Deng, Hongfeng published the artcilePotent Cannabinergic Indole Analogues as Radioiodinatable Brain Imaging Agents for the CB1 Cannabinoid Receptor, Application In Synthesis of 27483-92-7, the main research area is indole iodobenzoyl piperidinylmethyl radioiodinated preparation CB1 cannabinoid receptor agonist; iodine labeled indole brain imaging agent.
A series of novel aminoalkylindoles was synthesized in an effort to develop compounds that are potent agonists at the CB1 cannabinoid receptor and that are also easily labeled with radioisotopes of iodine for biochem. and imaging studies. 2-Iodophenyl-[1-(1-methylpiperidin-2-ylmethyl)-1H-indol-3-yl]methanone I (AM2233) had a very high affinity for the rat CB1 receptor, with most of the affinity residing with the (R)-enantiomer. Radioiodinated racemic I and its enantiomers were prepared by radioiododestannylation of the tributyltin analogs in high yields, radiochem. purities, and specific radioactivities. In a mouse hippocampal membrane preparation with [131I](R)-I as radioligand, racemic I exhibited a Ki value of 0.2 nM compared with 1.6 nM for WIN55212-2. In autoradiog. experiments with mouse brain sections, the distribution of radioiodinated I was consistent with that of brain CB1 receptors. Again, very little specific binding was seen with the (S)-enantiomer [131I](S)-I and none occurred with the (R)-enantiomer [131I](R)-I in sections from CB1 receptor knockout mice. Radioiodinated I thus appears to be a suitable radioligand for studies of CB1 cannabinoid receptors.
Journal of Medicinal Chemistry published new progress about Labeled chemical compounds Role: DGN (Diagnostic Use), PAC (Pharmacological Activity), SPN (Synthetic Preparation), BIOL (Biological Study), USES (Uses), PREP (Preparation). 27483-92-7 belongs to class piperidines, name is 2-(Chloromethyl)-1-methylpiperidine hydrochloride, and the molecular formula is C7H15Cl2N, Application In Synthesis of 27483-92-7.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem