Biomedical Engineering Reference
In-Depth Information
O
O
N
H
MeO
N
OH
N
H
N
Cl
H
O
O
Cl
Cl
JHW 133
GW 405833
SR 144528
FIGURE 19.13
Agonists and antagonists for CB
2
-receptor.
19.2.9 D
IACYLGLYCEROL
L
IPASE
I
NHIBITORS
There are no really specii c inhibitors of diacylglycerol lipase, but RHC 80267, tetrahydrolipstatin
(Orlistat), and O-3841 have been used in experimental settings (Figure 19.14).
N
H
O
PF
O
O
O
O
O
O
O
O
OMe
Tetrahydrolipstatin
RHC 80267
O
N
O
N
N
H
O
O
O-3841
FIGURE 19.14
Inhibitors of diacylglycerol lipase, the enzyme generating 2-arachidonoylglycerol.
19.2.10 M
ONOACYLGLYCEROL
L
IPASE
I
NHIBITORS
URB602 (Figure 19.15) is used as an inhibitor of monoacylglycerol lipase in experimental settings,
but is not a very specii c inhibitor.
As can be seen from the description of the enzyme inhibitors above, this research area is at
the very early stage of drug discovery, but if potent and specii c inhibitors can be found, there are
numerous clinical settings where such enzyme inhibitors may be alternatives to cannabinoid recep-
tor agonists or antagonists.
N
O
O
URB602
FIGURE 19.15
Inhibitor of monoacylglycerol lipase, the enzyme degrading 2-arachidonoylglycerol.
