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Thienopyrimidine Derivatives as GPR55 Receptor Antagonists: Insight into Structure–Activity Relationship
Figuerola-Asencio, Laura Morales, Paula Zhao, Pingwei Hurst, Dow P. Sayed, Sommayah S. Colón, Katsuya L. Gómez-Cañas, María Fernández-Ruiz, Javier Croatt, Mitchell P. Reggio, Patricia H.
Figuerola-Asencio, Laura
Morales, Paula
Zhao, Pingwei
Hurst, Dow P.
Sayed, Sommayah S.
Colón, Katsuya L.
Gómez-Cañas, María
Fernández-Ruiz, Javier
Croatt, Mitchell P.
Reggio, Patricia H.
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2022-12-02
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http://dx.doi.org/10.1021/acsmedchemlett.2c00325
Abstract
GPR55 is an orphan G-protein coupled receptor involved in various pathophysiological conditions. However, there are only a few noncannabinoid GPR55 ligands reported so far. The lack of potent and selective GPR55 ligands precludes a deep exploration of this receptor. The studies presented here focused on a thienopyrimidine scaffold based on the GPR55 antagonist ML192, previously discovered by high-throughput screening. The GPR55 activities of the new synthesized compounds were assessed using β-arrestin recruitment assays in Chinese hamster ovary cells overexpressing human GPR55. Some derivatives were identified as GPR55 antagonists with functional efficacy and selectivity versus CB1 and CB2 cannabinoid receptors.
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ACS Medicinal Chemistry Letters, Vol. 14
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