《Synthesis of a carbon-11 radiolabeled BACE1 inhibitor》 was published in Medicinal Chemistry Research in 2020. These research results belong to Zhu, Yiwei; Fiedler, Stephanie A.; Hibert, Matthew L.; Wang, Changning. Reference of 3-Methoxyphenylboronic acid The article mentions the following:
Beta-secretase (BACE1), a transmembrane aspartyl protease, can cleave membrane-bound β-amyloid precursor proteins (APPs) to initiate the accumulation of amyloid-β (Aβ). The inhibition of BACE-1 to limit the accumulation of neurotoxic Aβ peptides could offer a potential treatment for Alzheimer’s Disease (AD). However, little is known about the distribution and d. of BACE1 in the central nervous system. As a step toward filling this gap in knowledge, we have evaluated a potential radiotracer for the imaging of BACE1 using positron emission tomog. (PET). A BACE1 inhibitor, 5, is reported with blood-brain barrier (BBB) permeability and high binding affinity. To characterize the pharmacokinetics and distribution of 5 in the brain, we radiolabeled 5 with carbon-11. Using PET, we found that [11C]5 shows moderate uptake in the brain when administered i.v. to rodents and further work will be performed in animal models to test its application as a PET imaging probe for the central nervous system. Our study demonstrates the effectiveness of PET at providing brain pharmacokinetic data for BACE1 inhibitors, crucial for the development of treatments for AD where CNS penetration is critical3-Methoxyphenylboronic acid(cas: 10365-98-7Reference of 3-Methoxyphenylboronic acid) was used in this study.
3-Methoxyphenylboronic acid(cas: 10365-98-7) belongs to boronic acids. Boronic acids are mild Lewis acids which are generally stable and easy to handle, making them important to organic synthesis.Reference of 3-Methoxyphenylboronic acid
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