Ligand |
|
|
|
|
|
|
|
|
|
|
|
[3H]fananserin
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.9
|
pKd
|
48
|
|
⤷ |
pKd
9.9
(Kd 1.3x10-10 M)
[48]
|
[3H]ketanserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6 – 9.7
|
pKd
|
38,71
|
|
⤷ |
pKd
8.6 – 9.7
(Kd 2.9x10-9 – 2x10-10 M)
[38,71]
|
[3H]N-methylspiperone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.1
|
pKd
|
82
|
|
⤷ |
pKd
9.1
[82]
|
[3H]ketanserin
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.8
|
pKd
|
82
|
|
⤷ |
pKd
8.8
[82]
|
compound 3b [PMID:28943244]
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.6
|
pKi
|
18
|
|
⤷ |
pKi
10.6
(Ki 2.24x10-11 M)
[18]
|
asenapine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.2
|
pKi
|
80
|
|
⤷ |
pKi
10.2
(Ki 6x10-11 M)
[80]
|
AC-90179
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
9.7
|
pKi
|
90
|
|
⤷ |
pKi
9.7
[90]
|
risperidone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
9.3 – 10.0
|
pKi
|
39,41,77
|
|
⤷ |
pKi
9.3 – 10.0
[39,41,77]
|
pimavanserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
9.3
|
pKi
|
23,90
|
|
⤷ |
pKi
9.3
[23,90]
Description: Ki determined in membrane radioligand binding assay.
|
lumateperone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.3
|
pKi
|
45,85
|
|
⤷ |
pKi
9.3
(Ki 5x10-10 M)
[45,85]
|
sertindole
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.2 – 9.4
|
pKi
|
39,41,77
|
|
⤷ |
pKi
9.2 – 9.4
[39,41,77]
|
ritanserin
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.2
|
pKi
|
72,82
|
|
⤷ |
pKi
9.2
[72,82]
|
LY86057
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.2
|
pKi
|
34
|
|
⤷ |
pKi
9.2
[34]
|
ziprasidone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.8 – 9.5
|
pKi
|
39,41,77,80
|
|
⤷ |
pKi
8.8 – 9.5
[39,41,77,80]
|
spiperone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.0 – 9.2
|
pKi
|
15,82
|
|
⤷ |
pKi
9.0 – 9.2
[15,82]
|
[11C]GSK215083
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.1
|
pKi
|
62
|
|
⤷ |
pKi
9.1
(Ki 7.9x10-10 M)
[62]
|
blonanserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.1
|
pKi
|
60
|
|
⤷ |
pKi
9.1
(Ki 8.1x10-10 M)
[60]
|
9-OH-risperidone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.0
|
pKi
|
77
|
|
⤷ |
pKi
9.0
[77]
|
amoxapine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.0
|
pKi
|
70
|
|
⤷ |
pKi
9.0
[70]
|
methysergide
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.4 – 9.5
|
pKi
|
15,40
|
|
⤷ |
pKi
8.4 – 9.5
[15,40]
|
clozapine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Inverse agonist |
8.9
|
pKi
|
15
|
|
⤷ |
pKi
8.9
[15]
|
ketanserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.1 – 9.7
|
pKi
|
10,38,71
|
|
⤷ |
pKi
8.1 – 9.7
(Ki 7.94x10-9 – 1.99x10-10 M)
[10,38,71]
|
ritanserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.3 – 9.4
|
pKi
|
38,72
|
|
⤷ |
pKi
9.4
[72]
pKi
8.3
[38]
|
cyamemazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.8
|
pKi
|
31
|
|
⤷ |
pKi
8.8
[31]
|
ketanserin
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.6 – 9.0
|
pKi
|
15,82
|
|
⤷ |
pKi
8.6 – 9.0
[15,82]
|
olanzapine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6 – 8.9
|
pKi
|
39,41,77,80
|
|
⤷ |
pKi
8.6 – 8.9
[39,41,77,80]
|
chlorpromazine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Inverse agonist |
8.7
|
pKi
|
15
|
|
⤷ |
pKi
8.7
[15]
|
mianserin
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.4 – 9.0
|
pKi
|
15,70
|
|
⤷ |
pKi
8.4 – 9.0
[15,70]
|
lurasidone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.7
|
pKi
|
32
|
|
⤷ |
pKi
8.7
(Ki 2.03x10-9 M)
[32]
|
mianserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.7 – 9.6
|
pKi
|
38,40,55
|
|
⤷ |
pKi
7.7 – 9.6
[38,40,55]
|
(+)-butaclamol
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6
|
pKi
|
8
|
|
⤷ |
pKi
8.6
[8]
|
spiperone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.8 – 9.4
|
pKi
|
8,38,84
|
|
⤷ |
pKi
7.8 – 9.4
[8,38,84]
|
zotepine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6
|
pKi
|
77
|
|
⤷ |
pKi
8.6
[77]
|
metergoline
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6
|
pKi
|
38
|
|
⤷ |
pKi
8.6
[38]
|
mesulergine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.6
|
pKi
|
34
|
|
⤷ |
pKi
8.6
[34]
|
BF-1
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6
|
pKi
|
76
|
|
⤷ |
pKi
8.6
[76]
|
EGIS-11150
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.5
|
pKi
|
21
|
|
⤷ |
pKi
8.5
(Ki 3.1x10-9 M)
[21]
|
methiothepin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.5
|
pKi
|
38
|
|
⤷ |
pKi
8.5
[38]
|
risperidone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.5
|
pKi
|
15
|
|
⤷ |
pKi
8.5
[15]
|
LY215840
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.5
|
pKi
|
34
|
|
⤷ |
pKi
8.5
[34]
|
LY53857
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.5
|
pKi
|
34
|
|
⤷ |
pKi
8.5
[34]
|
amesergide
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.5
|
pKi
|
34
|
|
⤷ |
pKi
8.5
[34]
|
sarpogrelate
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.5
|
pKi
|
71
|
|
⤷ |
pKi
8.5
[71]
|
methysergide
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.4
|
pKi
|
38
|
|
⤷ |
pKi
8.4
[38]
|
LY108742
|
 | |