Details

Autor(en) / Beteiligte

• Shu-yi WANG Yao SONG Ming XU Qi-hua HE Qi-de HAN You-yi ZHANG

Titel

Internalization and distribution of three α1-adrenoceptor subtypes in HEK293A cells before and after agonist stimulation

Ist Teil von

• Acta pharmacologica Sinica, 2007-03, Vol.28 (3), p.359-366

Erscheinungsjahr

2007

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• Aim： To examine the subcellular distribution of the 3 α1-adrenoceptor （α1-AR） subtypes and their internalization and trafficking upon agonist stimulation in human embryonic kidney 293A cells. Methods： Confocal real-time imaging, enzyme linked immunosorbent assay （ELISA） and whole cell [^3H]-prazosin binding assay were applied to detect the distribution and localization of the 3 α1-AR subtypes. Results： （α1A-AR was found both on the cell surface and in the cytoplasm; α1B- AR, however, was predominantly detected on the cell surface, while α1D-AR was detected mainly in the intracellular compartments. After stimulation with phenylephrine, localization changes were detected by confocal microscopy for α1A- and α1B-AR, but the localization of α1D-AR were unaffected. Phenylephrine stimulation promoted a more rapid internalization of α1B-AR than α1A-AR, α1D-AR internalization was detected only by ELISA. Whole cell [^3H]-prazosin binding assay showed that α1A-AR functional receptors were detected both on the cell surface and in the cytoplasm; α1B-AR, however, were detected predominantly on the cell surface, while α1D-AR were detected mainly in intracellular compartments. Phenylephrine stimulation promoted internalization of α1A- and α1B-AR. Conclusion： Phenylephrine stimulation induced changes in the localization of the 3 α1-AR.