ++ | + | ++ | ++ | SERT, NET | + | + | + | ||||
A. Receptor-binding profile. Antagonism and inverse agonism are indicated by blue color whereas partial agonism by yellow. The number of crosses and color intensity are correlated to binding affinity. Quetiapine is demonstrated along with norquetiapine, a metabolite of the drug with distinct binding profile. 100 < Ki < 1000: + weak association. 10< Ki < 100: ++ moderate association. 1< Ki < 10: +++ strong association. 1 > Ki: ++++ very strong association. [Data taken from [30, 43-45, 48-50], PDSP [47] and iPHACE [46] databases]. B. Metabolic risk. The number of crosses are correlated to risk of weight gain (maximum ++++), glucose and lipid abnormalities (maximum ++). (LD): Limited Data, abn: abnormalities. [Data taken from [4, 12, 14-20].