Cannabinoid Receptor Antagonist

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

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.

SR144528 is a potent and selective CB2 receptor antagonist with a K_i of 0.6 nM.

(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.

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.

Rimonabant Hydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an K_i of 1.8 nM. Rimonabant Hydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

JD-5037 is a potent CB₁R antagonist with an IC₅₀ of 1.5 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).

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.

AM281 is a selective CB1 receptor antagonist with an IC₅₀ of 9.91 nM. AM281 inhibits CB2 receptor with an IC₅₀ of 13000 nM.

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.

Ibipinabant (SLV319) is a potent, selective and orally active antagonist of cannabinoid CB1 receptor, with a K_i of 7.8 nM. Ibipinabant shows more than 1000-fold selectivity for CB1 over CB2 (K_i=7943 nM). Ibipinabant can be used for the research of obesity and diabetic.

CB1 antagonist 4 (compound 8) is a selective cannabinoid receptor 1 (CB1) inverse agonist with an IC₅₀ of 8.5 nM for human CB1. CB1 antagonist 4 shows selective for CB1 over CB2 receptors (IC₅₀ of 604.9 nM). CB1 antagonist 4 inhibits GTP binding to CB1-overexpressing cell membranes with an EC₅₀ of 18.5 nM.

PGN36 is a selective cannabinoid CB2 receptor (CB2R) antagonist with K_is of 0.09 µM and >40 µM for CB2R and CB1R, respectively. PGN36 abolishes the increase in collagen type I gene expression by the inducer of bone activity. PGN36 is able to cross the blood-brain barrier. PGN36 can be used for the study of frontotemporal dementia (FTD).

Drinabant (AVE1625) is an orally active CB1 receptor antagonist. Drinabant (AVE1625) inhibits the agonist-stimulated calcium signal with IC₅₀ values of 25 nM and 10 nM for the hCB1-R and rCB1-R, respectively, and is ineffective for the hCB2-R.