CB1 Modulator

Dodec-2E-ene-8,10-diynoic acid isobutylamide is an alkamide found in Echinacea angustifolia that binds to CB₁ (rat K_i = 61.1 μM) and CB₂ (mouse K_i = 47.2 μM) cannabinoid receptors. Dodec-2E-ene-8,10-diynoic acid isobutylamide can be used in research on inflammatory diseases.

RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB₁) receptor with a pIC₅₀ of 7.54 in Ca²⁺ mobilization assay. RTICBM-189 has pIC₅₀s of 5.29 and 6.25 for hCB₁ and mCB₁, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the addictive agent-seeking behavior in rats.

CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment.

CB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC₅₀ values of 0.018 μM and 1.241 μM, respectively.

PSB-SB-1203 (Compound 25b) is a dual CB1/CB2 ligand that blocks CB1 but activates CB2 receptors (CB1 K_i 0.244 μM; CB2 K_i 0.210 μM, EC₅₀ 0.054 μM). PSB-SB-1203 is promising for research of obesity and cancers.

RTICBM-74 is a blood-brain barrier-permeable, selective CB1 allosteric modulator with IC₅₀ values of 23 nM (calcium mobilization assay) and 153 nM ([³⁵S]GTPγS assay). RTICBM-74 inhibits CB1 receptor signaling. RTICBM-74 reduces alcohol intake in rats. RTICBM-74 can be used for the research of alcohol use disorder.

CB1R Allosteric modulator 2 (compound 18) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 2 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.

CB1R Allosteric modulator 1 (compound 11) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 1 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.