Home GPCR & G Protein Cannabinoid Receptor

Cannabinoid Receptor Antagonists

Cat.No. Product Name Information Product Use Citations Product Validations
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
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
Cellular Physiology and Biochemistry, 2016, 1521-1536
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
S8694 CID16020046 CID16020046 (C390-0219) is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor.
Pharmacol Res, 2024, 203:107176
Pharmacological Research, 2024, 107176
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.
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.