Characterization of Novel and Known Activators of Cannabinoid Receptor Subtype 2 Reveals Mixed Pharmacology That Differentiates Mycophenolate Mofetil and GW-842,166X from MDA7 DOI Open Access
Alice L. Rodriguez,

Aidong Qi,

Allie Han

и другие.

International Journal of Molecular Sciences, Год журнала: 2025, Номер 26(10), С. 4956 - 4956

Опубликована: Май 21, 2025

CB1 and CB2 cannabinoid receptors are members of the GPCR superfamily that modulate effects endocannabinoids. is most abundant CB receptor in central nervous system, while present both peripherally brain. plays a role inflammation, as well neurodegenerative psychiatric disorders. To identify new ligands for CB2, we screened library FDA-approved drugs activity at using thallium flux assay, resulting discovery immunosuppressant mycophenolate mofetil potent, selective activator CB2. Further characterization compound confirmed agonist variety complementary assays, including PI hydrolysis, cAMP inhibition, β-arrestin recruitment. Radioligand binding assays established non-competitive interaction with site occupied by [3H]CP55,940. agonists GW-842,166X MDA7 were also profiled, revealing exhibits similar profile to mofetil, whereas presents distinct profile. These differences provide insight into complex pharmacology impacting preclinical clinical studies, ultimately, treatment strategies brain

Язык: Английский

Characterization of Novel and Known Activators of Cannabinoid Receptor Subtype 2 Reveals Mixed Pharmacology That Differentiates Mycophenolate Mofetil and GW-842,166X from MDA7 DOI Open Access
Alice L. Rodriguez,

Aidong Qi,

Allie Han

и другие.

International Journal of Molecular Sciences, Год журнала: 2025, Номер 26(10), С. 4956 - 4956

Опубликована: Май 21, 2025

CB1 and CB2 cannabinoid receptors are members of the GPCR superfamily that modulate effects endocannabinoids. is most abundant CB receptor in central nervous system, while present both peripherally brain. plays a role inflammation, as well neurodegenerative psychiatric disorders. To identify new ligands for CB2, we screened library FDA-approved drugs activity at using thallium flux assay, resulting discovery immunosuppressant mycophenolate mofetil potent, selective activator CB2. Further characterization compound confirmed agonist variety complementary assays, including PI hydrolysis, cAMP inhibition, β-arrestin recruitment. Radioligand binding assays established non-competitive interaction with site occupied by [3H]CP55,940. agonists GW-842,166X MDA7 were also profiled, revealing exhibits similar profile to mofetil, whereas presents distinct profile. These differences provide insight into complex pharmacology impacting preclinical clinical studies, ultimately, treatment strategies brain

Язык: Английский

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