Ligand |
|
|
|
|
|
|
|
|
|
|
[3H]QNB
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.6 – 10.8
|
pKd
|
27,101
|
|
⤷ |
pKd
10.6 – 10.8
(Kd 2.51x10-11 – 1.58x10-11 M)
[27,101]
|
Cy3B-telenzepine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.5
|
pKd
|
54
|
|
⤷ |
pKd
10.5
[54]
|
[3H]N-methyl scopolamine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.4 – 10.3
|
pKd
|
23,26-27,56,61-63,65,73
|
|
⤷ |
pKd
9.4 – 10.3
(Kd 4.2x10-10 – 5x10-11 M)
[23,26-27,56,61-63,65,73]
|
[3H]N-methyl scopolamine
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.7
|
pKd
|
24,132
|
|
⤷ |
pKd
9.7
[24,132]
|
biperiden
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.3
|
pKd
|
11
|
|
⤷ |
pKd
9.3
(Kd 4.8x10-10 M)
[11]
|
Alexa-488-telenzepine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.3
|
pKd
|
54
|
|
⤷ |
pKd
9.3
[54]
|
[3H]darifenacin
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.8
|
pKd
|
115
|
|
⤷ |
pKd
8.8
[115]
|
[3H]pirenzepine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.9
|
pKd
|
135
|
|
⤷ |
pKd
7.9
(Kd 1.4x10-8 M)
[135]
|
[3H]pirenzepine
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.7 – 7.9
|
pKd
|
35,49
|
|
⤷ |
pKd
7.7 – 7.9
[35,49]
|
otenzepad
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.2
|
pKd
|
34
|
|
⤷ |
pKd
6.2
[34]
|
N-methyl scopolamine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.9
|
pKi
|
38
|
|
⤷ |
pKi
9.9
[38]
|
umeclidinium
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.8
|
pKi
|
69,109
|
|
⤷ |
pKi
9.8
(Ki 1.6x10-10 M)
[69,109]
|
propantheline
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.7
|
pKi
|
58
|
|
⤷ |
pKi
9.7
[58]
|
AE9C90CB
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.7
|
pKi
|
114
|
|
⤷ |
pKi
9.7
[114]
|
tiotropium
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.6
|
pKi
|
31
|
|
⤷ |
pKi
9.6
[31]
|
[3H](+)telenzepine
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.4
|
pKi
|
35
|
|
⤷ |
pKi
9.4
[35]
|
revefenacin
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.4
|
pKi
|
53
|
|
⤷ |
pKi
9.4
(Ki 4.17x10-10 M)
[53]
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
|
18,24,64
|
|
⤷ |
pKi
9.0 – 9.7
[18,24,64]
|
ipratropium
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.3
|
pKi
|
56
|
|
⤷ |
pKi
9.3
[56]
|
4-DAMP
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.2
|
pKi
|
32
|
|
⤷ |
pKi
9.2
[32]
|
dicyclomine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.1
|
pKi
|
5
|
|
⤷ |
pKi
9.1
(Ki 8.3x10-10 M)
[5]
|
atropine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.5 – 9.6
|
pKi
|
26,38,56,58,101,115
|
|
⤷ |
pKi
8.5 – 9.6
[26,38,56,58,101,115]
|
benzatropine
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.0
|
pKi
|
95
|
|
⤷ |
pKi
9.0
(Ki 9.5x10-10 M)
[95]
Description: Displacement binding experiment using homogenised rat caudate putamen.
|
scopolamine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.0
|
pKi
|
58
|
|
⤷ |
pKi
9.0
[58]
|
4-DAMP
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.9
|
pKi
|
64
|
|
⤷ |
pKi
8.9
[64]
|
trihexyphenidyl
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.9
|
pKi
|
5
|
|
⤷ |
pKi
8.9
(Ki 1.35x10-9 M)
[5]
|
tripitramine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.8
|
pKi
|
83
|
|
⤷ |
pKi
8.8
[83]
|
silahexocyclium
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.7
|
pKi
|
18
|
|
⤷ |
pKi
8.7
[18]
|
UH-AH 37
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6 – 8.7
|
pKi
|
43,142
|
|
⤷ |
pKi
8.6 – 8.7
[43,142]
|
hexocyclium
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.6
|
pKi
|
18
|
|
⤷ |
pKi
8.6
[18]
|
oxybutynin
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6
|
pKi
|
30,59,114
|
|
⤷ |
pKi
8.6
(Ki 2.4x10-9 M)
[30,59,114]
|
tolterodine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.5 – 8.7
|
pKi
|
43,114
|
|
⤷ |
pKi
8.5 – 8.7
[43,114]
|
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.
