Cannabinoid Receptor Antagonist

AM251 is a selective cannabinoid 1 (CB1) receptor antagonist with an IC₅₀ of 8 nM. AM251 also acts as a potent GPR55 agonist with an EC₅₀ of 39 nM.

Monlunabant ((S)-MRI-1891) is an orally active antagonist for cannabinoid receptor 1 (CB1), binds to hCB1 and hCB2 with K_i of 0.3 nM and 613 nM.

S-Methoprene is an insect juvenile hormone analog and effective insecticide that blocks the transition from pupa to adult. S-Methoprene is also a CB(1) receptor ligand and inhibits the binding of the CB1 receptor antagonist [³H]CP-55940 to the CB1 receptor (IC₅₀: 19.31 μM).

(R)-JD-5037 (compound 4a) is the R- isomer of JD-5037 (HY-18697). (R)-JD-5037 is a CBiR antagonist with an IC₅₀ of ＞1 μM.

Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with K_i of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.

CB1 antagonist 2 (AM4113) is an orally active cannabinoid receptor type 1 (CB1R) antagonist. CB1 antagonist 2 suppresses appetite, reduces body weight, and blocks addictive behaviors such as heroin addiction, without causing adverse effects like nausea and depression that are associated with traditional CB1 inverse agonists. CB1 antagonist 2 can be used in studies related to obesity and opioid addiction.

NESS 0327 is a cannabinoid antagonist with high selectivity for the cannabinoid CB1 receptor. NESS 0327 is more than 60,000-fold selective for the CB1 receptor.

O1918 is a selective non-CB₁ receptor and GPR18 antagonist.

AM6545 is a highly selective, brain-free (peripherally active) CB1 receptor antagonist (K_i=1.7 nM). AM6545 inhibits endocannabinoid signaling by competitively antagonizing CB1 receptors, inhibiting CB1-mediated appetite stimulation and inflammatory responses without affecting cAMP levels. AM6545 significantly reduces food intake and body weight in mice, while improving metabolic syndrome-related renal impairment (such as proteinuria, fibrosis) and insulin resistance. AM6545 can be used in the study of obesity and its complications.

(±)-Ibipinabant ((±)-SLV319) is the racemate of SLV319. (±)-Ibipinabant ((±)-SLV319) is a potent and selective cannabinoid-1 (CB-1) receptor antagonist with an IC₅₀ of 22 nM.

AM6538 is a long-acting, high affinity and pseudo-irreversible cannabinoid (CB) antagonist. AM6538 is a structural analog of rimonabant. AM6538 can be effectively used to evaluate the apparent efficacy of cannabinoid full and partial agonists. AM6538 may be useful in future studies that require temporary reductions in cannabinoid receptor availability. AM-6538 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models.

Voacamine is an indole alkaloid with cannabinoid 1 (CB1) antagonistic activity. Voacamine can inhibit nuclear translocation. Voacamine is effective in enhancing the effect of Doxorubicin (HY-15142A) as it interferes with the P-glycoprotein (P-gp) function. Voacamine promotes apoptosis-independent autophagic cell death in human osteosarcoma cells. Voacamine activates mitochondrial-associated apoptosis signaling pathway and inhibition of PI3K/Akt/mTOR signaling pathway to suppress breast cancer progression. Voacamine inhibits EGFR to exert oncogenic activity against colorectal cancer.

Taranabant racemate (MK-0364 racemate) is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor extracted from patent WO 2004048317 A1.

Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models.

Rimonabant-d₁₀ is deuterium labeled Rimonabant. Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

LH-21 is a potent in vivo neutral cannabinoid CB1 receptor antagonist. LH-21 reduces food intake and body weight gain in obese Zucker rats. , and displays efficacy as a feeding inhibitor.

(Rac)-Zevaquenabant ((Rac)-MRI-1867, compound 6b) is a cannabinoid receptor type 1 (CB₁R)/iNOS antagonist, with a K_i of 5.7 nM for CB₁R. (Rac)-Zevaquenabant is potential for the research of liver fibrosis.

Surinabant (SR 147778) is an orally active, selective cannabinoid receptor type 1 CB1R antagonist. Surinabant is used in studies of obesity and alcoholism.

Rosonabant is a selective antagonist for cannabinoid receptor (CB1 receptor), which reduces body weight and improves improves the risk of obesity-related cardiovascular metabolic diseases. Rosonabant exhibits adverse side effect, such as nausea and mental disorder.