CB1/2 agonist 3

Names

[ Name ]:
CB1/2 agonist 3

Biological Activity

[Description]:

CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a CB1/CB2 (cannabinoid receptor) competitive agonist. CB1/2 agonist 3 acts on hCB1 and hCB2 with Ki values of 5.9 nM and 3.5 nM, respectively[1].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor

[Target]

hCB1-R:5.9 nM (Ki)

hCB2-R:3.5 nM (Ki)

[In Vitro]

CB1/2 agonist 3 (compound 52) can partially induce [35S]GTPγS binding to hCB1-CHO cell membranes with an EC50 value of 30.99 nM, and slightly inhibit [35S]GTPγS binding to hCB2-CHO cell membranes with a mean EC50 value of 1.28 nM[1]. CB1/2 agonist 3 (compound 52) ((1 μM, 1 h) has antagonistic effect on CB1/CB2 agonist CP-55940 with a Kb value of 78.17 nM[1].

[References]

[1]. Antonella Brizzi, et al. Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity. Bioorg Med Chem. 2020 Jun 1;28(11):115513.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₄₁NO₂

[ Molecular Weight ]:
387.60

Related Compounds

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