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

TABLE 6.

Cannabinoids, endogenous lipids, and synthetic CB₁ and/or CB₂ receptor ligands that interact with TRP receptors

Compound	TRPV1		TRPV2	TRPM8	TRPA1
Compound	Calcium Assay or Mesenteric Artery Tension	Currents by Patch Clamp	TRPV2	TRPM8	TRPA1
Anandamide	EC₅₀ = 1.15 μM^a; EC₅₀ = 0.63 μM^b; EC₅₀ = 0.16 μM^c (rat TRPV1)	EC₅₀ = 4.9 μM^d; EC₅₀ = 2.5 μM^e	N.E. at 100 μM^f	IC₅₀ = 0.15 μM (HEK293 cells) or 10 μM (DRG neurons) (vs. icilin); IC₅₀ = 3.1 μM (vs. menthol in HEK293 cells)^g,h	EC₅₀ = 4.9 μMⁱ
2-AG	N.E. at 10 μM^b; EC₅₀ = 8.4 μM^f	N.T.	N.E. at 100 μM^f	N.E.	N.T.
NADA	EC₅₀ = 26 nM^b	EC₅₀ = 1.6 μM (DRG); 794 nM (TG)^j	N.T.	IC₅₀ = 0.7 μM (vs. icilin); IC₅₀ = 2.0 μM (vs. menthol)^g	N.E. at 10 μM^k
OEA	EC₅₀ = 3.7 μM^l; EC₅₀ = 0.4 μM^c	EC₅₀ = 6.3 μM^c	N.T.	N.T.	N.T.
Δ⁹-THC	N.E. at 100 μM^f	N.T.	EC₅₀ = 15.5 μM^f	IC₅₀ = 0.16 μM (vs. icilin); IC₅₀ = 0.15 μM (vs. menthol)^h	EC₅₀ = 12 ± 2 μM^m; EC₅₀ = 32.3 μM^f; EC₅₀ = 0.23 μM^h in HEK293 cells
HU-210	EC₅₀ = 1.2 μM but very low maximal effect^b; no effect at 100 μM^f	N.T.	Slight agonism at 100 μM^f	N.T.	N.E. at 100 μM^f
CP55940	N.E. at 100 μM^f	N.T.	Slight effect at 100 μM^f	N.T.	Slight effect at 100 μM^f
R-(+)-WIN55212	Slight effect at 100 μM^f	N.T.	N.E. at 100 μM^f	N.T.	EC₅₀ = 9.8 μM^f
Rimonabant	Antagonist 1–5 μMⁿ	N.T.	N.T.	IC₅₀ = 52.3 nM vs. icilin; no effect vs menthol^g	N.T.
JWH-015	EC₅₀ = 41.2 μM^f	N.T.	N.E. at 100 μM^f	N.T.	Slight effect at 100 μM^f
Cannabidiol	EC₅₀ = 3.5 μM (human)^o; very little effect (rat)^f	N.T.	EC₅₀ = 3.7 μM^f	IC₅₀ = 80 nM (vs. icilin); IC₅₀ = 0.14 μM (vs. menthol)^h	>10 μM^m; EC₅₀ = 96 nM^h in HEK293 cells; EC₅₀ = 81.4 μM^f
Cannabinol	N.E. at 100 μM^f	N.T.	EC₅₀ = 77.7 μM^f	IC₅₀ = 0.21 μM (vs. icilin)^k	>10 μM^m; very little effect at 100 μM^f; EC₅₀ = 0.18 μM in HEK293 cells^k
Cannabichromene	EC₅₀ >50 μM^p	N.T.	N.T.	40 μM (vs. icilin)^k	EC₅₀ = 60 nM^h
Cannabigerol	EC₅₀ = 11.5 μM^p	N.T.	N.T.	IC₅₀ = 0.14 μM (vs. icilin); IC₅₀ = 0.16 μM (vs. menthol)^h	EC₅₀ = 3.4 μM^h

N.E., no effect; N.T., not tested; NADA, N-arachidonoyl dopamine; OEA, oleoyl ethanolamide; TG, trigeminal ganglia.

Smart et al., 2000.

De Petrocellis et al., 2000.

Movahed et al., 2005.

Zygmunt et al., 1999.

Roberts et al., 2002.

Qin et al., 2008.

De Petrocellis et al., 2007.

De Petrocellis et al., 2008.

ⁱ

De Petrocellis and Di Marzo, 2009.

McDonald et al., 2008.

L. De Petrocellis and V. Di Marzo, unpublished observations.

Appendino et al., 2009.

Jordt et al., 2004.

ⁿ

De Petrocellis et al., 2001.

Bisogno et al., 2001.

Ligresti et al., 2006.