. Author manuscript; available in PMC: 2010 Mar 1.

Published in final edited form as: Prostaglandins Other Lipid Mediat. 2009 Jul 15;89(3-4):105–111. doi: 10.1016/j.prostaglandins.2009.07.001

Table 1.

Pharmacological profile of compounds tested as GPR55 ligands.

Compound	Cell type	Measured response [references]

		[³⁵S]GTPγS	[Ca²⁺]_i mobilization	pERK 1/2	RhoA	NAFT	β-Arrestin [36]
Cannabinoids
AEA	hGPR55-HEK293	EC₅₀ 18 nM [24]	5 µM [29]; no effect [32,35]	No effect [30,35]	1 µM [24]	-	Very weak
	EA.hy926	-	EC₅₀ 7.3 µM [28]	10 µM [28]	-	10 µM [28]	-
Meth-AEA	hGPR55-HEK293	-	5 µM [29]	-	-	-	-
	EA.hy926	-	EC₅₀ 10.6 µM [28] 5 µM [29]	-	-	-	-
OEA	hGPR55-HEK293	EC₅₀ 440 nM [24]	-	No effect [30]	-	-	-
PEA	hGPR55-HEK293	EC₅₀ 3–4 nM [24]	No effect [29]	No effect [30]	-	-	-
Virodhamine	hGPR55-HEK293	EC₅₀ 10–12 nM [24]	No effect [29]	No effect [30]	-	-	-
2-AG	hGPR55-HEK293	EC₅₀ 3 nM [24]	No effect [29,32,35]	No effect [30,35]	-	-	No effect
Noladin ether	hGPR55-HEK293	EC₅₀ 10–11 nM [24]	-		-	-
abnormal-CBD	hGPR55-HEK293	EC₅₀ 2.5 nM to 2.8 µM [20,24,31]	No effect [29]	No effect [30]	-	-	No effect
O1602	hGPR55-HEK293	EC₅₀ 2.5–13 nM [24,31]	No effect [35]	No effect [30]	1 µM [24]	-	No effect
CBD	hGPR55-HEK293	IC₅₀ 350 nM [24]	No effect [29]	-	Antagonist-10 µM [6]	-	-
	EA.hy926	-	10 µM [28]	-	1 µM [24]	-	No effect
O1918	EA.hy926	-	Antagonist [28]	-	-	-	-
Δ⁹THC	hGPR55-HEK293	EC₅₀ 8 nM [24]	5 µM [29]	5 µM [29]; No effect [30]	5 µM [29]	-	Weak
	Mouse DRG	-	5 µM [29]	-	-	-	-
HU210	hGPR55-HEK293	EC₅₀ 26–33 nM [10,24]	-	No effect [30]	-	-	No effect
CP55940	hGPR55-HEK293	EC₅₀ 5–7 nM [24]	No effect [29,35]; antagonist [32]	No effect [30]	-	-	No effect
WIN55212-2	hGPR55-HEK293	No effect [24,31]	No effect [29]	No effect [30]	No effect [24]	-	-
AM251	hGPR55-HEK293	EC₅₀ 39 nM [24]	-	-	-	-	EC₅₀ 2.7 µM
Rimonabant	hGPR55-HEK293	EC₅₀ 600 nM [24]	-	No effect [30]	-	-	EC₅₀ 9.3 µM
	Mouse DRG	-	Antagonist-2 µM [29]	-	-	-	-
JWH015	hGPR55-HEK293	EC₅₀ 4 nM [24]	3 µM [29]	3 µM [29]	3 µM [29]	-	-
	Mouse DRG	-	3 µM [29]	-	-	-	-
Lysophospholipids
LPI	hGPR55-HEK293	EC₅₀ 1 µM [30]	EC₅₀ 49 nM to 1 µM [30,32]	EC₅₀ 200 nM [30]	1 µM [32]	1 µM [32]	EC₅₀ 3.6 µM
	EA.hy926	-	10 µM [28]	-	-	-	-
	Mouse DRG	-	3 µM [29]	-	-	-	-
2-AG-LPI	hGPR55-HEK293	-	EC₅₀ 30 nM [35]	EC₅₀ 1 µM [35]	-	-	-