HU-308 ([(1R,2R,5R)-2-[2,6-dimethoxy-4-(2-methyloctan-2-yl)phenyl]-7,7-dimethyl-4-bicyclo[3.1.1]hept-3-enyl]methanol) is a potent, selective agonist for the CB2 receptor. The synthesis and characterization took place in the laboratory of Prof. Mechoulam at the Hebrew University of Jerusalem in the late 1990s. It has analgesic effects, promotes proliferation of neural stem cells,[3] and protects both liver and blood vessel tissues against oxidative stress via inhibition of TNF-α. In vivo, HU-308 has hypotensive, analgesic, and anti-inflammatory activities in mice that can be reversed by the CB2 receptor antagonist SR 144528 but not the CB1 receptor antagonist rimonabant. Pretreatment of mice with HU-308 decreases the I/R-induced tissue damage, inflammatory cell infiltration, tissue, and serum TNF-α, MIP-1, and MIP-2 levels, tissue lipid peroxidation, and apoptosis. HU-308 increases proliferation of HT29 colon cancer cells and growth of tumors in an HT29 mouse xenograft model. The physiological and toxicological properties of this compound have not been evaluated in humans.

ORG-28611 (SCH-900,111) is a potent cannabinoid receptor full agonist, developed by Organon International for treatment pain. In preclinical studies, Org 28611 exhibited high affinity for both CB1 and CB2 cannabinoid receptors, as determined by radioligand competition binding assays and rapidly metabolized by mouse and human hepatic microsomes and showed higher total levels in the brain compared to plasma. In clinical trials, Org 28611 does not provide enough sedation for outpatient surgical procedures, does not induce anterograde amnesia and causes undesirable subjective effects at higher doses. However, bolus doses up to 3 μ/kg (with maximum initial plasma concentrations of 24 ng/mL) or mean plasma levels up to 4 ng/mL are well tolerated and make it worthwhile to further explore the analgesic or antiemetic properties.

JTE-907 is selective high-affinity cannabinoid CB2 receptor inverse agonist. JTE-907 showed a concentration-dependent increase of forskolin-stimulated cAMP production in CHO cells expressing human and mouse CB2 in vitro. In mice model of atopic dermatitis, JTE-907 suppresses spontaneous itch-associated responses of NC mice without adverse effects such as weight loss.