CB1 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).

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.

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

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.

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.

Zevaquenabant ((S)-MRI-1867) is a peripherally restricted, orally bioavailable dual cannabinoid CB1 receptor and inducible NOS antagonist. Zevaquenabant ameliorates obesity-induced chronic kidney disease (CKD).

URB447 is a peripherally restricted CB₁ cannabinoid antagonist (IC₅₀: 313 nM and 41 nM for rat CB1 and human CB2 receptor respectively ). URB447 lowers food intake and body-weight gain in mice without entering the brain or antagonizing central CB₁-dependent responses. URB447 can be used for research of obesity.

BPRCB1184 is a peripherally restricted 1-type cannabinoid receptor (CB1) antagonist, whose activity is associated with the regulation of obesity-related endocannabinoid system. BPRCB1184 regulates the activity of the endocannabinoid system, promotes lipid mobilization, reduces triglyceride storage, improves glucose metabolism, decreases food intake and body weight, while enhances insulin resistance and improves blood lipid levels. BPRCB1184 can be used in obesity-related research.

MJ15 is a potent and selective CB1 receptor antagonist with a K_i of 27.2 pM and an IC₅₀ of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice.

PSNCBAM-1 is a selective CB1 receptor allosteric antagonist with an EC₅₀ of 0.1 μM. PSNCBAM-1 can be used in the researches of obesity.

(R)-SLV 319 is a potent and selective cannabinoid receptor 1 (CB1) antagonist with a K_i value of 894 nM. (R)-SLV 319 is a dextrorotatory counterpart of SLV 319

LY320135 is a potent and selective antagonist of CB1 receptor, with a K_i of 141 nM. LY320135 also binds to 5-HT₂ and muscarinic receptors with K_is of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect.

O-2050 is a high affinity cannabinoid CB₁ receptor antagonist with a K_i of 2.5 nM. O-2050 inhibits cannabinoid CB₂ receptor (K_i=0.2 nM). O-2050 can cause locomotor stimulation in mice.

CB1 antagonist 6 (Compound 11jE2) is an orally active CB1R antagonist, with an IC₅₀ value of 23 nM. CB1 antagonist 6 significantly reduces food intake and body weight, improves glucose tolerance and insulin resistance, and decreases serum ALT and AST levels in diet-induced obese (DIO) mice, demonstrating hepatoprotective effects. CB1 antagonist 6 can be used for the study of metabolic syndrome (obesity, diabetes).

Amauromine is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist with K_i and K_b values of 178 nM and 66.6 nM, respectively.

BNS808 is an orally active and selective cannabinoid-1 receptor (CB₁R) antagonist (IC₅₀ = 0.8 nM) with notable CB₂R selectivity and minimal brain penetration. BNS808 is studied in research on obesity and its associated metabolic complications, such as metabolic dysfunctional-associated steatotic liver disease (MASLD). BNS808 has reduced free drug availability for CNS entry, enhancing safety and minimizing drug-drug interactions through high plasma binding.

rel-O-2050 (Compound O-2050) is a neutral cannabinoid CB₁ receptor antagonist. rel-O-2050 also decreases food intake in mice.

AZD-2207 is a cannabinoid receptor CB1 antagonist, known for its high lipophilicity. AZD-2207 has good intestinal permeability in the Caco-2 model and can be used in research related to type 2 diabetes and obesity.