Differential phosphorylation, desensitization, and internalization of α1A-adrenoceptors activated by norepinephrine and oxymetazoline.

@article{Akinaga2013DifferentialPD,
  title={Differential phosphorylation, desensitization, and internalization of α1A-adrenoceptors activated by norepinephrine and oxymetazoline.},
  author={Juliana Akinaga and Vanessa R Lima and Luiz Ricardo de Almeida Kiguti and Fl{\'a}via Hebeler-Barbosa and R J Alc{\'a}ntara-Hern{\'a}ndez and Jes{\'u}s Adolfo Garc{\'i}a-S{\'a}inz and Andr{\'e} Sampaio Pupo},
  journal={Molecular pharmacology},
  year={2013},
  volume={83 4},
  pages={870-81}
}
Loss of response on repetitive drug exposure (i.e., tachyphylaxis) is a particular problem for the vasoconstrictor effects of medications containing oxymetazoline (OXY), an α1-adrenoceptor (AR) agonist of the imidazoline class. One cause of tachyphylaxis is receptor desensitization, usually accompanied by phosphorylation and internalization. It is well established that α1A-ARs are less phosphorylated, desensitized, and internalized on exposure to the phenethylamines norepinephrine (NE… CONTINUE READING