TABLE B-2 Results of In Vitro Binding Studies: Displacement of Flunitrazepam in the Human Cortex

Drug

Kd (37§C) nMa

t1/2-off (min)b

Ratio to Kd Halcionc

Halcion

0.5 ± 0.01

5.3

1

Alpha-hydroxytriazolam

2.2 ± 0.06

 

4

Clonazepam

2.2 ± 0.2

3.4

4

Lorazepam

3.8 ± 0.2

 

8

Midazolam

4.9 ± 0.07

 

10

Diazepam

9.8 ± 0.7

 

20

Desmethyldiazepam

48 ± 2

 

96

Alprazolam

10.6 ± 0.4

3.4

21

Oxazepam

39 ± 3

 

78

Flurazepam

51 ± 2

4.6

102

Desalkylflurazepam

8.2 ± 0.3

 

16

Quazepam

58 ± 4

 

116

Desalkylflurazepam

8.2 ± 0.3

 

16

Temazepam

66 ± 1

 

132

Chlordiazepoxide

694 ± 8

 

>103

a Ratio of Kd of drug to Kd of Halcion

bt1/2-off, dissociation half-life.

cKd dissociation constant.

SOURCE: Richelson et al. (1991).



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