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.
GPR55 Agonists |
|
|---|---|
| Cat. No. | 产品名称/活性 |
| 1117 | AM 251 |
| GPR55 agonist; also CB1 antagonist | |
| 6668 | ML 184 |
| Selective GPR55 agonist; also promotes NSC proliferation and differentiation | |
| 2797 | O-1602 |
| Potent GPR55 agonist | |
| 1484 | Oleylethanolamide |
| GPR55 agonist; also PPARα agonist | |
| 0879 | Palmitoylethanolamide |
| Selective GPR55 agonist. FAAH and PAA substrate | |
GPR55 Antagonists |
|
| Cat. No. | 产品名称/活性 |
| 4959 | CID 16020046 |
| Selective GPR55 antagonist | |
| 4860 | ML 193 |
| Potent, selective GPR55 antagonist | |
Other |
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| Cat. No. | 产品名称/活性 |
| 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* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Cannabinoid Receptor Ligands Scientific Review
Written by Roger Pertwee, this review discusses compounds which affect the activity of the endocannabinoid system, focusing particularly on ligands that are most widely used as experimental tools and denotes compounds available from Tocris.
Our Cannabinoid review gives an overview of the pharmacological ligands used to study the cannabinoid CB1 and CB2 receptors.
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