Ligand |
|
|
|
|
|
|
|
|
|
|
|
risperidone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Inverse agonist |
8.9 – 9.0
|
pKd
|
31,49
|
|
⤷ |
pKd
8.9 – 9.0
[31,49]
|
[3H]SB269970
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.9
|
pKd
|
60
|
|
⤷ |
pKd
8.9
(Kd 1.2x10-9 M)
[60]
|
lurasidone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.3
|
pKi
|
24
|
|
⤷ |
pKi
9.3
(Ki 4.95x10-10 M)
[24]
|
pimozide
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.3
|
pKi
|
49
|
|
⤷ |
pKi
9.3
[49]
|
methiothepin
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.0 – 9.4
|
pKi
|
52
|
|
⤷ |
pKi
9.0 – 9.4
[52]
|
tiospirone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.2
|
pKi
|
49
|
|
⤷ |
pKi
9.2
[49]
|
methiothepin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.4 – 9.4
|
pKi
|
5,25,32,61
|
|
⤷ |
pKi
8.4 – 9.4
[5,25,32,61]
|
zotepine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Inverse agonist |
8.8
|
pKi
|
49
|
|
⤷ |
pKi
8.8
[49]
|
SB269970
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6 – 8.9
|
pKi
|
60
|
|
⤷ |
pKi
8.6 – 8.9
[60]
|
SB656104
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.7
|
pKi
|
13
|
|
⤷ |
pKi
8.7
(Ki 1.9x10-9 M)
[13]
|
DR-4004
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.7
|
pKi
|
15,28
|
|
⤷ |
pKi
8.7
(Ki 2x10-9 M)
[15,28]
|
metergoline
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.2 – 8.9
|
pKi
|
5,25,32
|
|
⤷ |
pKi
8.2 – 8.9
[5,25,32]
|
risperidone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
8.3 – 8.7
|
pKi
|
47,61
|
|
⤷ |
pKi
8.3 – 8.7
[47,61]
|
ziprasidone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
8.4
|
pKi
|
47
|
|
⤷ |
pKi
8.4
[47]
|
zotepine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
8.4
|
pKi
|
47
|
|
⤷ |
pKi
8.4
[47]
|
pirenperone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.2 – 8.5
|
pKi
|
25
|
|
⤷ |
pKi
8.2 – 8.5
[25]
|
fluperlapine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Inverse agonist |
8.3
|
pKi
|
49
|
|
⤷ |
pKi
8.3
[49]
|
methiothepin
|
|
|
|
|
|
|
|
|
|
|
Mm |
Antagonist |
8.2
|
pKi
|
46
|
|
⤷ |
pKi
8.2
[46]
|
JNJ-18038683
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.2
|
pKi
|
7
|
|
⤷ |
pKi
8.2
[7]
|
fluphenazine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Inverse agonist |
8.1
|
pKi
|
49
|
|
⤷ |
pKi
8.1
[49]
|
EGIS-11150
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
8.1
|
pKi
|
14
|
|
⤷ |
pKi
8.1
(Ki 9x10-9 M)
[14]
|
dihydroergotamine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.0
|
pKi
|
5
|
|
⤷ |
pKi
8.0
[5]
|
2-bromo-LSD
|
|
|
|
|
|
|
|
|
|
|
Mm |
Antagonist |
8.0
|
pKi
|
46
|
|
⤷ |
pKi
8.0
[46]
|
metergoline
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.2 – 8.7
|
pKi
|
50,52
|
|
⤷ |
pKi
7.2 – 8.7
[50,52]
|
mesulergine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.7 – 8.2
|
pKi
|
52
|
|
⤷ |
pKi
7.7 – 8.2
[52]
|
methysergide
|
|
|
|
|
|
|
|
|
|
|
Mm |
Antagonist |
7.9
|
pKi
|
46
|
|
⤷ |
pKi
7.9
[46]
|
methysergide
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.9
|
pKi
|
52
|
|
⤷ |
pKi
7.9
[52]
|
fluphenazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
7.9
|
pKi
|
47
|
|
⤷ |
pKi
7.9
[47]
|
spiperone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.7 – 8.0
|
pKi
|
49-50
|
|
⤷ |
pKi
7.7 – 8.0
[49-50]
|
mesulergine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.5 – 8.2
|
pKi
|
5,25,32,61
|
|
⤷ |
pKi
7.5 – 8.2
[5,25,32,61]
|
ritanserin
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.7 – 7.8
|
pKi
|
52
|
|
⤷ |
pKi
7.7 – 7.8
[52]
|
clozapine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Inverse agonist |
7.2 – 8.2
|
pKi
|
31,49-50,52
|
|
⤷ |
pKi
7.2 – 8.2
[31,49-50,52]
|
iloperidone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.7
