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
|
81
|
|
pKd
9.1
[81]
|
[3H]ketanserin
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.8
|
pKd
|
81
|
|
pKd
8.8
[81]
|
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
|
79
|
|
pKi
10.2
(Ki 6x10-11 M)
[79]
|
AC-90179
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
9.7
|
pKi
|
89
|
|
pKi
9.7
[89]
|
risperidone
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
9.3 – 10.0
|
pKi
|
39,41,76
|
|
pKi
9.3 – 10.0
[39,41,76]
|
pimavanserin
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
9.3
|
pKi
|
23,89
|
|
pKi
9.3
[23,89]
Description: Ki determined in membrane radioligand binding assay.
|
lumateperone
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.3
|
pKi
|
45,84
|
|
pKi
9.3
(Ki 5x10-10 M)
[45,84]
|
sertindole
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.2 – 9.4
|
pKi
|
39,41,76
|
|
pKi
9.2 – 9.4
[39,41,76]
|
ritanserin
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.2
|
pKi
|
72,81
|
|
pKi
9.2
[72,81]
|
LY86057
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.2
|
pKi
|
34
|
|
pKi
9.2
[34]
|
ziprasidone
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.8 – 9.5
|
pKi
|
39,41,76,79
|
|
pKi
8.8 – 9.5
[39,41,76,79]
|
spiperone
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.0 – 9.2
|
pKi
|
16,81
|
|
pKi
9.0 – 9.2
[16,81]
|
[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
|
76
|
|
pKi
9.0
[76]
|
amoxapine
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.0
|
pKi
|
70
|
|
pKi
9.0
[70]
|
methysergide
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.4 – 9.5
|
pKi
|
16,40
|
|
pKi
8.4 – 9.5
[16,40]
|
clozapine
|
|
|
|
|
|
|
|
|
|
Rn |
Inverse agonist |
8.9
|
pKi
|
16
|
|
pKi
8.9
[16]
|
ketanserin
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.1 – 9.7
|
pKi
|
11,38,71
|
|
pKi
8.1 – 9.7
(Ki 7.94x10-9 – 1.99x10-10 M)
[11,38,71]
|
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
|
16,81
|
|
pKi
8.6 – 9.0
[16,81]
|
olanzapine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6 – 8.9
|
pKi
|
39,41,76,79
|
|
pKi
8.6 – 8.9
[39,41,76,79]
|
chlorpromazine
|
|
|
|
|
|
|
|
|
|
Rn |
Inverse agonist |
8.7
|
pKi
|
16
|
|
pKi
8.7
[16]
|
mianserin
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.4 – 9.0
|
pKi
|
16,70
|
|
pKi
8.4 – 9.0
[16,70]
|
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
|
9
|
|
pKi
8.6
[9]
|
spiperone
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.8 – 9.4
|
pKi
|
9,38,83
|
|
pKi
7.8 – 9.4
[9,38,83]
|
zotepine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6
|
pKi
|
76
|
|
pKi
8.6
[76]
|
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
|
75
|
|
pKi
8.6
[75]
|
methiothepin
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.5
|
pKi
|
38
|
|
pKi
8.5
[38]
|
risperidone
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.5
|
pKi
|
16
|
|
pKi
8.5
[16]
|
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
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.4
|
pKi
|
34
|
|
pKi
8.4
[34]
|
sergolexole
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.4
|
pKi
|
34
|
|
pKi
8.4
[34]
|
clozapine
|
|
|
|
|
|
|
|
|
|
Hs |
Inverse agonist |
7.6 – 9.0
|
pKi
|
38,41,52,76,89
|
|
pKi
7.6 – 9.0
[38,41,52,76,89]
|
pipamperone
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.3
|
pKi
|
76
|
|
pKi
8.3
[76]
|
nefazodone
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.2
|
pKi
|
78
|
|
pKi
8.2
(Ki 5.8x10-9 M)
[78]
|
roxindole
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.2
|
pKi
|
54
|
|
pKi
8.2
[54]
|
perphenazine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.2
|
pKi
|
41
|
|
pKi
8.2
[41]
|
amitriptyline
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.0 – 8.4
|
pKi
|
70,87
|
|
pKi
8.4
[70]
pKi
8.0
(Ki 1.1x10-8 M)
[87]
|
chlorpromazine
|
|
|
|
|
|
|
|
|
|
| |