cannabinoidreceptor

CB1 inverse agonist 1 (MRL-650) is an orally active and selective CB1 agonist. The IC50s for CB1 and CB2 are 7.5 nM and 4100 nM, respectively. CB1 inverse agonist 1 shows anorexigenic effects.

CB2 modulator 1 is a potent CB2 modulator. It can be used for the research for immune disorders, osteoporosis, inflammation, renal ischemia.

OMDM-6 is a dual agonist of TRPV1(EC50 = 75 nM) and CB1 (Ki = 3.2 μM). OMDM-6 inhibits anandamide cellular uptake with a Ki of 7.0 μM.

Drinabant (AVE-1625) is an orally active CB1 receptor antagonist. Drinabant 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.

CB2 receptor agonist 2 (ZINC72105556) is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor, Ki = 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2.

AM-1235 is a potent and selective cannabinoid receptor CB1 agonist.

GW 833972A is a selective CB2 receptor agonist that inhibits induced neural depolarization and citric acid-induced cough in an animal model.

Pregnenolone (Arthenolone) is an endogenous steroid hormone synthesized from cholesterol, used in the treatment of Alzheimer's disease.

Rimonabant hydrochloride (SR 141716A) is a cannabinoid receptor antagonist, binding selectively to central cannabinoid receptors (CB1) with high affinity.

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.

β-Caryophyllene ((-)-(E)-Caryophyllene) acts as an CB2 receptor agonist.

Pregnenolone acetate is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. It acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. It can protect the brain from cannabis intoxication

EHP-101 (VCE-004.8) is a specific dual agonist of PPARγ and CB2 receptor with potent anti-inflammatory activity. EHP-101 attenuates adipogenesis and prevents diet-induced obesity.

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.

Bay 59-3074 is a CB1/CB2 receptor partial agonist (Ki: 48.3/45.5 nM). In rat models of chronic neuropathic and inflammatory pain, it displays anti-hyperalgesic and antiallodynic properties.

CB1R Allosteric modulator 3 is a potent CB1R modulator that inhibits cAMP and β-Arrestin and can be used for the study of obesity and nicotine addiction.

CB2R/FAAH modulator-1, a cannabinoid type 2 receptor (CB2R) agonist, is also a fatty acid amide hydrolase (FAAH) inhibitor (IC50=4 μM) that reduces the production of pro-inflammatory and anti-inflammatory cytokines and is commonly used in inflammation studies. The Kis for CB2R and CB1R are 14.8 nM and 241.3 nM, respectively.

A-836339 acts as a potent cannabinoid receptor full agonist which has a higher affinity for the peripheral CB2 receptor (Ki = 0.64 nM) over the central CB1 receptor (Ki = 270 nM). It displays analgesic, anti-inflammatory, and anti-hyperalgesic effects in

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.

OMDM-5 is a selective anandamide cellular uptake (ACU)inhibitor(Ki of 4.8 μM).

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

Taranabant racemate is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor.

N-Oleoyl Glycine, a Lipoamino Acid, Stimulates Adipogenesis Associated With Activation of CB1 Receptor and Akt Signaling Pathway in 3T3-L1 Adipocyte

In the central nervous system, 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand