%0 Journal Article
%T Chromatography studies on bioaffinity of nine ligands of α1 adrenoceptor to α1D subtypes overexpressed in cell membrane
Chromatography studies on bio-affinity of nine ligands of α1-adrenoceptor to α1D subtypes overexpressed in cell membrane
%A ZHANG Dian
%A YUAN Bingxiang
%A DENG Xiuling
%A YANG Guangde
%A HE Langchong
%A ZHANG Youyi
%A HAN Qide
%A
%J 中国科学C辑(英文版)
%D 2004
%I Springer
%X To improve selectivity and specificity of cell membrane chromatography (CMC), the chromatography affinities of nine ligands of alpha1-adrenergic receptor(AR)to alpha1D-AR subtype were investigated. The human embryonic kidney (HEK) 293 cells expressed by cDNA of alpha1D-AR subtypes were cultured and cell membrane stationary phase (CMSP) was prepared. Then the interactions between ligands and alpha1D-AR in CMSP were investigated using CMC. The affinity rank order to alpha1D-AR subtype obtained from CMC for the nine alpha1-adrenoceceptor ligands is: prazosin, BMY7378, phentolamine, oxymetazoline, 5-methylurapidil, norepinephrine, phenylephrine, methoxamine, RS-17053. The affinity rank order is similar and correlates well with that obtained from others' radioligand binding assays (RBA). CMSP prepared by transfected HEK293 cells with alpha1-D-adrenoceptor cDNA and CMC method could be used to evaluate affinities of -drug-receptor and drug-receptor subtypes and to screen drugs selective to alpha1D-AR.
%K cell membrane
%K chromatography
%K α
%K 1-adrenergic receptor
%K α
%K 1D-adrenoceptor subtype
%U http://www.alljournals.cn/get_abstract_url.aspx?pcid=90BA3D13E7F3BC869AC96FB3DA594E3FE34FBF7B8BC0E591&jid=180CF3A72E750F3261A8A60EDC957784&aid=9A6F0E6B71D8BA82940A2BA7608BAA37&yid=D0E58B75BFD8E51C&vid=F4B561950EE1D31A&iid=E158A972A605785F&sid=09D368C679EC819B&eid=B9B90065CF5CD7F0&journal_id=1674-7305&journal_name=ScienceChina.Lifesciences&referenced_num=0&reference_num=17