Drug intelligence / Profile preview

HU-910

Development stage
Preclinical
Lead developer
Hebrew University of Jerusalem
Modality
Small Molecules
Administration
Intraperitoneal, Oral (preclinical, Based On Solubility And Bioavailability Studies)
01

Overview

HU-910 is a **synthetic cannabinoid** and a potent and selective agonist of the **cannabinoid CB2 receptor**. Its chemical structure features a unique bicyclic moiety incorporated into the non-aromatic region of the molecule[2][1]. HU-910 binds to the CB2 receptor with high affinity (Ki for human CB2 ≈ 6 nM) and demonstrates much lower affinity for the CB1 receptor (Ki ≈ 1.4 μM)[1]. Its selectivity results in functional activity at CB2 (EC50 for cAMP inhibition ≈ 162 nM; EC50 for GTPγS binding ≈ 26.4 nM)[1]. Mechanistically, HU-910 activates CB2 receptors, leading to **immunosuppressive and anti-inflammatory effects**. It reduces pro-inflammatory cytokines (TNF-α, IL-6, IL-1β), chemokines (CCL3, CXCL2, CCL2), and adhesion molecules, attenuates neutrophil infiltration, and decreases oxidative stress and apoptosis[1][2][4]. These effects have been demonstrated in preclinical models of hepatic ischemia-reperfusion injury and in activated microglia and astrocytes[1][2][4][11]. HU-910 was developed in academic collaboration, including work by Raphael Mechoulam's group, for use primarily in research on inflammation and neuroinflammation, with no evidence of human clinical trials or marketing authorization as a pharmaceutical[6][1].

02

Targets

CNR1 (Cannabinoid receptor 1)

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