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The vasopressin receptor (V1 subtype) is a G protein-coupled receptor located on vascular smooth muscle, where it mediates vasoconstriction in response to the endogenous hormone vasopressin. Terlipressin is a synthetic analogue of vasopressin that acts as an agonist at this receptor, used primarily to treat hepatorenal syndrome and bleeding esophageal varices. By stimulating the V1 receptor, terlipressin induces splanchnic vasoconstriction, increases effective circulating volume, and improves renal perfusion. Terlipressin is notable for its longer duration of action compared to vasopressin and its use as a first-in-class medication for acute kidney injury in hepatorenal syndrome. Safety concerns include risk of ischemia, respiratory failure, and potential fetal harm.
Vasopressin receptor agonism (V1 subtype): causes splanchnic and systemic vasoconstriction, increases mean arterial pressure, and reduces portal hypertension. Prodrug conversion: terlipressin is a prodrug for lysine-vasopressin, which also activates vasopressin receptors.
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