Page 3
Antagonists at the AT1 receptor (sartans)
The AT1 receptor mediates several effects which lead to an increase in blood pressure:
(click for list)
Cell surface receptor
G protein-coupled receptor (Gq/11)
Contraction of vascular smooth muscle (vasoconstriction)
Increased release of catecholamines from sympathetic neurones (and hence vasoconstriction)
Increased release of aldosterone by zona glomerulosa cells of the adrenal cortex (and hence hypervolaemia)
Increased reabsorption of Na+ from the renal proximal convoluted tubule (and hence hypervolaemia; see Physiology chapter on long term control of blood pressure)
The sartans:
Are competitive antagonists at the AT1 receptor. By blocking the effects of AT1 receptor activation,
they usefully lower the blood pressure...
