Ligand |
|
|
|
|
|
|
|
|
|
|
|
[3H]QNB
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.6 – 10.8
|
pKd
|
63,107
|
|
⤷ |
pKd
10.6 – 10.8
(Kd 2.51x10-11 – 1.58x10-11 M)
[63,107]
|
Cy3B-telenzepine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.5
|
pKd
|
56
|
|
⤷ |
pKd
10.5
[56]
|
[3H]N-methyl scopolamine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.4 – 10.3
|
pKd
|
23,27-28,58,64-66,69,77
|
|
⤷ |
pKd
9.4 – 10.3
(Kd 4.2x10-10 – 5x10-11 M)
[23,27-28,58,64-66,69,77]
|
[3H]N-methyl scopolamine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.7
|
pKd
|
25,143
|
|
⤷ |
pKd
9.7
[25,143]
|
biperiden
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.3
|
pKd
|
11
|
|
⤷ |
pKd
9.3
(Kd 4.8x10-10 M)
[11]
|
Alexa-488-telenzepine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.3
|
pKd
|
56
|
|
⤷ |
pKd
9.3
[56]
|
[3H]darifenacin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.8
|
pKd
|
123
|
|
⤷ |
pKd
8.8
[123]
|
[3H]pirenzepine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.9
|
pKd
|
24,116,139,146
|
|
⤷ |
pKd
7.9
(Kd 1.4x10-8 M)
[24,116,139,146]
|
[3H]pirenzepine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.7 – 7.9
|
pKd
|
37,51
|
|
⤷ |
pKd
7.7 – 7.9
[37,51]
|
otenzepad
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.2
|
pKd
|
36
|
|
⤷ |
pKd
6.2
[36]
|
tiotropium
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.6 – 10.7
|
pKi
|
33,110,132,134
|
|
⤷ |
pKi
9.6 – 10.7
[33,110,132,134]
|
N-methyl scopolamine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.9
|
pKi
|
40
|
|
⤷ |
pKi
9.9
[40]
|
umeclidinium
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.8
|
pKi
|
73,115
|
|
⤷ |
pKi
9.8
(Ki 1.6x10-10 M)
[73,115]
|
propantheline
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.7
|
pKi
|
60
|
|
⤷ |
pKi
9.7
[60]
|
ipratropium
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.3 – 9.8
|
pKi
|
58,110
|
|
⤷ |
pKi
9.3 – 9.8
[58,110]
|
[3H](+)telenzepine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.4
|
pKi
|
37
|
|
⤷ |
pKi
9.4
[37]
|
revefenacin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.4
|
pKi
|
55
|
|
⤷ |
pKi
9.4
(Ki 4.17x10-10 M)
[55]
Description: Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM1 receptor, and displacement of [3H]NMS tracer.
|
atropine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.0 – 9.7
|
pKi
|
18,25,67
|
|
⤷ |
pKi
9.0 – 9.7
[18,25,67]
|
4-DAMP
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.3
|
pKi
|
34
|
|
⤷ |
pKi
9.3
[34]
|
dicyclomine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.1
|
pKi
|
5
|
|
⤷ |
pKi
9.1
(Ki 8.3x10-10 M)
[5]
|
atropine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.5 – 9.6
|
pKi
|
27,40,58,60,107,123
|
|
⤷ |
pKi
8.5 – 9.6
[27,40,58,60,107,123]
|
benzatropine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.0
|
pKi
|
99
|
|
⤷ |
pKi
9.0
(Ki 9.5x10-10 M)
[99]
Description: Displacement binding experiment using homogenised rat caudate putamen.
|
darifenacin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.9 – 9.1
|
pKi
|
45,58,122
|
|
⤷ |
pKi
8.9 – 9.1
[45,58,122]
|
scopolamine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.0
|
pKi
|
30,60
|
|
⤷ |
pKi
9.0
[30,60]
|
4-DAMP
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.9
|
pKi
|
67
|
|
⤷ |
pKi
8.9
[67]
|
trihexyphenidyl
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.9
|
pKi
|
5
|
|
⤷ |
pKi
8.9
(Ki 1.35x10-9 M)
[5]
|
tripitramine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.8
|
pKi
|
87
|
|
⤷ |
pKi
8.8
[87]
|
silahexocyclium
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.7
|
pKi
|
18
|
|
⤷ |
pKi
8.7
[18]
|
hexocyclium
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.6
|
pKi
|
18
|
|
⤷ |
pKi
8.6
[18]
|
oxybutynin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6
|
pKi
|
32,122
|
|
⤷ |
pKi
8.6
(Ki 2.4x10-9 M)
[32,122]
|
ethopropazine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.5
|
pKi
|
19
|
|
⤷ |
pKi
8.5
(Ki 3.1x10-9 M)
[19]
Description: Displacement of [H]QNB binding in rat forebrain brain homogenate.
