Cannabinoid Receptor

(R)-Monlunabant ((R)-MRI-1891) serves as a CB1 receptor antagonist utilized in obesity and metabolic disease research [1].

Monlunabant ((S)-MRI-1891), a solid dispersion compound, functions as an inhibitor of the cannabinoid CB1 receptor [1].

Delta8-THC acetate (Delta8-tetrahydrocannabinol) is a psychoactive cannabinoid that binds to the cannabinoid receptor 1 (CB1 receptor) and exhibits anti-nausea, appetite-stimulating, and anti-inflammatory effects. It may also offer neuroprotective benefits and has potential applications in research on anxiety and depression.

2'-Hydroxydaidzein is an isoflavonoid phytonutrient found in plant species, when a natural compound. 2'-Hydroxydaidzein has antioxidant activity, driven mainly by o-hydrogen bond dissociation enthalpy (BDE) and hydrogen atom transfer (HAT) mechanisms. 2'-Hydroxydaidzein inhibits chemical mediators in inflammatory cells and may be of value in the treatment and prevention of inflammatory diseases associated with excessive chemical mediator production. It may have a role in the treatment and prevention of central and peripheral inflammatory diseases associated with excessive chemical mediator production. 2'-Hydroxydaidzein inhibited the release of neutrophils and formyl-Met-Leu-Phe/cytochalasin B (fMLP/CB) in rats, with IC(50) values of 2.8+/-0.1 and 5.9+/-1.4 microM, respectively.

WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Kis of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively. Cannabinoid analogue WIN 55,212-2 Mesylate exhibited a novel anticancer effect against human tumors.

RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay.

Bay 59-3074 is a CB1/CB2 receptor partial agonist (Ki: 48.3/45.5 nM).

CB2R PAM, an oral drug, boosts CB2 receptor response to specific agonists, showing potential in neuropathic pain relief.

Compound 38-S is an orally active CB1R/AMPK modulator with a K i of 0.81 nM and an IC50 of 3.9 nM for CB1R.

CB2 receptor agonist 2 (ZINC72105556): potent, Ki=8.5 nM, high selectivity for CB2.

CB2R/FAAH modulator-2 (compound 26) is a dual modulator targeting at CB2R and FAAH.

Olivetol, found in lichens, is an organic antioxidant and THC synthesis precursor.

ML192 (CID1434953) is a selective GPR55 ligand antagonist.

(±)-Cannabichromene is a major non-psychotropic phytocannabinoid that inhibits endocannabinoid inactivation and activates the TRPA1.

ML-184 (CID2440433) is a potent synthetic agonist of GPR55 with EC50 of 0.26 μM.

SCH-336: potent, selective CB2 agonist (Ki=1.8 nM, EC50=2 nM), orally active, 100x CB2 vs. CB1 preference, reduces leukocyte migration and eosinophilia.

EHP-101 is a PPARγ/CB2 dual agonist with anti-inflammatory properties, inhibits fat formation, and combats diet-related obesity.

Pregnenolone (Arthenolone) is an endogenous steroid hormone synthesized from cholesterol, used in the treatment of Alzheimer's disease.

Taranabant: potent CB1 receptor inverse agonist; inhibits agonists with 0.13 nM Ki in vitro.

CB1-IN-1 (DBPR211) is a peripherally restricted CB1R antagonist, for CB1R and CB2R with Ki of 0.3 nM and 21 nM,respectively.