Synthesis and biodistribution of R- and S-isomers of [18F]-fluoropropranolol, a lipophilic ligand for the β-adrenergic receptor
- 作者：Tewson ; Timothy J. ; Stekhova ; Svetlana ; Kinsey ; Berma ; Chen ; Lay ; Wiens ; Linda ; Barber ; Roger
- 关键词：β ; -Adrenergic receptor ; Fluorine-18 ; Fluoropropranolol ; Stereoisomers
- 刊名：Nuclear Medicine and Biology
- 出版年：1999
- 期刊代码：43_09698051
- 类别：ph
- 出版时间：November, 1999
- 卷：26
- 期：8
- 页码：891-896
- 文件大小：282 K
摘要
The S and R isomers of [18F]-fluoropropranolol (1-[1-fluoro-2-isopropylamino]-3-naphthalen-1-yloxy-propan-2-ol) have been prepared by reductive alkylation of the appropriate aminoalcohols. The radiosynthesis provides a reasonable yield (
25%) to give products of 99%enantiomeric excess and specific activities of 1–3 Ci/μmol. The dissociation constants for the β2 adrenergic receptor are 0.5 and 2.5 nM for the S and the R isomers, respectively. The biodistribution data in rats show that uptake and egress of the tracer is rapid but that the result of blocking studies and the difference between the R and the S isomers suggest receptor-mediated uptake in receptor-rich tissue.
25%) to give products of 99%enantiomeric excess and specific activities of 1–3 Ci/μmol. The dissociation constants for the β2 adrenergic receptor are 0.5 and 2.5 nM for the S and the R isomers, respectively. The biodistribution data in rats show that uptake and egress of the tracer is rapid but that the result of blocking studies and the difference between the R and the S isomers suggest receptor-mediated uptake in receptor-rich tissue.