Chromatography studies on bio-affinity of nine ligands of alpha1-adrenoceptor to alpha1D subtypes overexpressed in cell membrane.
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Zhang D, Yuan B, Deng X, Yang G, He L, Zhang Y, Han Q
Chromatography studies on bio-affinity of nine ligands of alpha1-adrenoceptor to alpha1D subtypes overexpressed in cell membrane.
Sci China C Life Sci. 2004 Aug;47(4):376-81.
- PubMed ID
- 15493479 [ View in PubMed]
- Abstract
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.