|
oxybutynin
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.2
|
pKi
|
94
|
|
⤷ |
pKi
8.2
[94]
|
pirenzepine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.8 – 8.3
|
pKi
|
18,32,52,58,63,142
|
|
⤷ |
pKi
7.8 – 8.3
[18,32,52,58,63,142]
|
hexahydrodifenidol
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.0
|
pKi
|
18
|
|
⤷ |
pKi
8.0
[18]
|
solifenacin
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
8.0
|
pKi
|
94
|
|
⤷ |
pKi
8.0
[94]
|
darifenacin
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.5 – 8.3
|
pKi
|
43,52,56,59,114
|
|
⤷ |
pKi
7.5 – 8.3
[43,52,56,59,114]
|
pirenzepine
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.8 – 7.9
|
pKi
|
18,64
|
|
⤷ |
pKi
7.8 – 7.9
[18,64]
|
amitriptyline
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.8
|
pKi
|
118
|
|
⤷ |
pKi
7.8
(Ki 1.47x10-8 M)
[118]
|
methoctramine
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.8
|
pKi
|
18
|
|
⤷ |
pKi
7.8
[18]
|
VU0255035
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.8
|
pKi
|
112
|
|
⤷ |
pKi
7.8
(Ki 1.487x10-8 M)
[112]
|
dosulepin
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.7
|
pKi
|
118
|
|
⤷ |
pKi
7.7
(Ki 1.8x10-8 M)
[118]
|
hexahydrosiladifenidol
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.7
|
pKi
|
34
|
|
⤷ |
pKi
7.7
[34]
|
hexahydrosiladifenidol
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.4 – 7.9
|
pKi
|
18,64
|
|
⤷ |
pKi
7.4 – 7.9
[18,64]
|
solifenacin
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.6
|
pKi
|
59,114
|
|
⤷ |
pKi
7.6
[59,114]
|
AFDX384
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.5
|
pKi
|
32
|
|
⤷ |
pKi
7.5
[32]
|
p-F-HHSiD
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.1 – 7.8
|
pKi
|
34,58
|
|
⤷ |
pKi
7.1 – 7.8
[34,58]
|
muscarinic toxin 1
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.3 – 7.6
|
pKi
|
38,50
|
|
⤷ |
pKi
7.3 – 7.6
[38,50]
|
guanylpirenzepine
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.3 – 7.6
|
pKi
|
3,131
|
|
⤷ |
pKi
7.3 – 7.6
[3,131]
|
AQ-RA 741
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.2 – 7.5
|
pKi
|
32,43
|
|
⤷ |
pKi
7.2 – 7.5
[32,43]
|
muscarinic toxin 3
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.1
|
pKi
|
63
|
|
⤷ |
pKi
7.1
[63]
|
BODIPY-pirenzepine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.0
|
pKi
|
60
|
|
⤷ |
pKi
7.0
[60]
|
methoctramine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.6 – 7.3
|
pKi
|
32,34,52,115
|
|
⤷ |
pKi
6.6 – 7.3
[32,34,52,115]
|
himbacine
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.7 – 7.1
|
pKi
|
32,63,91
|
|
⤷ |
pKi
6.7 – 7.1
[32,63,91]
|
(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
|
50
|
|
⤷ |
pKi
6.4
[50]
|
otenzepad
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
5.9 – 6.3
|
pKi
|
18,64
|
|
⤷ |
pKi
5.9 – 6.3
[18,64]
|
lithocholylcholine
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
5.6
|
pKi
|
24
|
|
⤷ |
pKi
5.6
[24]
|
ML381
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
<5.0
|
pKi
|
40
|
|
⤷ |
pKi
<5.0
(Ki >1x10-5 M)
[40]
|
glycopyrrolate
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.9
|
pIC50
|
120
|
|
⤷ |
pIC50
9.9
(IC50 1.26x10-10 M)
[120]
Description: Assay uses glycopyrronium bromide
|
aclidinium
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.9
|
pIC50
|
104
|
|
⤷ |
pIC50
9.9
(IC50 1.4x10-10 M)
[104]
Description: Human M1 receptors expressed in CHO-K1 cells
|
solifenacin
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.2
|
pIC50
|
103
|
|
⤷ |
pIC50
7.2
(IC50 6.35x10-8 M)
[103]
|
[18F](R,R)-quinuclidinyl-4-fluoromethyl-benzilate
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
-
|
-
|
66
|
|
⤷ |
[66]
|
|