Home GPCR & G Protein Cannabinoid Receptor

Cannabinoid Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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).
E0458 RTICBM-189 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.
E1841 Monlunabant Monlunabant (INV-202, (S)-MRI-1891) is a peripherally acting inverse agonist of the cannabinoid type-1 receptor (CB1R), with the potential to treat respiratory and renal complications associated with metabolic disorders. It improves lung compliance in a mouse model of asthma and reduces renal fibrosis in a streptozotocin-induced diabetic nephropathy mouse model.
E4585 N-Arachidonyldopamine N-Arachidonyldopamine is a potent agonist of Cannabinoid Receptor 1 (CB1), with a Ki of 250 nM in rat brain membranes, showing 40-fold selectivity for CB1 over CB2 receptors. It also triggers intracellular calcium mobilisation in N18TG2 neuroblastoma cells.
E4858 Rimonabant hydrochloride Rimonabant hydrochloride (SR 141716A hydrochloride) is a highly potent and selective antagonist of the central Cannabinoid Receptor (CB1), with a Ki of 1.8 nM. It is an anorectic anti-obesity drug with potential to treat obesity and cardiovascular risk factors.
S9048 (+)-Gallocatechin (+)-Gallocatechin, found notably in green tea, has moderate affinity to the human cannabinoid receptor and acts as an antioxidant.
S0412 Bay 59-3074 Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki of 55.4 nM, 48.3 nM and 45.5 nM at rat and human CB1 and human CB2 receptors, respectively. This compound displays analgesic properties.
S9413 Yangonin Yangonin (Y100550) is a dienolide kavalactone originally found in Piper methysticum (kava plant) and exhibits neuroprotective, neuromodulatory, and antifungal activities. It activates cannabinoid (CB1) receptors and potentiates the effects of GABA-A receptors.
S6735 JD-5037 JD-5037 is a peripherally restricted (PR) cannabinoid-1 receptor blocker with an IC50 value of 2 nM for CB1 receptor and > 1000 nM for CB2 receptor.