3. Aminoalkylindole: Members of aminoalkylindole group have different structures
from both the classical and non-classical cannabinoids. R-(+)-WIN 55,212-2 is
the most studied member of this group which has the similar intrinsic activity as
CP55940 and HU-210. However, it possesses higher CB2 affinity than CB1.
4. Eicosanoids: They are endogenous fatty acid amides. Endocannabinoids like
anandamide and 2-AG are classified as the members of this group. They have
lower affinity and relative intrinsic activity for CB2 receptor in comparison to
CB1 receptor. Two other compounds included in this group are virodhamine and
N-arachidonoyl dopamine (Table 12.1).
12.5
Pathophysiological Role of Cannabinoid System in Human
Diseases
Over the years, various preclinical researches have confirmed the involvement of
endocannabinoid system (ECS) components in different pathophysiological
conditions and diseases. In this section, we will discuss briefly the implications of
ECS components in different human diseases (Fig. 12.2).
Table 12.1 Ligands and their interaction with the receptors
S. no.
Ligand
CB1
receptor
CB2
receptor
Agonist
Antagonist
GPR55
receptor
agonist
1
Tetrahydrocannabinol
(THC)
✓
✓
✓
–
–
2
WIN 55,212-2
✓
✓
–
–
–
3
Cannabidiol (CBD)
✓
✓
–
✓
–
4
Arachidonyl-
20-chloroethylamide
(ACEA)
✓
–
✓
–
–
5
Anandamide (AEA)
✓
✓
✓
–
✓
6
JWH015
–
✓
✓
–
–
7
AM251
✓
–
–
✓
✓
8
GW405,833 (GW)
–
–
–
9
JWH-133
–
✓
✓
–
✓
10
2-
Arachidonoylgylcerol
(2-AG)
✓
✓
✓
–
✓
11
CP 55940
✓
✓
✓
–
✓
✓(tick mark) represents the binding affinity of ligand toward the particular receptor
12
Emerging Role of Cannabinoid System Modulators in Treatment of Cancer
183