Original ArticlesSynthesis and evaluation of 6-[11C]Methoxy-3-[2- [1-(phenylmethyl)-4-piperidinyl]ethyl]-1,2-benzisoxazole as an in vivo radioligand for acetylcholinesterase

Add time:08/20/2019    Source:sciencedirect.com

ABSTRACT. 6-Methoxy-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-1,2-benzisoxazole is a high affinity (Ki = 8.2 nM) reversible inhibitor of acetylcholinesterase (AChE). The carbon-11 labeled form was prepared in high (>97%) radiochemical purity and with specific activities of 37 ± 20 GBq/μmol at end of synthesis, by the alkylation of the desmethyl precursor with [11C]methyl trifluoromethanesulfonate in N,N-dimethylformamide at room temperature. In vivo studies in mice demonstrated good blood brain permeability but essentially uniform regional brain distribution. Thus, despite in vitro and in vivo activity as an AChE inhibitor, 6-[11C]methoxy-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-1,2-benzisoxazole does not appear to be a good candidate for in vivo imaging studies of AChE in the mammalian brain.

We also recommend Trading Suppliers and Manufacturers of 5-Hydroxy-1-(phenylmethyl)-2,4-imidazolindion (cas 110668-56-9). Pls Click Website Link as below: cas 110668-56-9 suppliers

Prev:Synthesis and characterization of 1,1′-bis[1-(carboxymethyl)thioalkyl]ferrocenes and 1,1′-bis[1-(carboxymethyl)thio-1-phenylmethyl] ferrocene
Next:Research paperCombretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors)