Ligand |
|
|
|
|
|
|
|
|
|
|
|
[3H]nemonapride
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.9
|
pKd
|
77
|
|
⤷ |
pKd
10.9
[77]
|
[3H]spiperone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
10.2
|
pKd
|
24,52,141
|
|
⤷ |
pKd
10.2
(Kd 5.7x10-11 M)
[24,52,141]
|
[3H]raclopride
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.9
|
pKd
|
67
|
|
⤷ |
pKd
8.9
(Kd 1.2x10-9 M)
[67]
|
[3H]N-methylspiperone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
10.7
|
pKi
|
104
|
|
⤷ |
pKi
10.7
[104]
|
benperidol
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.6
|
pKi
|
111
|
|
⤷ |
pKi
10.6
(Ki 2.7x10-11 M)
[111]
|
blonanserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.9
|
pKi
|
90
|
|
⤷ |
pKi
9.9
(Ki 1.4x10-10 M)
[90]
|
pipotiazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.7
|
pKi
|
119
|
|
⤷ |
pKi
9.7
(Ki 2x10-10 M)
[119]
|
risperidone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.4
|
pKi
|
11
|
|
⤷ |
pKi
9.4
(Ki 4.4x10-10 M)
[11]
|
perphenazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.9 – 9.6
|
pKi
|
64,108
|
|
⤷ |
pKi
8.9 – 9.6
(Ki 1.4x10-9 – 2.6x10-10 M)
[64,108]
|
perospirone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.2
|
pKi
|
109
|
|
⤷ |
pKi
9.2
(Ki 6x10-10 M)
[109]
|
eticlopride
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.2
|
pKi
|
75,125
|
|
⤷ |
pKi
9.2
[75,125]
|
trifluoperazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.9 – 9.0
|
pKi
|
64,110
|
|
⤷ |
pKi
8.9 – 9.0
(Ki 1.3x10-9 – 9.6x10-10 M)
[64,110]
|
asenapine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.9
|
pKi
|
114
|
|
⤷ |
pKi
8.9
(Ki 1.2x10-9 M)
[114]
|
terguride
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.9
|
pKi
|
86
|
|
⤷ |
pKi
8.9
[86]
|
spiperone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.4 – 9.4
|
pKi
|
75,87,120,125
|
|
⤷ |
pKi
8.4 – 9.4
[75,87,120,125]
|
fluphenazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.8
|
pKi
|
101
|
|
⤷ |
pKi
8.8
(Ki 1.44x10-9 M)
[101]
|
flupentixol
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.8
|
pKi
|
41
|
|
⤷ |
pKi
8.8
(Ki 1.5x10-9 M)
[41]
|
nafadotride
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.8
|
pKi
|
104
|
|
⤷ |
pKi
8.8
[104]
|
lurasidone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.8
|
pKi
|
55
|
|
⤷ |
pKi
8.8
(Ki 1.68x10-9 M)
[55]
|
olanzapine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.7
|
pKi
|
11
|
|
⤷ |
pKi
8.7
(Ki 2.1x10-9 M)
[11]
|
mesoridazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.7
|
pKi
|
32
|
|
⤷ |
pKi
8.7
(Ki 2.2x10-9 M)
[32]
|
roxindole
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6
|
pKi
|
86
|
|
⤷ |
pKi
8.6
[86]
|
ziprasidone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6
|
pKi
|
11
|
|
⤷ |
pKi
8.6
(Ki 2.8x10-9 M)
[11]
|
chlorprothixene
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.5
|
pKi
|
130
|
|
⤷ |
pKi
8.5
(Ki 2.96x10-9 M)
[130]
|
nafadotride
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.5
|
pKi
|
103
|
|
⤷ |
pKi
8.5
[103]
|
raclopride
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.7 – 9.3
|
pKi
|
104,120
|
|
⤷ |
pKi
7.7 – 9.3
[104,120]
|
domperidone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.5
|
pKi
|
120
|
|
⤷ |
pKi
8.5
[120]
|
sertindole
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.0 – 8.9
|
pKi
|
63-64,108
|
|
⤷ |
pKi
8.0 – 8.9
(Ki 9.1x10-9 – 1.2x10-9 M)
[63-64,108]
|
prochlorperazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.4
|
pKi
|
13
|
|
⤷ |
pKi
8.4
(Ki 3.61x10-9 M)
[13]
|
haloperidol
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.3
|
pKi
|
120
|
|
⤷ |
pKi
8.3
[120]
|
(+)-sulpiride
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.2
|
pKi
|
41
|
|
⤷ |
pKi
8.2
(Ki 6x10-9 M)
[41]
|
L-741,626
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.9 – 8.5
|
pKi
|
47,66
|
|
⤷ |
pKi
7.9 – 8.5
[47,66]
|
domperidone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.9 – 8.4
|
pKi
|
41,118
