Zak, Agnieszka; Lemaire, Lucas; Chalon, Sylvie; Chicheri, Gabrielle; Marzag, Hamid; Bodard, Sylvie; Serriere, Sophie; Routier, Sylvain; Buron, Frederic; Vercouillie, Johnny published an article in 2021. The article was titled 《[18F]-labeled positron emission tomography ligand for the histamine H4 receptor》, and you may find the article in Journal of Labelled Compounds and Radiopharmaceuticals.Recommanded Product: 109-01-3 The information in the text is summarized as follows:
We synthesized 5-[18F]-fluoro-1H-indol-2-yl)(4-methyl-1-piperazinyl)methanone ([18F]5) via a Suzuki approach starting from a protected pinacol borane precursor followed by acidic hydrolysis of the t-Boc protecting group. The non-optimized radiochem. yield was 5.7 ± 1.35%, radiochem. purity was over 99%, and molar activity was 100.7 ± 34.5 GBq/μmol (n = 3). [18F]5 was stable in rat plasma for at least 4 h and was evaluated by μPET imaging and biodistribution using a unilateral quinolinic acid rat model of neuroinflammation. The time-activity curve showed that [18F]5 entered the brain immediately after i.v. injection and then left it progressively with a very low level reached from 30 min after injection. The biodistribution study showed no difference in the accumulation of [18F]5 between the lesioned and intact side of the brain and between control rats and animals pretreated with a saturating dose of JNJ-7777120 as a specific H4R antagonist. Hence, despite its in vitro nanomolar affinity for H4R, and its ability to cross the blood-brain barrier in rats, [18F]5 does not appear suitable to image in vivo the receptor by PET. The results came from multiple reactions, including the reaction of 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 109-01-3)
1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Recommanded Product: 109-01-3
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics