Synthesis and biological evaluation of 3-alkyl-dihydrotetrabenazine derivatives as vesicular monoamine transporter-2 (VMAT2) ligands was written by Zheng, Pinguan;Lieberman, Brian P.;Choi, Seok Rye;Ploeessl, Karl;Kung, Hank F.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2011.Reference of 2328-12-3 This article mentions the following:
In the search of new probes for in vivo brain imaging of vesicular monoamine transporter type 2 (VMAT2), an efficient synthesis of a novel series of 3-alkyldihydrotetrabenazine (DTBZ) derivatives was developed. The affinity of VMAT2 was evaluated by an in vitro inhibitory binding assay using [125I]-iodovinyl-TBZ or [18F](+)-FP-DTBZ as radioligands in rat striatal tissue homogenates. New DTBZ derivatives exhibited moderate to good binding affinity to VMAT2. Among these new ligands, 9,10-dimethoxy-3-(2-methylallyl)-2,3,4,6,7,11b-hexahydro-1H-pyrido[2,1-a]isoquinolin-2-ol showed the best affinity for VMAT2 (K i = 5.98 nM) and may be a useful lead compound for future structure-activity studies. In the experiment, the researchers used many compounds, for example, 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride (cas: 2328-12-3Reference of 2328-12-3).
6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride (cas: 2328-12-3) belongs to tetrahydroisoquinoline derivatives. The tetrahydroisoquinoline skeleton is encountered in a number of bioactive compounds and drugs. Arene/Ru/TsDPEN complexes bearing a heterocyclic group catalyze the asymmetric transfer hydrogenation (ATH) of 1-aryl dihydroisoquinolines (DHIQs) to provide tetrahydroisoquinolines of high enantiomeric excess.Reference of 2328-12-3
Referemce:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem