CB2 Antagonist

SR144528 is a potent and selective CB2 receptor antagonist with a K_i of 0.6 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.

PGN36 is a selective cannabinoid CB2 receptor (CB2R) antagonist with K_is of 0.09 µM and >40 µM for CB2R and CB1R, respectively. PGN36 abolishes the increase in collagen type I gene expression by the inducer of bone activity. PGN36 is able to cross the blood-brain barrier. PGN36 can be used for the study of frontotemporal dementia (FTD).

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.

CB2R antagonist 3 is a selective antagonist of cannabinoid type 2 receptor (CB2R). CB2R antagonist 3 has high affinity for human CB2R and specific selectivity for CB1R. CB2R antagonist 3 can be combined with CB65 (HY-110047), the activator of CB2R. CB2R antagonist 3 effectively up-regulates the expression of anti-inflammatory cytokines and down-regulates the expression of pro-inflammatory cytokines.

AChE/BChE-IN-18 (Compound 4g) is a dual inhibitor of AChE/BChE , with a IC₅₀ value of 0.315 μM for AchE. AChE/BChE-IN-18 is also a CB2R antagonist with a K_i value of 31 nM. AChE/BChE-IN-18 has neuroprotective activity.

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.

UVI3502 is a cannabinoid receptor 1 (CB1) antagonist with an IC₅₀ value of 4641 nM for CB1 and approximately 16200 nM for CB2. UVI3502 blocks G_i/o protein coupling induced by the agonist CP55,940. UVI3502 is promising for research of endocannabinoid system-related diseases in the central nervous system (such as cognitive impairment and neurodegenerative diseases).

CB2R antagonist 4 is a selective CB2R antagonist/inverse agonist with a pK_i of 6.54. CB2R antagonist 4 shows a ≥11-fold selectivity towards CB2R over CB1R and can be utilized in neurological research.