cannabinoidreceptor

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.

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

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.

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

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.

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.

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.

(R)-Monlunabant ((R)-MRI-1891) is a CB1 receptor antagonist used in obesity and metabolic disease research [1].

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

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.

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.

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].

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

AM841, a high-affinity electrophilic ligand, covalently interacts with a cysteine residue in helix six, thus activating the CB1 cannabinoid receptor. It diminishes forskolin-stimulated cAMP accumulation and slows gastrointestinal motility [1] [2].

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.

CB-25 is a partial agonist ligand of CB1 cannabinoid receptors, augmenting Forskolin-induced cAMP formation in cancer cells, though not affecting hCB1-CHO cells [1].

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.

Compound 38-S is an orally active CB1R AMPK modulator with a K i of 0.81 nM and an IC50 of 3.9 nM for CB1R. This compound activates AMPK and has been shown to decrease food intake and body weight, in addition to enhancing glucose tolerance and insulin sensitivity [1].

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.

Monlunabant ((S)-MRI-1891), a solid dispersion compound, functions as an inhibitor of the cannabinoid CB1 receptor [1].

CB2 PET Radioligand 1 (compound [18F]9) is a positron emission tomography (PET) radioligand with high affinity for the human cannabinoid receptor 2 (hCB2, Ki=7.7 nM). It is synthesized via Cu-mediated 18F-fluorination and demonstrates significant brain uptake in a mouse model of neuroinflammation [1].

CB2R agonist 2 (cis-17-para) is a CB2R agonist [1].

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 agonist 3, a potent activator of cannabinoid receptor 2 (CB2R), exhibits an EC50 value of 0.37μM, indicative of its significant role in the immune system [1].