1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. GPR55

GPR55

G protein-coupled receptor 55

GPR55 (G protein-coupled receptor 55) is a G protein-coupled receptor that in humans is encoded by the GPR55 gene. GPR55, along with GPR119 and GPR18, have been implicated as novel cannabinoid receptors. GPR55 is activated by the plant cannabinoids 9-THC and cannabidiol, and the endocannabinoids anandamide, 2-AG, noladin ether in the low nanomolar range. Recent research suggests that lysophosphatidylinositol and its 2-arachidonoyl derivative may be the endogenous ligands for GPR55, and the receptor appears likely to be a possible target for treatment of inflammation and pain as with the other cannabinoid receptors. The physiological role of GPR55 is unclear. GPR55 has been proposed as a new potential drug target for the treatment of diabetes, Parkinson’s disease, neuropathic pain, and cancer.

GPR55 Related Products (7):

Cat. No. Product Name Effect Purity
  • HY-16697
    CID 16020046
    Antagonist 99.87%
    CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function.
  • HY-103336
    Tocrifluor 1117
    Agonist
    Tocrifluor 1117 (T1117), a fluorescent form of the cannabinoid CB1 receptor antagonist AM251 (HY-15443), is a selective fluorescent GPR55 ligand. Tocrifluor 1117 is a potent tool for identifying the cellular location of cannabinoid receptors (including GPR55 in living tissues) (Ex/Em=543/590 nm).
  • HY-125111
    PSB-SB-487
    Antagonist
    PSB-SB-487 is a potent GPR55 antagonist and CB2 agonist with an IC50 value of 0.113 µM for GPR55, and a Ki value of 0.292 µM for human CB2. PSB-SB-487 can be used for researching diabetes, Parkinson’s disease, neuropathic pain, and cancer.
  • HY-116461
    ML-184
    Agonist 99.53%
    ML-184 (CID2440433) is a selective GPR55 agonist with an EC50 of 250 nM and exhibits >100-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-184 induces phosphorylation of ERK1/2 and translocation of PKCβII to the plasma membrane by activating GPR55. ML-184(CID2440433) increases proliferation of neural stem cells and promotes neuronal differentiation in vitro.
  • HY-111083
    ML191
    Antagonist
    ML-191 is an antagonist of GPR55. It inhibits GPR55 signaling induced by lysophosphatidylinositol (EC50=1.076 µM in U2OS cells overexpressing GPR55). ML-191 inhibits LPI-induced phosphorylation of ERK1/2 (IC50=328 nM) and receptor-dependent translocation of PKCβII when used at a concentration of 30 µM.
  • HY-116637
    Tetrahydromagnolol
    Antagonist
    Tetrahydromagnolol (Magnolignan), a main metabolite of Magnolol, is a potent and selective cannabinoid CB2 receptor agonist with an EC50 of 170 nM and a Ki of 416 nM. Tetrahydromagnolol possesses 20-fold more selective for CB2 receptor than CB1 receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist.
  • HY-110125
    ML-193
    Antagonist 98.74%
    ML-193 (CID 1261822) is a potent and selective antagonist of GPR55, with an IC50 of 221 nM. ML-193 shows more than 27-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-193 can improve the motor and the sensorimotor deficits of Parkinson’s disease (PD) rats.