Biomedical Engineering Reference
In-Depth Information
19.2.6 FAAH-I
NHIBITORS
AND
A
NANDAMIDE
U
PTAKE
I
NHIBITORS
As discussed above it is not clear whether an anandamide transporter exists and several compounds
believed to be uptake inhibitors have turned out to be inhibitors of FAAH. URB597 is shown as an
example of a experimental FAAH-inhibitor (Figure 19.11).
O
NH
2
N
O
O
URB597
FIGURE 19.11
Inhibitor of FAAH, the enzyme degrading anandamide and other acylethanolamides.
19.2.7 CB
1
-R
ECEPTOR
A
GONIST
/A
NTAGONIST
Besides THC, anandamide, and 2-AG, experimentally used synthetic CB
1
-receptor agonists involves
CP55,940 and the aminoalkylindole WIN55,212-2 that target both the cannabinoid receptors. More
selective CB
1
-receptor agonists are arachidonic acid derivatives like O-1812. Selective CB
1
-receptor
antagonist involves rimonabant that are in clinical use and the experimental compounds AM251
and LY 320135 (Figure 19.12).
O
OH
O
OH
H
OH
O
N
CN
N
O
HO
O-1812
CP 55,940
WIN 55,212-2
O
O
N
N
H
H
CN
O
N
N
N
N
l
Cl
OMe
Cl
Cl
O
MeO
Cl
Cl
Rimonabant
AM251
LY 320135
FIGURE 19.12
Agonists and antagonists for CB
1
-receptor.
19.2.8 CB
2
-R
ECEPTOR
A
GONIST
/A
NTAGONIST
THC, 2-AG, and to a lesser extent anandamide activates the CB
2
-receptor. Selective synthetic ago-
nists include JHW 133 and GW 405833 (partial agonist) that are used experimentally (Figure 19.13).
SR 144528 is a selective CB
2
-receptor antagonist.
