Ligand |
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[3H]mesulergine
|
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Hs |
Inverse agonist |
8.7 – 9.3
|
pKd
|
22,63
|
|
⤷ |
pKd
8.7 – 9.3
(Kd 2.2x10-9 – 5x10-10 M)
[22,63]
|
methysergide
|
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Rn |
Antagonist |
9.3
|
pKi
|
32
|
|
⤷ |
pKi
9.3
[32]
|
mesulergine
|
|
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Rn |
Inverse agonist |
9.2
|
pKi
|
32
|
|
⤷ |
pKi
9.2
[32]
|
sertindole
|
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Hs |
Inverse agonist |
9.0 – 9.2
|
pKi
|
34,40
|
|
⤷ |
pKi
9.0 – 9.2
[34,40]
|
mianserin
|
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Rn |
Antagonist |
8.8 – 9.4
|
pKi
|
32,62
|
|
⤷ |
pKi
8.8 – 9.4
[32,62]
|
SB 228357
|
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Hs |
Antagonist |
9.0 – 9.1
|
pKi
|
7,65
|
|
⤷ |
pKi
9.0 – 9.1
[7,65]
|
mesulergine
|
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|
Hs |
Inverse agonist |
8.7 – 9.3
|
pKi
|
30,38-39
|
|
⤷ |
pKi
8.7 – 9.3
[30,38-39]
|
FR260010
|
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Hs |
Antagonist |
9.0
|
pKi
|
31
|
|
⤷ |
pKi
9.0
(Ki 1.1x10-9 M)
[31]
|
ritanserin
|
|
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Hs |
Antagonist |
8.2 – 9.6
|
pKi
|
38
|
|
⤷ |
pKi
8.2 – 9.6
[38]
|
methysergide
|
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Hs |
Antagonist |
8.6 – 9.1
|
pKi
|
20,38
|
|
⤷ |
pKi
8.6 – 9.1
[20,38]
|
metergoline
|
|
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Hs |
Inverse agonist |
8.8
|
pKi
|
38
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|
⤷ |
pKi
8.8
[38]
|
mianserin
|
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Hs |
Inverse agonist |
8.3 – 9.2
|
pKi
|
22,38,49
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⤷ |
pKi
8.3 – 9.2
[22,38,49]
|
SB 221284
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Hs |
Antagonist |
8.7
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pKi
|
38
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⤷ |
pKi
8.7
[38]
|
amoxapine
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Rn |
Antagonist |
8.7
|
pKi
|
62
|
|
⤷ |
pKi
8.7
[62]
|
zotepine
|
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Hs |
Inverse agonist |
8.6
|
pKi
|
34
|
|
⤷ |
pKi
8.6
[34]
|
SB 242084
|
|
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|
Hs |
Antagonist |
8.2 – 9.0
|
pKi
|
36,38
|
|
⤷ |
pKi
8.2 – 9.0
(Ki 6.31x10-9 – 1x10-9 M)
[36,38]
|
ziprasidone
|
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Hs |
Inverse agonist |
7.9 – 9.0
|
pKi
|
34,40,70
|
|
⤷ |
pKi
7.9 – 9.0
[34,40,70]
|
methiothepin
|
|
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Hs |
Inverse agonist |
8.4
|
pKi
|
38
|
|
⤷ |
pKi
8.4
[38]
|
RS-102221
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Rn |
Antagonist |
8.4
|
pKi
|
5
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⤷ |
pKi
8.4
[5]
|
RS-102221
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Hs |
Antagonist |
8.3 – 8.4
|
pKi
|
5,38
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⤷ |
pKi
8.3 – 8.4
(Ki 5.01x10-9 – 3.98x10-9 M)
[5,38]
|
tiospirone
|
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Hs |
Inverse agonist |
8.3
|
pKi
|
34
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⤷ |
pKi
8.3
[34]
|
olanzapine
|
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Hs |
Inverse agonist |
8.1 – 8.4
|
pKi
|
34,40,70
|
|
⤷ |
pKi
8.1 – 8.4
[34,40,70]
|
SDZ SER-082
|
|
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Hs |
Antagonist |
8.1
|
pKi
|
38
|
|
⤷ |
pKi
8.1
[38]
|
amitriptyline
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Rn |
Antagonist |
8.1
|
pKi
|
74
|
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⤷ |
pKi
8.1
(Ki 8x10-9 M)
[74]
|
clozapine
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Hs |
Inverse agonist |
7.4 – 8.7
|
pKi
|
22,34,38,40,46,76
|
|
⤷ |
pKi
7.4 – 8.7
[22,34,38,40,46,76]
|
cyamemazine
|
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Hs |
Antagonist |
7.9
|
pKi
|
30
