128
8
GABA A receptor
γ-aminobutyric acid
ENDOGENOUS:
Anistatin
Allosteric
negative
modulator
Bicuculline
-
Barbituric acid
Allosteric
positive
modulator
Cicutoxin
-
Muscimol
+
Diazepam (Valium, Faustan)
Allosteric
positive
modulator
Thujone
Allosteric
negative
modulator
Valerenic acid
Allosteric
positive
modulator
Chlordiazepoxide (Librium)
Allosteric
positive
modulator
Picrotoxinin
Allosteric
negative
modulator
HO
O
O
O
O
O
O
N
N
N
HO
HO
O
H
N
N
C I
O
O
H
H 2 N
O
OH
OH
O
O
O
O
O
O
O
N
H
H
O
O
O
HO
H
HO
HO
C
C
C
C
OH
HN
NH
O
O
O
O
N
H
H
CI
H
H
OH
NH 2
. Fig. 8.4 Examples of natural compounds that act as agonists and antagonists as well as positive and
negative allosteric modulators of the GABA A receptor
Chapter 8 · Plant-Derived Drugs Affecting Ion Channels
8
GABA A receptor
γ-aminobutyric acid
ENDOGENOUS:
Anistatin
Allosteric
negative
modulator
Bicuculline
-
Barbituric acid
Allosteric
positive
modulator
Cicutoxin
-
Muscimol
+
Diazepam (Valium, Faustan)
Allosteric
positive
modulator
Thujone
Allosteric
negative
modulator
Valerenic acid
Allosteric
positive
modulator
Chlordiazepoxide (Librium)
Allosteric
positive
modulator
Picrotoxinin
Allosteric
negative
modulator
HO
O
O
O
O
O
O
N
N
N
HO
HO
O
H
N
N
C I
O
O
H
H 2 N
O
OH
OH
O
O
O
O
O
O
O
N
H
H
O
O
O
HO
H
HO
HO
C
C
C
C
OH
HN
NH
O
O
O
O
N
H
H
CI
H
H
OH
NH 2
. Fig. 8.4 Examples of natural compounds that act as agonists and antagonists as well as positive and
negative allosteric modulators of the GABA A receptor
Chapter 8 · Plant-Derived Drugs Affecting Ion Channels
