GPR55

GPR55 is a previously orphan receptor that exhibits affinity for endogenous, plant and synthetic cannabinoids, as well as lysophosphatidylinositols (LPIs), which are suggested to be its endogenous ligand.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
1297 Abn-CBD
Selective GPR55 agonist; neurobehaviorally inactive
1117 AM 251
GPR55 agonist; also CB1 antagonist
1411 Noladin ether
Endogenous agonist for GPR55 and CB1
2797 O-1602
Potent GPR55 agonist
1484 Oleylethanolamide
GPR55 agonist; also PPARα agonist
0879 Palmitoylethanolamide
Selective GPR55 agonist. FAAH and PAA substrate

Antagonists

Cat No Product Name / Activity
4959 CID 16020046
Selective GPR55 antagonist
4860 ML 193
Potent, selective GPR55 antagonist

Other

Cat No Product Name / Activity
2540 Tocrifluor T1117
Novel fluorescent cannabinoid ligand; displays GPR55 binding activity

GPR55 is a previously orphan receptor that exhibits affinity for endogenous, plant and synthetic cannabinoids, as well as lysophosphatidylinositols (LPIs), which are suggested to be its endogenous ligand. The effects of cannabinoid ligands that are inactive at CB1 and CB2, e.g. palmitoylethanolamide, are thought to be mediated through GPR55.

GPR55 is coupled to both the Gα12/13 and the Gαq intracellular pathways and displays complex pharmacology, with ligands having functional selectivity, also known as biased agonism. Some investigations show that the effects of LPI binding are mediated through Gαq and PLCβ, with the effects of virodhamine (O-arachidonoyl ethanolamine; O-AEA) being mediated through by Gα13, Rho, ROCK and PLCε. However, other studies show that LPI binding can activate the Gα13, Rho, ROCK pathway.

GPR55 mRNA is expressed in the brain, most abundantly in the caudate nucleus and putamen, with lower levels in the hippocampus, thalamus, pons, cerebellum and frontal cortex. Peripherally, GPR55 mRNA is present in the spleen, adrenals and parts of the gastrointestinal tract. Putative physiological roles of GPR55 include pain signaling, control of vascular tone and inflammation. The human GPR55 receptor gene is localized to chromosome 2q36.3.

External sources of pharmacological information for GPR55 :

    Literature for GPR55

    Tocris offers the following scientific literature for GPR55 to showcase our products. We invite you to request* or download your copy today!

    *Please note that Tocris will only send literature to established scientific business / institute addresses.


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    GPR55 Gene Data

    Species Gene Symbol Gene Accession No. Protein Accession No.
    Human GPR55 NM_005683 Q9Y2T6
    Mouse Gpr55 NM_001033290 Q3UJF0
    Rat Gpr55 XM_576605 Q9WU09