. 2010 Dec;62(4):588–631. doi: 10.1124/pr.110.003004

TABLE 2.

Reported activities of cannabinoid receptor ligands at recombinant GPR55 in various assays

The structures of all compounds listed are shown in Figures 1–5.

Ligand	[³⁵S]GTPγS Binding	ERK1/2 Phosphorylation	[Ca²⁺]_i Mobilization	β-Arrestin	GPR55 Internalization	RhoA Activation
LPI	EC₅₀ = 1 μM^a	EC₅₀ = 200 nM^a	30 nM^a	EC₅₀ = 3.6 μM^b	3 μM^c	1 μM^d,e
		1 μM^d,f	3 μM^g,h	EC₅₀ = 1.2 μM^c
			3 μM^c	EC₅₀ = 49 nMⁱ
			10 μM^j
Anandamide	EC₅₀ = 18 nM^k	10 μM^j	5 μM^g	Very weak agonist^b	N.E.^c	1 μM^k
			EC₅₀ = 7.3 μM^j	N.E.^c
2-AG	EC₅₀ = 3 nM^k	N.E.^a,c	N.E.^h,i	N.E.^c	N.E.^c	N.T.
Δ⁹-THC	EC₅₀ = 8 nM^k	N.E.^a	5 μM^g,h	N.E.^c	N.E.^c	5 μM^g
Cannabidiol	IC₅₀ = 350 nM^k	1 μM antagonist^d	N.E.^g	N.E.^c	N.E.^c	1–10 μM antagonist^d,k
Abn-CBD	EC₅₀ = 2.5 μM^k	N.E.^a	N.E.^g	N.E.^b,c	N.T.	N.T.
O-1602	EC₅₀ = 13 nM^k	1 μM^d	10 μM^j	N.E.^c	N.T.	1 μM^d,e,f
	EC₅₀ = 2.5 nM^l
CP55940	EC₅₀ =5 nM^k	10 μM antagonist^c	10 μM antagonistⁱ	K_i ∼200 nM^c	K_i ∼200 nM^c	N.T.
Rimonabant	N.T.	N.E.^a	1–2 μM antagonist^g,h,j	EC₅₀ = 9.3 μM^b	30 μM^c	N.T.
				EC₅₀ = 3.9 μM^c
AM251	EC₅₀ =39 nM^k	N.E.^a	N.T.	3 μM^b	30 μM^c	N.T.
				9.6 μM^c
AM281	EC₅₀ >30 μM^k	N.T.	N.T.	N.E.^c	N.E.^c	N.T.

N.E., no effect; N.T., not tested.

Oka et al. (2007): hGPR55 stably transfected in HEK293 cells with a tetracycline-inducible promoter.

Yin et al. (2009): hGPR55 transiently transfected in HEK293 cells.

Kapur et al. (2009): hGPR55E stably transfected in HEK293 cells (β-arrestin assay) or U2OS cells (β-arrestin and GPR55 internalization assays).

Whyte et al. (2009): human osteoclast primary cultures.

Whyte et al. (2009): mouse osteoclast primary cultures.

Pietr et al. (2009): BV-2 (mouse microglial cell line).

Lauckner et al. (2008): hGPR55 transiently transfected in HEK293 cells.

Lauckner et al. (2008): mouse DRG primary cultures.

ⁱ

Henstridge et al. (2009): hGPR55 stably transfected in HEK293 cells.

Waldeck-Weiermair et al. (2008): EA.hy926 (human umbilical vein derived endothelial cell line).

Ryberg et al. (2007): hGPR55 transiently transfected in HEK293s cells.

Johns et al. (2007): hGPR55 transiently transfected in HEK293T cells.