Ligand |
|
|
|
|
|
|
|
|
|
|
|
[3H]LSD
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
8.7
|
pKd
|
38
|
|
⤷ |
pKd
8.7
(Kd 2.1x10-9 M)
[38]
|
[3H]5-HT
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
8.1
|
pKd
|
50
|
|
⤷ |
pKd
8.1
(Kd 8x10-9 M)
[50]
|
[125I]DOI
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.6 – 7.7
|
pKd
|
|
|
⤷ |
pKd
7.6 – 7.7
(Kd 2.5x10-8 – 2x10-8 M)
|
methylergonovine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Partial agonist |
9.3
|
pKi
|
14,41
|
|
⤷ |
pKi
9.3
[14,41]
|
(+)-LSD
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
9.0
|
pKi
|
14
|
|
⤷ |
pKi
9.0
[14]
|
cabergoline
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
8.9
|
pKi
|
27
|
|
⤷ |
pKi
8.9
[27]
|
methysergide
|
|
|
|
|
|
|
|
|
|
|
Hs |
Partial agonist |
8.0 – 9.4
|
pKi
|
14,41,51
|
|
⤷ |
pKi
8.0 – 9.4
[14,41,51]
|
ergotamine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Partial agonist |
8.5 – 8.9
|
pKi
|
14,41
|
|
⤷ |
pKi
8.5 – 8.9
[14,41]
|
Lysergide
|
|
|
|
|
|
|
|
|
|
|
Hs |
Biased agonist |
8.4
|
pKi
|
49
|
|
⤷ |
pKi
8.4
[49]
Description: Biased for β-arrestin sihnalling.
|
S 16924
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
8.4
|
pKi
|
25
|
|
⤷ |
pKi
8.4
[25]
|
Lysergide
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
8.3
|
pKi
|
33
|
|
⤷ |
pKi
8.3
[33]
|
AL-37350A
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
8.3
|
pKi
|
23
|
|
⤷ |
pKi
8.3
[23]
|
Ro 60-0175
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
8.3
|
pKi
|
14
|
|
⤷ |
pKi
8.3
(Ki 5.01x10-9 M)
[14]
|
pergolide
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
8.2
|
pKi
|
27
|
|
⤷ |
pKi
8.2
[27]
|
methysergide
|
|
|
|
|
|
|
|
|
|
|
Rn |
Partial agonist |
8.2
|
pKi
|
50
|
|
⤷ |
pKi
8.2
[50]
|
5-hydroxytryptamine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.9 – 8.4
|
pKi
|
2,14,16,23,41
|
|
⤷ |
pKi
7.9 – 8.4
[2,14,16,23,41]
|
α-methyl-5-HT
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.9 – 8.3
|
pKi
|
2,14,16
|
|
⤷ |
pKi
7.9 – 8.3
[2,14,16]
|
5-hydroxytryptamine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
8.0
|
pKi
|
50
|
|
⤷ |
pKi
8.0
[50]
|
5-MeOT
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
8.0
|
pKi
|
50
|
|
⤷ |
pKi
8.0
[50]
|
α-methyl-5-HT
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
8.0
|
pKi
|
50
|
|
⤷ |
pKi
8.0
[50]
|
(+)-norfenfluramine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
8.0
|
pKi
|
41
|
|
⤷ |
pKi
8.0
[41]
|
BW723C86
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.3 – 8.6
|
pKi
|
2,14,42
|
|
⤷ |
pKi
7.3 – 8.6
(Ki 5.01x10-8 – 2.51x10-9 M)
[2,14,42]
|
m-chlorophenylpiperazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Partial agonist |
7.4 – 8.5
|
pKi
|
14,32,41-42,51
|
|
⤷ |
pKi
7.4 – 8.5
[14,32,41-42,51]
|
RU 24969
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
7.8
|
pKi
|
50
|
|
⤷ |
pKi
7.8
[50]
|
DOI
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.6 – 7.7
|
pKi
|
16,32,42
|
|
⤷ |
pKi
7.6 – 7.7
(Ki 2.51x10-8 – 1.99x10-8 M)
[16,32,42]
|
m-chlorophenylpiperazine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Partial agonist |
7.6
|
pKi
|
50
|
|
⤷ |
pKi
7.6
[50]
|
DOI
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
7.6
|
pKi
|
16,50
|
|
⤷ |
pKi
7.6
[16,50]
|
(+)-DOI
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.6
|
pKi
|
14
|
|
⤷ |
pKi
7.6
[14]
|
relenopride
|
|
|
|
|
|
|
|
|
|
|
Hs |
Agonist |
7.5
|
pKi
|
12
|
|
⤷ |
pKi
7.5
(Ki 3.1x10-8 M)
[12]
|
(R)-DOI
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.3 – 7.7
|
pKi
|
14,23,34
|
|
⤷ |
pKi
7.7
[23]
pKi
7.3 – 7.4
[14,34]
|
brolamfetamine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.4 – 7.6
|
pKi
|
14,32
|
|
⤷ |
pKi
7.4 – 7.6
[14,32]
|
VER-3323
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.5
|
pKi
|
14
|
|
⤷ |
pKi
7.5
[14]
|
dihydroergocryptine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Biased agonist |
7.5
|
pKi
|
49
|
|
⤷ |
pKi
7.5
[49]
Description: Biased for β-arrestin signalling.
