A Limited Vs a Transient AT1R Internalization Indicates that Distinct Mechanisms of AT1R Activation are Possible Article uri icon

abstract

  • We have shown that a 15,000 kDa polymer of Ang II (Ang II-POL) at maximal concentration upon a sustained action on the AT1R of rat coronary endothelial luminal membrane (CELM) produced sustained vasoconstriction and inotropic effects, and a lack of CELM AT1R internalization. In contrast, an equivalent concentration of the monomer Ang II (1 kDa) caused transient effects: desensitization, associated with the expected progressive internalization of CELM AT1R. It is accepted that AT1R Internalization into the cell, results from the CELM agonist-receptor complex sequestration into vesicles which depends on the internalization proteins: β-arrestin, clathrin and dynamin.

publication date

  • 2021-01-01