|
|
⤷ |
pKi
7.9 – 8.4
(Ki 1.26x10-8 – 3.98x10-9 M)
[41,118]
|
loxapine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.9 – 8.3
|
pKi
|
64,110
|
|
⤷ |
pKi
7.9 – 8.3
(Ki 1.2x10-8 – 5x10-9 M)
[64,110]
|
(+)-butaclamol
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.5 – 8.7
|
pKi
|
25,41,75,125
|
|
⤷ |
pKi
7.5 – 8.7
[25,41,75,125]
|
haloperidol
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.4 – 8.8
|
pKi
|
41,75,85,118,126
|
|
⤷ |
pKi
7.4 – 8.8
[41,75,85,118,126]
|
raclopride
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.0
|
pKi
|
87
|
|
⤷ |
pKi
8.0
(Ki 1x10-8 M)
[87]
|
zotepine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.0
|
pKi
|
107
|
|
⤷ |
pKi
8.0
(Ki 1.1x10-8 M)
[107]
|
(-)-stepholidine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.9
|
pKi
|
84
|
|
⤷ |
pKi
7.9
(Ki 1.16x10-8 M)
[84]
|
pimozide
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.0 – 8.8
|
pKi
|
41,118
|
|
⤷ |
pKi
7.0 – 8.8
[41,118]
|
amisulpride
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.8 – 8.0
|
pKi
|
79,118,120
|
|
⤷ |
pKi
7.9 – 8.0
[79,118]
pKi
7.8
[120]
|
cinnarizine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.9
|
pKi
|
58
|
|
⤷ |
pKi
7.9
(Ki 1.32x10-8 M)
[58]
|
flunarizine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
6.9 – 8.4
|
pKi
|
4,58
|
|
⤷ |
pKi
6.9 – 8.4
(Ki 1.12x10-7 – 3.96x10-9 M)
[4,58]
|
pimozide
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.6
|
pKi
|
120
|
|
⤷ |
pKi
7.6
[120]
|
sulpiride
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.2 – 7.9
|
pKi
|
25
|
|
⤷ |
pKi
7.2 – 7.9
(Ki 6x10-8 – 1.2x10-8 M)
[25]
|
metoclopramide
|
|
|
|
|
|
|
|
|
|
|
Mm |
Antagonist |
7.5
|
pKi
|
81
|
|
⤷ |
pKi
7.5
(Ki 2.88x10-8 M)
[81]
|
chlorpromazine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.5
|
pKi
|
120
|
|
⤷ |
pKi
7.5
[120]
|
lumateperone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.5
|
pKi
|
73,117
|
|
⤷ |
pKi
7.5
(Ki 3.2x10-8 M)
[73,117]
|
chlorpromazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.0 – 7.6
|
pKi
|
41,118
|
|
⤷ |
pKi
7.0 – 7.6
[41,118]
|
quetiapine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.2
|
pKi
|
11
|
|
⤷ |
pKi
7.2
(Ki 6.9x10-8 M)
[11]
|
(-)-sulpiride
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.3 – 8.0
|
pKi
|
41,118,125
|
|
⤷ |
pKi
6.3 – 8.0
(Ki 5.2x10-7 – 1x10-8 M)
[41,118,125]
|
R-VK4-40
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.1
|
pKi
|
57
|
|
⤷ |
pKi
7.1
(Ki 7.58x10-8 M)
[57]
|
(+)-sulpiride
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.0
|
pKi
|
120
|
|
⤷ |
pKi
7.0
[120]
|
ML321
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.0
|
pKi
|
135-136
|
|
⤷ |
pKi
7.0
(Ki 1x10-7 M)
[135-136]
|
trans-flupenthixol
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.9
|
pKi
|
41
|
|
⤷ |
pKi
6.9
(Ki 1.2x10-7 M)
[41]
|
EGIS-11150
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.9
|
pKi
|
42
|
|
⤷ |
pKi
6.9
(Ki 1.2x10-7 M)
[42]
|
(+)-UH232
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.4 – 7.1
|
pKi
|
41,120
|
|
⤷ |
pKi
6.4 – 7.1
[41,120]
|
promazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.5
|
pKi
|
26
|
|
⤷ |
pKi
6.5
(Ki 3x10-7 M)
[26]
|
(+)-UH232
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
6.4
|
pKi
|
120
|
|
⤷ |
pKi
6.4
[120]
|
clozapine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.8 – 6.9
|
pKi
|
41,75,114,118,125
|
|
⤷ |
pKi
5.8 – 6.9
[41,75,114,118,125]
|
clozapine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
6.2
|
pKi
|
120
|
|
⤷ |
pKi
6.2
[120]
|
(+)-S-14297
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.5
|
pKi
|
87
|
|
⤷ |
pKi
5.5
[87]
|
(+)-SCH-23390
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.3
|
pKi
|
41
|
|
⤷ |
pKi
5.3
[41]
|
iloperidone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.0
|
pIC50
|
123
|
|
⤷ |
pIC50
7.0
(IC50 1.1x10-7 M)
[123]
Description: Measuring displacement of [3H]spiperone from rat striatum.
|
metopimazine
|
| |