Chromatography studies on bioaffinity of nine ligands of α1 adrenoceptor to α1D subtypes overexpressed in cell membrane |
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Authors: | Zhang Dian Yuan Bingxiang DENG Xiuling Yang Guangde HE Langchong ZHANG Youyi Han Qide |
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Institution: | 1. School of Medicine,Xi'an Jiaotong University,Xi'an 710061,China 2. College of pharmacy,Xi'an Jiaotong University,Xi'an 710061,China 3. Third Hospital,Beijing University,Beijing 100083,China |
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Abstract: | To improve selectivity and specificity of cell membrane chromatography (CMC), the chromatography affinities of nine ligands
of α1-adrenergic receptor(AR)to α1D-AR subtype were investigated. The human embryonic kidney (HEK) 293 cells expressed by cDNA of α1D-AR subtypes were cultured and cell membrane stationary phase (CMSP) was prepared. Then the interactions between ligands and
α1D-AR in CMSP were investigated using CMC. The affinity rank order to α1D-AR subtype obtained from CMC for the nine α1-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 α1D-adrenoceptor cDNA and CMC method could be used to evaluate affinities of drug-receptor and drug-receptor subtypes and to
screen drugs selective to α1D-AR. |
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Keywords: | cell membrane chromatography α1-adrenergic receptor α1D-adrenoceptor subtype |
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