|
tolterodine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.4 – 8.5
|
pKi
|
45,122
|
|
⤷ |
pKi
8.4 – 8.5
[45,122]
|
oxybutynin
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.2
|
pKi
|
98
|
|
⤷ |
pKi
8.2
[98]
|
hexahydrodifenidol
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.0
|
pKi
|
18
|
|
⤷ |
pKi
8.0
[18]
|
solifenacin
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.0
|
pKi
|
98
|
|
⤷ |
pKi
8.0
[98]
|
pirenzepine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.6 – 8.3
|
pKi
|
18,34,54,60,66,153
|
|
⤷ |
pKi
7.6 – 8.3
[18,34,54,60,66,153]
|
pirenzepine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.8 – 7.9
|
pKi
|
18,67
|
|
⤷ |
pKi
7.8 – 7.9
[18,67]
|
amitriptyline
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.8
|
pKi
|
126
|
|
⤷ |
pKi
7.8
(Ki 1.47x10-8 M)
[126]
|
methoctramine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.8
|
pKi
|
18
|
|
⤷ |
pKi
7.8
[18]
|
VU0255035
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.8
|
pKi
|
120
|
|
⤷ |
pKi
7.8
(Ki 1.487x10-8 M)
[120]
|
dosulepin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.7
|
pKi
|
126
|
|
⤷ |
pKi
7.7
(Ki 1.8x10-8 M)
[126]
|
hexahydrosiladifenidol
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.7
|
pKi
|
36
|
|
⤷ |
pKi
7.7
[36]
|
hexahydrosiladifenidol
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.4 – 7.9
|
pKi
|
18,67
|
|
⤷ |
pKi
7.4 – 7.9
[18,67]
|
solifenacin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.6
|
pKi
|
61,122
|
|
⤷ |
pKi
7.6
[61,122]
|
AFDX384
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.5
|
pKi
|
34
|
|
⤷ |
pKi
7.5
[34]
|
p-F-HHSiD
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.1 – 7.8
|
pKi
|
36,60
|
|
⤷ |
pKi
7.1 – 7.8
[36,60]
|
muscarinic toxin 1
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.3 – 7.6
|
pKi
|
40,52
|
|
⤷ |
pKi
7.3 – 7.6
[40,52]
|
guanylpirenzepine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.3 – 7.6
|
pKi
|
3,142
|
|
⤷ |
pKi
7.3 – 7.6
[3,142]
|
AQ-RA 741
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.2 – 7.5
|
pKi
|
34,45
|
|
⤷ |
pKi
7.2 – 7.5
[34,45]
|
muscarinic toxin 3
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.1
|
pKi
|
66
|
|
⤷ |
pKi
7.1
[66]
|
droxidopa
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.1
|
pKi
|
30
|
|
⤷ |
pKi
7.1
[30]
|
BODIPY-pirenzepine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.0
|
pKi
|
62
|
|
⤷ |
pKi
7.0
[62]
|
methoctramine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.6 – 7.3
|
pKi
|
34,36,54,123
|
|
⤷ |
pKi
6.6 – 7.3
[34,36,54,123]
|
himbacine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.7 – 7.1
|
pKi
|
34,66,95
|
|
⤷ |
pKi
6.7 – 7.1
[34,66,95]
|
(S)-dimetindene
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.7
|
pKi
|
21
|
|
⤷ |
pKi
6.7
(Ki 1.906x10-7 M)
[21]
Description: Binding to hM1 receptors expressed in CHO cells.
|
muscarinic toxin 2
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.4
|
pKi
|
52
|
|
⤷ |
pKi
6.4
[52]
|
otenzepad
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
5.9 – 6.3
|
pKi
|
18,67
|
|
⤷ |
pKi
5.9 – 6.3
[18,67]
|
lithocholylcholine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
5.6
|
pKi
|
25
|
|
⤷ |
pKi
5.6
[25]
|
ML381
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
<5.0
|
pKi
|
42
|
|
⤷ |
pKi
<5.0
(Ki >1x10-5 M)
[42]
|
aclidinium
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.1 – 10.2
|
pIC50
|
110,134
|
|
⤷ |
pIC50
10.1 – 10.2
[110,134]
|
glycopyrrolate
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.6 – 10.1
|
pIC50
|
128,132
|
|
⤷ |
pIC50
9.6 – 10.1
[128,132]
Description: Assay uses glycopyrronium bromide
|
solifenacin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.2
|
pIC50
|
109
|
|
⤷ |
pIC50
7.2
(IC50 6.35x10-8 M)
[109]
|
[18F](R,R)-quinuclidinyl-4-fluoromethyl-benzilate
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
-
|
-
|
70
|
|
⤷ |
[70]
|
|