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Table 1 Antipsychotic affinities ( K i ) and target daily dosing range in schizophrenia [7, 911]

From: Evidence review and clinical guidance for the use of ziprasidone in Canada

Antipsychotic Very high High Moderate Low Negligible
daily dose (K i  < 1.0) (K i 1.0–9.9) (K i 10–99) (K i 100–999) (K i ≥1000)
Ziprasidone 5HT2a (0.4) 5HT1a (2.5) ** α1 (13) D1 (130) M1 (5100)
120-160 mg 5HT2c (0.7) D2 (3.1) D4 (32) α2 (310)  
   D3 (7.2) H1 (47)   
   5HT7 (9.3) NAuptake (48)   
    5HTuptake (53)   
    5HT6 (76)   
Aripiprazole D2(0.3) ** 5HT1a (1.7) ** D4 (44)   M1 (>1000)
15-30 mg D3(0.8) 5HT2a(3.4) 5HT2c (15)   
    5HT7 (39)   
    α1 (57)   
    H1 (61)   
    5HTuptake (98)   
Risperidone 5HT2a(0.3) α1 (1.4) 5HT2c (10) 5HT1A(210) 5HTuptake (1400)
4-6 mg   D2 (2.2) H1 (19) D1(580) 5HT6 (2000)
   5HT7 (3.0)    M1 (2800)
   D3 (9.6)    NAuptake (28,000)
   D4 (8.5)    
   α2 (5.1)    
Paliperidone   5HT2a(1.0) α2 (17) 5HT1A(590) M1 (3570)
6-9 mg   5HT7 (1.3) H1 (32) D1(670)  
   α1 (4.0) D4 (30)   
   D2 (4.8) 5HT2c (71)   
   D3 (6.9)    
Olanzapine   H1(2.8) 5HT2c (10) α2 (170) 5HT1a (2100)
10-20 mg   5HT2a(3.3) 5HT6 (10) 5HT7 (250) NAuptake (2000)
   M1(4.7) D2 (20)   5HTuptake (>15,000)
    D3 (45)   
    D1 (52)   
    α1 (54)   
    D4 (60)   
Clozapine   H1(1.8) 5HT6 (11) D4 (54) 5HTuptake (3900)
200-500 mg   M1(1.8) 5HT2c (17) D2 (130)  
   α1 (4.0) α2 (33) 5HT1a (140) **  
   5HT2a (8.9) 5HT7 (66) D3 (240)  
     D1 (290)  
     NAuptake (390) *  
Quetiapine   H1 (8.7) α1 (15) M1 (100) α2 (1000)
400-800 mg     D2 (180) D1 (1300)
     5HT2a (220) 5HT2c (1400)
     5HT1a (230) ** 5HT7 (1800)
     D3 (320) D4 (2200)
     NAuptake (680)* 5HT6 (4100)
      5HTuptake (>18,000)
  1. * Quetiapine’s active metabolite N-desalkyl-quetiapine inhibits NA uptake (35 nM). Clozapine’s active metabolite N-desmethyl-clozapine also has a low affinity for NA uptake inhibition.
  2. ** Partial agonist. Quetiapine’s active metabolite N-desalkyl-quetiapine is a 5HT1a partial agonist (191 nM). Clozapine’s active metabolite N-desmethyl-clozapine is a 5HT1a partial agonist (105 nM).
  3. 5-HT: serotonin; D: dopamine; H: histamine; M: muscarinic cholinergic; α: alpha-adrenergic.
  4. Lower values (shown in parentheses) indicate higher affinities at receptors or greater inhibition of pre-synaptic neurotransmitter uptake. Antipsychotics used in relatively small daily doses are unlikely to have clinical effects at receptors for which they have low affinity, unlike antipsychotics used at high daily doses.
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