Ligand |
|
|
|
|
|
|
|
|
|
|
|
[3H]fananserin
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.9
|
pKd
|
51
|
|
⤷ |
pKd
9.9
(Kd 1.3x10-10 M)
[51]
|
[3H]ketanserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6 – 9.7
|
pKd
|
41,75
|
|
⤷ |
pKd
8.6 – 9.7
(Kd 2.9x10-9 – 2x10-10 M)
[41,75]
|
[3H]N-methylspiperone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.1
|
pKd
|
86
|
|
⤷ |
pKd
9.1
[86]
|
[3H]ketanserin
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.8
|
pKd
|
86
|
|
⤷ |
pKd
8.8
[86]
|
compound 3b [PMID:28943244]
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.6
|
pKi
|
19
|
|
⤷ |
pKi
10.6
(Ki 2.24x10-11 M)
[19]
|
asenapine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.2
|
pKi
|
84
|
|
⤷ |
pKi
10.2
(Ki 6x10-11 M)
[84]
|
MT-1207
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.1
|
pKi
|
95
|
|
⤷ |
pKi
10.1
(Ki 7.9x10-11 M)
[95]
|
AC-90179
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
9.7
|
pKi
|
94
|
|
⤷ |
pKi
9.7
[94]
|
risperidone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
9.3 – 10.0
|
pKi
|
42,44,81
|
|
⤷ |
pKi
9.3 – 10.0
[42,44,81]
|
pimavanserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
9.3
|
pKi
|
25,94
|
|
⤷ |
pKi
9.3
[25,94]
Description: Ki determined in membrane radioligand binding assay.
|
lumateperone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.3
|
pKi
|
48,89
|
|
⤷ |
pKi
9.3
(Ki 5x10-10 M)
[48,89]
|
sertindole
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.2 – 9.4
|
pKi
|
42,44,81
|
|
⤷ |
pKi
9.2 – 9.4
[42,44,81]
|
ritanserin
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.2
|
pKi
|
76,86
|
|
⤷ |
pKi
9.2
[76,86]
|
LY86057
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.2
|
pKi
|
36
|
|
⤷ |
pKi
9.2
[36]
|
ziprasidone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.8 – 9.5
|
pKi
|
42,44,81,84
|
|
⤷ |
pKi
8.8 – 9.5
[42,44,81,84]
|
spiperone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.0 – 9.2
|
pKi
|
16,86
|
|
⤷ |
pKi
9.0 – 9.2
[16,86]
|
[11C]GSK215083
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.1
|
pKi
|
67
|
|
⤷ |
pKi
9.1
(Ki 7.9x10-10 M)
[67]
|
blonanserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.1
|
pKi
|
64
|
|
⤷ |
pKi
9.1
(Ki 8.1x10-10 M)
[64]
|
9-OH-risperidone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.0
|
pKi
|
81
|
|
⤷ |
pKi
9.0
[81]
|
amoxapine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.0
|
pKi
|
66
|
|
⤷ |
pKi
9.0
[66]
|
methysergide
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.4 – 9.5
|
pKi
|
16,43
|
|
⤷ |
pKi
8.4 – 9.5
[16,43]
|
clozapine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Inverse agonist |
8.9
|
pKi
|
16
|
|
⤷ |
pKi
8.9
[16]
|
ketanserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.1 – 9.7
|
pKi
|
10,41,75
|
|
⤷ |
pKi
8.1 – 9.7
(Ki 7.94x10-9 – 1.99x10-10 M)
[10,41,75]
|
ritanserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.3 – 9.4
|
pKi
|
41,76
|
|
⤷ |
pKi
9.4
[76]
pKi
8.3
[41]
|
cyamemazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.8
|
pKi
|
33
|
|
⤷ |
pKi
8.8
[33]
|
ketanserin
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.6 – 9.0
|
pKi
|
16,86
|
|
⤷ |
pKi
8.6 – 9.0
[16,86]
|
olanzapine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6 – 8.9
|
pKi
|
42,44,81,84
|
|
⤷ |
pKi
8.6 – 8.9
[42,44,81,84]
|
chlorpromazine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Inverse agonist |
8.7
|
pKi
|
16
|
|
⤷ |
pKi
8.7
[16]
|
mianserin
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.4 – 9.0
|
pKi
|
16,66
|
|
⤷ |
pKi
8.4 – 9.0
[16,66]
|
lurasidone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.7
|
pKi
|
34
|
|
⤷ |
pKi
8.7
(Ki 2.03x10-9 M)
[34]
|
mianserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.7 – 9.6
|
pKi
|
41,43,59
|
|
⤷ |
pKi
7.7 – 9.6
[41,43,59]
|
(+)-butaclamol
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6
|
pKi
|
8
|
|
⤷ |
pKi
8.6
[8]
|
spiperone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.8 – 9.4
|
pKi
|
8,41,88
|
|
⤷ |
pKi
7.8 – 9.4
[8,41,88]
|
zotepine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6
|
pKi
|
81
|
|
⤷ |
pKi
8.6
[81]
|
metergoline
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6
|
pKi
|
41
|
|
⤷ |
pKi
8.6
[41]
|
mesulergine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.6
|
pKi
|
36
|
|
⤷ |
pKi
8.6
[36]
|
BF-1
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6
|
pKi
|
80
|
|
⤷ |
pKi
8.6
[80]
|
EGIS-11150
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.5
|
pKi
|
23
|
|
⤷ |
pKi
8.5
(Ki 3.1x10-9 M)
[23]
|
methiothepin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.5
|
pKi
|
41
|
|
⤷ |
pKi
8.5
[41]
|
risperidone
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.5
|
pKi
|
16
|
|
⤷ |
pKi
8.5
[16]
|
LY215840
|
|