|
|
Human muscarinic receptor subtype
|
|
Drug
|
m1
|
m2
|
m3
|
m4
|
m5
|
|
Geometric mean of Kd
(nM)
|
|
|
|
|
|
|
|
|
Antidepressantsa
|
|
|
|
|
|
|
Amitriptyline
|
14.7
|
11.8
|
12.8
|
7.2
|
15.7
|
|
Bupropion
|
>35,000
|
>35,000
|
>35,000
|
>35,000
|
>35,000
|
|
Etoperidone
|
>35,000
|
>35,000
|
>35,000
|
>35,000
|
>35,000
|
|
Femoxetine
|
92
|
150
|
220
|
470
|
400
|
|
Fluoxetine
|
1030
|
2700
|
1000
|
2900
|
2700
|
|
Lofepramine
|
67
|
330
|
130
|
340
|
460
|
|
Paroxetine
|
300
|
340
|
80
|
320
|
650
|
|
Sertraline
|
1300
|
2100
|
1300
|
1400
|
1900
|
|
Venlafaxine
|
>35,000
|
>35,000
|
>35,000
|
>35,000
|
>35,000
|
|
|
|
|
|
|
|
|
Antimuscarinicsb
|
|
|
|
|
|
|
Benztropine
|
0.231
|
1.4
|
1.1
|
1.1
|
2.8
|
|
Biperiden
|
0.48
|
6.3
|
3.9
|
2.4
|
6.3
|
|
Pirenzepine
|
8
|
270
|
150
|
28
|
170
|
|
Procyclidine
|
4.6
|
25
|
12.4
|
7
|
24
|
|
Scopolamine
|
1.1
|
2.0
|
0.4
|
0.8
|
2.1
|
|
Trihexyphenidyl
|
1.6
|
7.0
|
6.4
|
2.6
|
15.9
|
|
|
|
|
|
|
|
|
Neurolepticsb,c
|
|
|
|
|
|
|
Chlorpromazine
|
25
|
150
|
67
|
40
|
42
|
|
Chlorprothixene
|
11
|
28
|
22
|
18
|
25
|
|
Clozapine
|
3.1
|
48
|
20
|
11
|
11
|
|
Fluperlapine
|
8.8
|
71
|
41
|
14
|
17
|
|
Melperone
|
15.000
|
2400
|
15,000
|
4400
|
15,000
|
|
Mesoridazine
|
10
|
15
|
90
|
19
|
60
|
|
Rilapine
|
190
|
470
|
1400
|
1000
|
1100
|
|
Risperidone
|
11.000
|
3700
|
13,000
|
2900
|
15,000
|
|
Thioridazine
|
2.7
|
14
|
15
|
9
|
13
|
|
Zotepine
|
18
|
140
|
73
|
77
|
260
|
|