Cannabinoid Receptor

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.

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

2,3-Butanediol, derived from the bioconversion of natural resources, holds significant potential for various industries, including chemical, cosmetics, agriculture, and pharmaceutical sectors.

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

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.

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

O-1602 is a novel GPR55 agonist, an atypical cannabinoid associated with the central nervous system and obesity, and is a candidate compound for the treatment of cystitis.O-1602 promotes hepatic steatosis through GPR55 and PI3 kinase Akt SREBP-1c signalling in mice.O-1602 induces, in a GPR3-independent manner, in Hep55B cells with elevated intracellular calcium.

Voacamine (Voacanginine) is an indole alkaloid. Voacamine exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.Voacanginine may have rhythmic effects.

AZD1940 (UNII-0J0035E9FT) is a high affinity CB(1) CB(2) receptor agonist of the cannabinoid with oral activity. Application in the study of orofacial pain.

Amauromine is a peripherally selective and potent cannabinoid receptor type 1 (CB1) receptor antagonist, a novel alkaloid with vasodilatory activity.

Olivetol (5-n-Amylresorcinol) (5-pentylresorcinol, 5-pentyl-1,3-benzenediol) is an organic compound found in certain species of lichen; it is also a precursor in various syntheses of tetrahydrocannabinol. Olivetol has an antioxidant effect.

AM404 is an endocannabinoid reuptake inhibitor, a TRPV(1) activator, a paracetamol metabolite, with neuroprotective and anticancer activity that blocks anandamide transport. AM404 inhibits NFAT and NF-kappaB signaling pathways and impairs migration and invasiveness of neuroblastoma cells, preventing prostaglandin synthesis in activated microglia by inhibiting COX activity.

CB1 2 agonist 3 is a competitive and potent CB1 CB2 agonist with high affinity for hCB1 and hCB2 and can be used to study neurological disorders.

CB1R antagonist 1 is a potent CB1R antagonist that can be used to study diseases related to the nervous system.

N-Arachidonyldopamine (NADA) is a selective and potent endogenous CB1 receptor agonist (Ki: 250 nM).N-Arachidonyldopamine is also a potent and selective TRPV1 agonist with an EC50 value of ~50 nM.

CB1 agonist 1 is a potent CB1 agonist with a pIC50 value of 5.7 for CB1 receptors.CB1 agonist 1 can be used to study brain disorders, pain, and inflammation.

Virodhamine (O-arachidonoyl ethanolamine), an endocannabinoid, is an antagonist of CB1 receptor and an agonist of CB2 receptor. Virodhamine can be used for the research of neurological disorders such as Alzheimer's diseases.

CB2R FAAH modulator-2 (compound 26) is a dual modulator targeting CB2R and FAAH, acting as a CB2R agonist (Ki = 10.8 nM) and FAAH inhibitor (IC50 = 6.2 μM), with a Ki value of 152.9 nM for CB1R. It has research value in cancer, deleterious inflammatory cascades in neurodegenerative diseases, and COVID-19 infection.

CB2R FAAH modulator-3 (compound 27) is a modulator targeting CB2R and FAAH, acting as a CB2R agonist with a Ki value of 20.1 nM and a CB1R agonist with a Ki value of 67.6 nM, while inhibiting FAAH with an IC50 value of 3.4 μM. This compound has research value in cancer, neurodegenerative disease-related inflammatory cascades, and COVID-19 infection.

Hemopressin TFA, a nonapeptide originating from the α1-chain of hemoglobin and initially isolated from rat brain homogenates, is an orally active, selective inverse agonist of CB1 cannabinoid receptors that demonstrates antinociceptive effects in inflammatory pain models [1] [2].

GW 405833 (L-768242) is an agonist of cannabinoid-2 (CB(2)) receptor-selective