Cannabinoid Receptors

Cannabinoid receptors are currently classified into three groups: central (CB1), peripheral (CB2) and GPR55, all of which are G-protein-coupled.

Cannabinoid Receptor Target Files

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CB1 receptors are primarily located at central and peripheral nerve terminals. CB2 receptors are predominantly expressed in non-neuronal tissues, particularly immune cells, where they modulate cytokine release and cell migration. Recent reports have suggested that CB2 receptors may also be expressed in the CNS. GPR55 receptors are non-CB1/CB2 receptors that exhibit affinity for endogenous, plant and synthetic cannabinoids. Endogenous ligands for cannabinoid receptors have been discovered, including anandamide and 2-arachidonylglycerol.

Receptor Subtype CB1 CB2 GPR55
Transduction Mechanism ↓Adenylyl Cyclase (Gi/o), ↓ N- and P/Q-type Ca2+ currents, ↑ Kir and A-types K+ currents ↓ Adenylyl Cyclase (Gi/o) Activation of Rho family GTPases
Primary Distribution CNS: hippocampus, basal ganglia, cerebellum, cortex, globus pallidus, substantia nigra, pars reticulata Spleen, tonsils, immune cells CNS: caudate and putamen
Tissue Function Modulation of neurotransmitter release Suppression of immune cell function Pain signaling, control of vascular tone, inflammation

Key Compounds Ki Values (nM) at CB1 Ki Values (nM) at CB2
Endogenous Agonists Anandamide (1339)
2-Arachidonylglycerol (1298)
NADA (1568)
Noladin ether (1411)
61-543
58.3-472
2501
21.2
279-1940
145-1400
12001
> 3000
Key CB1 Agonists ACEA (1319)
ACPA (1318)
(R)-(+)-Methanandamide (1121)
1.4
2.2
17.9-28.3
> 2000
715
815-868
Key CB2 Agonists CB 65 (2663)
GP 1a (2764)
GP 2a (2678)
GW 405833 (2374)*
JWH 015 (1341)
JWH 133 (1343)
L-759,656 (2434)
L-759,633 (2433)
> 1000
363
900
4772
383
677
4888
1043
3.3
0.037
7.6
3.92
13.8
3.4
11.8
6.4
Non-selective Agonists CP 55,940 (0949)
HU 210 (0966)
O-2545 (2680)
WIN 55,212-2 (1038)
Bay 59-3074 (2500)
Δ9-Tetrahydrocannabinol
0.5-5.0
0.06-0.73
1.5
5.05
1.89-123
48.3
5.05
0.69-2.8
0.17-0.52
0.32
3.13
0.28-16.2
45.5
3.13
Key CB1 Antagonists/
Inverse Agonists
AM 251 (1117)
AM 281 (1115)
LY 320135 (2387)
7.49
12
141
2290
4200
14900
Key CB2 Antagonists/
Inverse Agonists
AM 630 (1120) 5152 31.2

*partial agonist

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