Home GPCR & G Protein Cannabinoid Receptor

Cannabinoid Receptor

As a member of the cannabinoid receptor family, CB2 receptors (Cannabinoid receptor 2), a G protein-coupled receptor, can modulate adenylyl cyclase and MAP kinase activity, through their ability to couple to Gi/o proteins. CB2 receptor stimulation is believed not to modulate ion channel function.Cannabinoids not only can bid to CB2 receptor, but also can modulate the activity of other receptor types including Opioid receptors, NMDA receptor, and nAChRs. Cannabinoids activate p42/p44 MAP kinase in CHO cells and HL-60 cells expressing the CB2 receptor. Cannabinoids were also shown to induce the expression of krox-24 through a PKC-dependent activation of MAP kinase.

Other GPCR & G Protein Related Inhibitors

VEGFR EGFR c-Met CSF-1R IGF-1R c-Kit ALK Tie-2 HER2 c-RET Trk receptor

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S1544 AM1241 AM-1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, and this compound exhibits 82-fold selectivity over CB1 receptor.
Cell Rep, 2025, 44(4):115559
CNS Neurosci Ther, 2025, 31(8):e70591
Redox Rep, 2024, 29(1):2420572
Verified customer review of AM1241
S2819 AM251 AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.
Biol Pharm Bull, 2025, 48(6):769-781
Pharmacol Res, 2023, 194:106864
Physiol Rep, 2023, 11(1):e15565
Verified customer review of AM251
S3021 Rimonabant (SR141716) Rimonabant (SR141716) is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane, and it is also a dual inhibitor of acyl CoA:cholesterol acyltransferases(ACAT) 1 and 2 that inhibits mycobacterial MmpL3.
Biol Pharm Bull, 2025, 48(6):769-781
Toxicol Lett, 2023, 374:48-56
Int J Biol Sci, 2022, 18(4):1401-1414
S8012 Otenabant (CP-945598) HCl Otenabant (CP-945598) HCl is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. Phase 1.
Nat Commun, 2020, 11(1):71
Gastric Cancer, 2018, 10.1007/s10120-018-0859-1
S2854 BML-190 BML-190 (IMMA) is a selective cannabinoid CB2 receptor inverse agonist with Ki of 435 nM, with 50-fold selectivity over CB1 receptor.
Int J Mol Sci, 2020, 21(7)
University of Alberta, 2014, Yahya Muhammad Fiteih
Verified customer review of BML-190
S8033 6-Iodopravadoline (AM630) AM630 (6-Iodopravadoline) is a selective cannabinoid CB2 receptor antagonist with Ki of 31.2 nM.
Brain Behav Immun, 2023, 110:60-79
Pharmacol Res, 2023, 194:106864
S2778 GW842166X GW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2.
Nat Commun, 2020, 11(1):71
S1534 Org 27569 Org 27569 is an allosteric modulator of cannabinoid CB1 receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity.
Biochem Pharmacol, 2024, 224:116190
ACS Infect Dis, 2021, 10.1021/acsinfecdis.0c00754
S8017 WIN 55, 212-2 mesylate WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent cannabinoid (CB) receptor agonist with Ki of 3.3 nM and 62.3 nM for human recombinant CB2 and CB1, respectively. WIN 55,212-2 Mesylate regulates Glutamate transmission.
Eur Arch Psychiatry Clin Neurosci, 2022, 10.1007/s00406-022-01437-1
E4945 Pregnenolone monosulfate sodium Pregnenolone monosulfate sodium, a sodium salt form of pregnenolone monosulfate, is an active neurosteroid and a precursor of all steroid hormones. It functions act as a potent endogenous allosteric signal-specific inhibitor of CB1 receptors, reducing psychoactive effects associated with Δ9-tetrahydrocannabinol (THC).

Signaling Pathway Map