JZP-MA-11

JZP-MA-11 is a positron emission tomography (PET) ligand targeting the endocannabinoid α/β-hydrolase domain 6 (ABHD6) enzyme. JZP-MA-11 selectively inhibits ABHD6 with an IC50 value of 126 nM. JZP-MA-11 can cross the blood-brain barrier (BBB). [18F]JZP-MA-11 has the potential for preclinical evaluation targeting the brain ABHD6 in mice and nonhuman primate (NHP)[1].

Signaling Pathways >> Metabolic Enzyme/Protease >> MAGL

Research Areas >> Neurological Disease

JZP-MA-11 (10 μM) 对表达 CB1 或 CB2 的 HEK293 细胞中 毛喉素 (HY-15371) 刺激的 cAMP 没有影响[1]。

JZP-MA-11 (1.5 mg/kg; 静脉给药; 示踪剂注射前 20 分钟) 导致大脑、肝脏、心脏和肾脏等富含 ABHD6 的器官的放射性摄取减少[1]。 Animal Model: C57BL6 mice (female, 10-12-week-old)[1] Dosage: 1.5 mg/kg Administration: IV; 20 min before tracer injection Result: Resulted in a decrease in radioactivity uptake in ABHD6-rich organs such as, brain, liver, heart, and kidneys.

[1]. Karine Mardon, et al.Utilizing PET and MALDI Imaging for Discovery of a Targeted Probe for Brain Endocannabinoid α/ β-Hydrolase Domain 6 (ABHD6). J Med Chem. 2022 Dec 14.