|
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.
|
|
|