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CB1R Allosteric modulator 3

Names

[ CAS No. ]:
2633686-36-7

[ Name ]:
CB1R Allosteric modulator 3

Biological Activity

[Description]:

CB1R Allosteric modulator 3, a novel analogs derived from the 2-phenylindole scaffold, 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[1].

[Related Catalog]:

Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> Cannabinoid Receptor

[Target]

CB1


[In Vitro]

CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC50 values of 0.018 μM and 1.241 μM. CB1R Allosteric modulator 3 can enhance CB1R ago-PAM activity because of small lipophilic functional groups on the ortho-position of the GAT211 site-III phenyl ring[1].

[References]

[1]. Peter C Schaffer, et al. Focused structure-activity relationship profiling around the 2-phenylindole scaffold of a cannabinoid type-1 receptor agonist-positive allosteric modulator: site-III aromatic-ring congeners with enhanced activity and solubility. Bioorg Med Chem. 2020 Nov 1;28(21):115727.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H17ClN2O2

[ Molecular Weight ]:
376.84

Related Compounds