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The Sound of Evolution
Tolvaptan
托伐普坦
Mechanism of action:
Tolvaptan 是一種選擇性抗利尿激素 V₂ 受體拮抗劑（selective vasopressin V₂ receptor antagonist）。Tolvaptan 會選擇性拮抗腎臟集尿管主細胞上的 V₂ 受體（Gs 蛋白偶聯受體），阻止抗利尿激素（arginine vasopressin）與該受體結合，而抑制水通道蛋白 2（aquaporin-2）轉位至集尿管腔側膜，使水分再吸收顯著下降。
Reference(s):
1. Gheorghiade M et al. (2005). Pharmacology of new agents for acute heart failure syndromes. Am J Cardiol.
2. Ambrosy A et al. (2011). Tolvaptan for the treatment of heart failure: a review of the literature. Expert Opin Pharmacother.
3. Yi S et al. (2012). Pharmacokinetics and pharmacodynamics of oral tolvaptan administered in 15- to 60-mg single doses to healthy Korean men. J Cardiovasc Pharmacol.
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