cb1-in-1

CB1-IN-1 (DBPR211) is a peripherally restricted CB1R antagonist, for CB1R and CB2R with Ki of 0.3 nM and 21 nM,respectively.

SmCB1-IN-1 (Compound 2h) is an inhibitor of the Schistosoma mansoni cathepsin B1 (SmCB1) with a Ki of 0.05 μM. It demonstrates selectivity towards non-target human proteases, showing inhibition rates of 29% for CatB and 37% for CatL at 20 μM. At 1 μM, SmCB1-IN-1 inhibits 68% of Schistosoma mansoni.

ABCB1-IN-1 (compound 3) is a potent ABCB1 inhibitor that promotes cell apoptosis, featuring 1-benzylimidazole and exhibiting IC50 values of 1.26 μM for Colo205 cells and 2.21 μM for Colo320 cells, respectively [1].

PSNCBAM-1 (PSNCBAM 1) is a CB1 receptor negative allosteric modulator (EC50 = 0.1 μM) with hypophagic effects in vivo. PSNCBAM-1 can be used for obesity studies.

Rimonabant (SR141716) is an inverse agonist for the cannabinoid receptor CB1. It is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. Its main avenue of effect is a reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States.

Arvanil (N-Vanillylarachidonamide) is a synthetic capsaicin-amphetamine hybrid and a ligand for vanilloid receptor 1 (VR1) and cannabinoid receptor 1 (CB1), exhibiting neuroprotective activity, inhibiting spasm, and enhancing cisplatin chemotherapy sensitivity by inducing ferroptosis in HCC cells in vivo. It induces ferroptosis in liver cancer cells via binding to MICU1.

COR659 is a GABAB positive allosteric modulator (PAM) . COR659 suppresses alcohol and chocolate self-administration in rats[1]. COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABAB receptor and an action at the cannabinoid CB1 receptor[3]. COR659 (0, 2.5, 5 and 10 mg/kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats[1].COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats[2]. Animal Model: Male sP and Wistar rats[1]. [1]. Paola Maccioni, et al. Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABA B and cannabinoid CB 1 receptors. Psychopharmacology (Berl). 2017 Sep;234(17):2525-2543. [2]. Francesca Ferlenghi, et al. The GABA B receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives. Eur J Pharm Sci. 2020 Dec 1;155:105544. [3]. Paola Maccioni, et al. Anti-addictive properties of COR659 - Additional pharmacological evidence and comparison with a series of novel analogues. Alcohol. 2019 Mar;75:55-66.

AM9405 is a novel peripherally active cannabinoid type 1 (CB1) and serotonin type 3 receptor agonist. It inhibits twitch contraction of the ileum and colon with IC50 values of 45.71 nM and 0.076 nM, respectively. AM9405 significantly slowed mouse intestinal motility under physiological conditions and reversed hypermotility, reducing pain in mouse models that mimic symptoms of functional GI disorders, such as stress-induced diarrhea and writhing test.

CB1 antagonist 1 is a CB1 receptor antagonist, used in the research of obesity and metabolic syndrome, neuroinflammatory disorders, cognitive disorders, and gastrointestinal disorders, psychosis, and cardiovascular.

Leelamine hydrochloride, a tricyclic diterpene extracted from pine tree bark, inhibits the transcriptional activity of the androgen receptor, known to regulate fatty acid synthesis [2,3]. This compound acts as a cannabinoid receptor type 1 (CB1) agonist and suppresses SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells, irrespective of androgen receptor status.

Taranabant (MK-0364) is a selective and potent cannabinoid 1 (CB1) receptor inverse agonist used in the study of obesity and nicotine dependence.

CB1 antagonist 2 (AM4113) is caimabinoid 1 (CB1) antagonist which inhibits CB1 in vivo with an IC50 of 25.5 nM.

Parecoxib sodium is a prodrug of Valdecoxib and a selective, orally active COX-2 inhibitor that suppresses prostaglandin (PG) synthesis and alleviates pain and inflammation. Parecoxib sodium also acts as a cannabinoid 1 (CB1) receptor agonist (EC50=2.4 µM).

CB1/2 receptor-1 (compound 5.3) serves as an agonist for CB1/2 receptors and is utilized in angiogenesis research.

Delta8-THC acetate (Delta8-tetrahydrocannabinol) is a psychoactive cannabinoid that binds to the cannabinoid receptor 1 (CB1 receptor) and exhibits anti-nausea, appetite-stimulating, and anti-inflammatory effects. It may also offer neuroprotective benefits and has potential applications in research on anxiety and depression.

VIP36 is an agonist of the cannabinoid type 1 receptor (CB1) with analgesic properties. It reduces the recruitment of inhibitory proteins, thereby exerting its pain-relieving effects, and is applicable in research related to chronic pain.

CB1-IN-3 (Compound 6i) is a potent inhibitor of the cannabinoid receptor type 1 (CB1). It holds potential for research in obesity, inflammation, and neurological disorders.

UVI3502 is a cannabinoid receptor 1 (CB1) antagonist with an IC50 value of 4641 nM for CB1 and approximately 16200 nM for CB2. It can inhibit Gi/o protein coupling induced by the agonist CP55,940. UVI3502 shows potential for research into diseases related to the endocannabinoid system in the central nervous system, such as cognitive impairments and neurodegenerative disorders.

AM11542 acts as an orthosteric agonist of the cannabinoid receptor 1 (CB1), exhibiting a binding affinity with a Ki of 0.11 nM. It is useful in the investigation of CB1 receptor activation and its associated allosteric modulation mechanisms.

BI-5756 is a compound that acts as a CETP inhibitor and cannabinoid receptor 1 (CB1) agonist. It significantly raises HDL-C levels while reducing LDL-C levels. BI-5756 also enhances the function of regulatory T cells and maintains T cell-mediated anti-tumor activity. Additionally, it directly inhibits tumor cell growth and increases the expression of MHC I, MHC II, and CD80 on tumor cells. In models of graft-versus-host disease, BI-5756 offers protective effects. This compound is applicable for research in the areas of tumors, graft-versus-host disease, and metabolic disorders.

LH-21 is a potent in vivo neutral cannabinoid CB1 receptor antagonist that reduces food intake and body weight gain in obese Zucker rats, resulting in a dose-dependent inhibition of feeding [1].

Ibipinabant (SLV319) is a potent, selective, and orally active cannabinoid CB1 receptor antagonist, with a K_i of 7.8 nM and over 1000-fold selectivity for CB1 compared to CB2 (K_i = 7943 nM). It is utilized in obesity and diabetes research [1] [2] [3].

AM6545 is a selective and potent peripheral restricted cannabinoid receptor 1 (CB1) antagonist that inhibits the CB2 receptor, ameliorates hypometabolic obesity and improves adipokine secretion in monosodium glutamate-induced obese mice, and may be useful in the study of obesity and diabetes.

O-2050 is a high-affinity cannabinoid CB1 receptor antagonist with a Ki of 2.5 nM and inhibits the cannabinoid CB2 receptor with a Ki of 0.2 nM. O-2050 decreased food intake and stimulated locomotion in mice [1].