|
pKi
|
31
|
|
⤷ |
pKi
7.7
[31]
|
chlorpromazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
7.6
|
pKi
|
47
|
|
⤷ |
pKi
7.6
[47]
|
chlorpromazine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Inverse agonist |
7.6
|
pKi
|
49
|
|
⤷ |
pKi
7.6
[49]
|
mesulergine
|
|
|
|
|
|
|
|
|
|
|
Mm |
Antagonist |
7.6
|
pKi
|
46
|
|
⤷ |
pKi
7.6
[46]
|
perphenazine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Inverse agonist |
7.6
|
pKi
|
49
|
|
⤷ |
pKi
7.6
[49]
|
clozapine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
7.2 – 7.8
|
pKi
|
32,47,61
|
|
⤷ |
pKi
7.2 – 7.8
[32,47,61]
|
(+)-butaclamol
|
|
|
|
|
|
|
|
|
|
|
Mm |
Antagonist |
7.5
|
pKi
|
46
|
|
⤷ |
pKi
7.5
[46]
|
spiperone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.0 – 8.0
|
pKi
|
5,25,32
|
|
⤷ |
pKi
7.0 – 8.0
[5,25,32]
|
metergoline
|
|
|
|
|
|
|
|
|
|
|
Mm |
Antagonist |
7.5
|
pKi
|
46
|
|
⤷ |
pKi
7.5
[46]
|
2-bromo-LSD
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.5
|
pKi
|
5
|
|
⤷ |
pKi
7.5
[5]
|
fluperlapine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
7.5
|
pKi
|
47
|
|
⤷ |
pKi
7.5
[47]
|
SB 258719
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
7.5
|
pKi
|
61
|
|
⤷ |
pKi
7.5
(Ki 3.16x10-8 M)
[61]
|
methysergide
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.1 – 7.8
|
pKi
|
5,25,32
|
|
⤷ |
pKi
7.1 – 7.8
[5,25,32]
|
mianserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.3 – 7.6
|
pKi
|
25
|
|
⤷ |
pKi
7.3 – 7.6
[25]
|
clozapine
|
|
|
|
|
|
|
|
|
|
|
Mm |
Inverse agonist |
7.4
|
pKi
|
46
|
|
⤷ |
pKi
7.4
[46]
|
amoxapine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.4
|
pKi
|
49
|
|
⤷ |
pKi
7.4
[49]
|
ergotamine
|
|
|
|
|
|
|
|
|
|
|
Mm |
Antagonist |
7.3
|
pKi
|
46
|
|
⤷ |
pKi
7.3
[46]
|
cyproheptadine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.1 – 7.5
|
pKi
|
50,52
|
|
⤷ |
pKi
7.1 – 7.5
[50,52]
|
cyamemazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.2
|
pKi
|
19
|
|
⤷ |
pKi
7.2
[19]
|
spiperone
|
|
|
|
|
|
|
|
|
|
|
Mm |
Antagonist |
7.2
|
pKi
|
46
|
|
⤷ |
pKi
7.2
[46]
|
thioridazine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Inverse agonist |
7.2
|
pKi
|
49
|
|
⤷ |
pKi
7.2
[49]
|
mianserin
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.0 – 7.4
|
pKi
|
50,52
|
|
⤷ |
pKi
7.0 – 7.4
[50,52]
|
perphenazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
7.2
|
pKi
|
47
|
|
⤷ |
pKi
7.2
[47]
|
ritanserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.8 – 7.4
|
pKi
|
5,32
|
|
⤷ |
pKi
6.8 – 7.4
[5,32]
|
loxapine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
6.8 – 7.4
|
pKi
|
49,52
|
|
⤷ |
pKi
6.8 – 7.4
[49,52]
|
thioridazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
7.1
|
pKi
|
47
|
|
⤷ |
pKi
7.1
[47]
|
(+)-butaclamol
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.0
|
pKi
|
50
|
|
⤷ |
pKi
7.0
[50]
|
iloperidone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.0
|
pKi
|
26
|
|
⤷ |
pKi
7.0
[26]
|
mianserin
|
|
|
|
|
|
|
|
|
|
|
Mm |
Antagonist |
7.0
|
pKi
|
46
|
|
⤷ |
pKi
7.0
[46]
|
dihydroergocryptine
|
|
|
|
|
|
|
|
|
|
|
Mm |
Antagonist |
7.0
|
pKi
|
46
|
|
⤷ |
pKi
7.0
[46]
|
amitriptyline
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
6.9 – 7.0
|
pKi
|
52
|
|
⤷ |
pKi
6.9 – 7.0
[52]
|
olanzapine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
6.8 – 7.0
|
pKi
|
31,49
|
|
⤷ |
pKi
6.8 – 7.0
[31,49]
|
cyproheptadine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.9
|
pKi
|
5
|
|
⤷ |
pKi
6.9
[5]
|
MPDT
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.8
|
pKi
|
16
|
|
⤷ |
pKi
6.8
[16]
|
dihydroergotamine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
6.8
|
pKi
|
50
|
|
⤷ |
pKi
6.8
[50]
|
ketanserin
|
|
|
|
| |