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⤷ |
pKi
7.9
[30]
|
loxapine
|
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Hs |
Inverse agonist |
7.8 – 8.0
|
pKi
|
34,40
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⤷ |
pKi
7.8 – 8.0
[34,40]
|
chlorpromazine
|
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Hs |
Antagonist |
7.6 – 8.2
|
pKi
|
34,40
|
|
⤷ |
pKi
7.6 – 8.2
[34,40]
|
SB 206553
|
|
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|
Hs |
Antagonist |
7.8 – 7.9
|
pKi
|
35,38
|
|
⤷ |
pKi
7.8 – 7.9
[35,38]
|
EGIS-7625
|
|
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|
Hs |
Antagonist |
7.7
|
pKi
|
39
|
|
⤷ |
pKi
7.7
[39]
|
SB 215505
|
|
|
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|
Hs |
Antagonist |
7.7
|
pKi
|
65
|
|
⤷ |
pKi
7.7
[65]
|
volinanserin
|
|
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|
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|
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|
Hs |
Antagonist |
7.5 – 7.7
|
pKi
|
38,65
|
|
⤷ |
pKi
7.5 – 7.7
[38,65]
|
risperidone
|
|
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|
Hs |
Inverse agonist |
7.5 – 7.6
|
pKi
|
34,40
|
|
⤷ |
pKi
7.5 – 7.6
[34,40]
|
mirtazapine
|
|
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Hs |
Antagonist |
7.4
|
pKi
|
21
|
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⤷ |
pKi
7.4
(Ki 3.9x10-8 M)
[21]
|
xanomeline
|
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Hs |
Antagonist |
7.4
|
pKi
|
78
|
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⤷ |
pKi
7.4
[78]
|
sarpogrelate
|
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Hs |
Antagonist |
7.4
|
pKi
|
63
|
|
⤷ |
pKi
7.4
[63]
|
terguride
|
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Hs |
Antagonist |
7.3
|
pKi
|
48
|
|
⤷ |
pKi
7.3
[48]
|
fluoxetine
|
|
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|
Rn |
Antagonist |
7.3
|
pKi
|
66
|
|
⤷ |
pKi
7.3
[66]
|
thioridazine
|
|
|
|
|
|
|
|
|
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|
Hs |
Antagonist |
7.2 – 7.3
|
pKi
|
34,40
|
|
⤷ |
pKi
7.2 – 7.3
[34,40]
|
ketanserin
|
|
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|
Hs |
Antagonist |
6.8 – 7.5
|
pKi
|
8,22,38,63
|
|
⤷ |
pKi
6.8 – 7.5
[8,22,38,63]
|
S33084
|
|
|
|
|
|
|
|
|
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|
Hs |
Antagonist |
7.1
|
pKi
|
47
|
|
⤷ |
pKi
7.1
[47]
|
apomorphine
|
|
|
|
|
|
|
|
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|
Hs |
Antagonist |
7.0
|
pKi
|
48
|
|
⤷ |
pKi
7.0
[48]
|
LY334362
|
|
|
|
|
|
|
|
|
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|
Hs |
Antagonist |
7.0
|
pKi
|
8
|
|
⤷ |
pKi
7.0
[8]
|
perphenazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.9
|
pKi
|
40
|
|
⤷ |
pKi
6.9
[40]
|
glemanserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.6
|
pKi
|
38
|
|
⤷ |
pKi
6.6
[38]
|
trazodone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.6
|
pKi
|
38
|
|
⤷ |
pKi
6.6
[38]
|
idalopirdine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.6
|
pKi
|
41
|
|
⤷ |
pKi
6.6
(Ki 2.5x10-7 M)
[41]
|
trazodone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
6.4 – 6.7
|
pKi
|
62,66
|
|
⤷ |
pKi
6.4 – 6.7
[62,66]
|
roxindole
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.5
|
pKi
|
48
|
|
⤷ |
pKi
6.5
[48]
|
norfluoxetine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
6.5
|
pKi
|
66
|
|
⤷ |
pKi
6.5
[66]
|
trifluoperazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.4
|
pKi
|
40
|
|
⤷ |
pKi
6.4
[40]
|
mesoridazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.4
|
pKi
|
13
|
|
⤷ |
pKi
6.4
(Ki 4.12x10-7 M)
[13]
|
RS-127445
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.3
|
pKi
|
38
|
|
⤷ |
pKi
6.3
[38]
|
MPDT
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
6.2
|
pKi
|
29
|
|
⤷ |
pKi
6.2
[29]
|
agomelatine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.2
|
pKi
|
45
|
|
⤷ |
pKi
6.2
[45]
|
duloxetine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.0
|
pKi
|
11
|
|
⤷ |
pKi
6.0
[11]
|
SB 224289
|
|
|
|
|
|
|
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| |