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Table 1 Antipsychotic affinities ( K i ) and target daily dosing range in schizophrenia [7, 9–11]

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.