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].
in vivo
JZP-MA-11 (1.5 mg/kg; IV; 20 min before tracer injection) results in a decrease in radioactivity uptake in ABHD6-rich organs such as, brain, liver, heart, and kidneys[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.
References
[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. DOI:10.1021/acs.jmedchem.2c01485
