anandamide cellular uptake

OMDM-6 是 TRPV1(EC50 = 75 nM) 和 CB1 (Ki = 3.2 μM) 的双重激动剂。 OMDM-6 抑制 anandamide 细胞摄取，Ki 为 7.0 μM。

OMDM-5 是有效的、选择性的anandamide 细胞摄取抑制剂，Ki 为 4.8 μM。它是VR1 (TRPV1)激动剂，EC50为 75 nM，显示出对大麻素 1 型受体 (CB1) 的弱配体活性 (Ki=4.9 μM)。

OMDM-1 ((Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide) 是有效选择性的代谢稳定 anandamide 细胞摄取抑制剂，Ki=为2.4 μM。

OMDM-2 is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor(Ki of 3.0 μM).

OMDM-3 is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor(Ki of 16.6 μM).

OMDM-4 is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor(Ki of 17.7 μM).

Anandamide (AEA), an endogenous cannabinoid, interacts with both central (CB1) and peripheral (CB2) cannabinoid receptors. Its effects are concluded through the cellular uptake and enzymatic breakdown of its amide bond by fatty acid amide hydrolase. Arachidonoyl-N-methyl amide, an analog of anandamide, specifically targets the human CB1 receptor, displaying a binding affinity with a Ki of 60 nM. It completely inhibits rat glial gap junction intercellular communication at a concentration of 50 µM.