TABLE 2. Binding of antidepressants, antimuscarinics, and neuroleptics to human muscarinic receptor subtypes

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

a Data from ref. (82).

b Data from ref. (14)

c All but chlorpromazine, chlorprothixene, mesoridazine, and thioridaze are considered atypical neuroleptics.

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published 2000