|
BRL-15572
|
|
|
|
|
|
|
|
|
|
|
Hs |
Partial agonist |
7.4
|
pKi
|
37
|
|
⤷ |
pKi
7.4
[37]
|
ORG-37684
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.4
|
pKi
|
14
|
|
⤷ |
pKi
7.4
[14]
|
norfenfluramine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.3
|
pKi
|
41
|
|
⤷ |
pKi
7.3
[41]
|
(-)-norfenfluramine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.3
|
pKi
|
41
|
|
⤷ |
pKi
7.3
[41]
|
TFMPP
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.2
|
pKi
|
14
|
|
⤷ |
pKi
7.2
[14]
|
TFMPP
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
7.1
|
pKi
|
50
|
|
⤷ |
pKi
7.1
[50]
|
quipazine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.1
|
pKi
|
14
|
|
⤷ |
pKi
7.1
[14]
|
tryptamine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.0
|
pKi
|
14
|
|
⤷ |
pKi
7.0
[14]
|
tryptamine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
7.0
|
pKi
|
50
|
|
⤷ |
pKi
7.0
[50]
|
Org 12962
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
7.0
|
pKi
|
14
|
|
⤷ |
pKi
7.0
[14]
|
RU 24969
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
6.9
|
pKi
|
14
|
|
⤷ |
pKi
6.9
[14]
|
quipazine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
6.9
|
pKi
|
50
|
|
⤷ |
pKi
6.9
[50]
|
5-CT
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
6.7 – 6.9
|
pKi
|
14,16
|
|
⤷ |
pKi
6.7 – 6.9
[14,16]
|
5-CT
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
6.8
|
pKi
|
16,50
|
|
⤷ |
pKi
6.8
[16,50]
|
lorcaserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
6.8
|
pKi
|
48
|
|
⤷ |
pKi
6.8
[48]
|
2-methyl-5-HT
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
6.6
|
pKi
|
50
|
|
⤷ |
pKi
6.6
[50]
|
MK-212
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
6.2 – 6.8
|
pKi
|
14,42
|
|
⤷ |
pKi
6.2 – 6.8
[14,42]
|
MK-212
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
6.4
|
pKi
|
50
|
|
⤷ |
pKi
6.4
[50]
|
GR 127935
|
|
|
|
|
|
|
|
|
|
|
Hs |
Partial agonist |
6.2
|
pKi
|
37
|
|
⤷ |
pKi
6.2
[37]
|
CGS-12066
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
6.1
|
pKi
|
14
|
|
⤷ |
pKi
6.1
[14]
|
LY344864
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
5.8
|
pKi
|
35
|
|
⤷ |
pKi
5.8
[35]
|
SB 216641
|
|
|
|
|
|
|
|
|
|
|
Hs |
Partial agonist |
5.8
|
pKi
|
37
|
|
⤷ |
pKi
5.8
[37]
|
capeserod
|
|
|
|
|
|
|
|
|
|
|
Hs |
Partial agonist |
5.8
|
pKi
|
28
|
|
⤷ |
pKi
5.8
[28]
|
quinpirole
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
5.0 – 6.5
|
pKi
|
14,27
|
|
⤷ |
pKi
5.0 – 6.5
[14,27]
|
pindolol
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
5.7
|
pKi
|
14
|
|
⤷ |
pKi
5.7
[14]
|
8-OH-DPAT
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
5.4
|
pKi
|
14
|
|
⤷ |
pKi
5.4
[14]
|
8-OH-DPAT
|
|
|
|
|
|
|
|
|
|
|
Rn |
Full agonist |
5.4
|
pKi
|
50
|
|
⤷ |
pKi
5.4
[50]
|
lorcaserin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Full agonist |
6.0
|
pEC50
|
48
|
|
⤷ |
pEC50
6.0
[48]
|
|