TABLE 3. Dissociation constants and catalepsy doses.
  D2* D3* D4*
5-HT-2A*
5-HT-6#dose for

K

K

K

K

Ki

catalepsy**

 

nM

nM

nM

nM

nM

mg/kg rat

1.

Amoxapine

20

 

2

0.5

7 (a)

2.

Chlorpromazine

0.66

0.85

1.15

1.8

8600

2.7

[3H]Chlorpromazine

0.7

 

1.2

3.

Clozapine

44

150

1.6

3.5

12.5

161 (b)

[3H]clozapine

   

1.6

3.5

4.

Epidepride

0.01

 

5.

Fluphenazine

0.32

0.11

50

3.2

7540

0.13

6.

Glaxo 1192U90

4(c)

 

0.8 (c)

1.5 (d)

192 (b)

7.

Haloperidol

0.35

6.2

0.84

46

7540

0.5

[3H]Haloperidol

0.4

 

0.85

8.

Iloperidone

3.5

14

2.5

0.12

10

30.7

9.

Isoclozapine

6

12

5.8

1.8

35

3.2

##

Isoloxapine

6

 

4.5

3.7

20.5

4.1

##

Loxapine

5.2

18

7.8

1.8

17.5

0.17

##

"MDL 100,907"

9000

 

0.14

##

Melperone

88

160

410

150

6700

22.2

##

Molindone

6

20

2400

5800

3260

1.1

##

Norclozapine

100

 

20

##

Olanzapine

3

8

1.6

3

73

18.7

[3H]Olanzapine

2.7

 

1.6

1.6

##

Perlapine

60

100

30

13

478

33.6

##

Raclopride

0.64

2

620

3900

2600

0.4

##

Remoxipride

30

640

2800

5200

2800

##

Risperidone

0.3

2.6

0.25

0.21

4300

5.7

##

Ritanserin

10

 

30

0.54

120

nil at 40

##

Seroquel

78

150

3000

110

6890

22

##

Sertindole

1.5

2.5

~1

0.3

3230

6

[3H]Sertindole

0.95

 

0.85

0.3

##

S-sulpiride

5

6.4

200

##

Thioridazine

0.4

1.5

1.5

1.1

156

4.9

##

Trifluperazine

0.96

0.45

44

7.6

139

0.5

##

Ziprasidone

1.2

1.1

0.8

3.4

7800


"*: Radioligand-independent K values on human cloned D2, D3, D4 or 5-HT2A receptors"

"**: Refs. (164), (166)."

#: Human serotonin-6 receptors in Sf9 cells; 2 nM [3H]LSD (Kd = 1.2 nM)

a: Ref. (56).

b: Mouse ED50 (Ref. (136)

"c: Extrapolated from Ref. (36), using method of Refs. (164), (166)."

d: From Ref. (67) on rat cortex.

 

published 2000