Meng Y, Hu J, el-Fakahany E E
Department of Pharmacology and Toxicology, University of Maryland School of Pharmacy, Baltimore 21201.
Membr Biochem. 1990 Oct-Dec;9(4):293-300. doi: 10.3109/09687689009025848.
We investigated the potential ability of p-fluoro-hexahydro-sila-difenidol (p-F-HHSiD) to discriminate between M1 and M3 muscarinic receptor subtypes using Chinese hamster ovary cells stably transfected with the genes encoding the two receptors. Both radioligand binding and functional assays were utilized for this purpose. In contrast to initial reports of a 14-fold selectivity of this antagonist for M3 versus M1 receptors, we have detected a qualitatively similar selectivity that was markedly smaller in magnitude.
我们使用稳定转染了编码这两种受体基因的中国仓鼠卵巢细胞，研究了对氟六氢硅二苯哌啶（p-F-HHSiD）区分M1和M3毒蕈碱受体亚型的潜在能力。为此采用了放射性配体结合和功能测定两种方法。与最初报道的该拮抗剂对M3受体与M1受体有14倍的选择性不同，我们检测到的定性相似的选择性在程度上明显更小。
